Selitrectinib (Synonyms: LOXO-195)

目录号: HY-101977 纯度: 99.74%: Data Sheet SDS COA 产品使用指南
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Selitrectinib (LOXO-195) 是一种二代原肌凝蛋白相关激酶 (TRK) 抑制剂，其对 TRKA 和 TRKC 的 IC₅₀ 值分别为 0.6 nM 和 <2.5 nM。

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Selitrectinib Chemical Structure

CAS No. : 2097002-61-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥835	In-stock
1 mg	￥434	In-stock
5 mg	￥998	In-stock
10 mg	￥1500	In-stock
25 mg	￥2900	In-stock
50 mg	￥4300	In-stock
100 mg	￥5600	In-stock
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500 mg		询价

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Customer Review

Other Forms of Selitrectinib:

(3aR)-Selitrectinib 询价
Selitrectinib (Standard) 询价

MCE 顾客使用本产品发表的 5 篇科研文献

Selitrectinib 相关产品

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TrkA TrkB TrkC Trk

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC₅₀s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively^[1].

IC₅₀ & Target^[1]

TrkA

0.6 nM (IC₅₀)

TrkC

<2.5 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.001 μM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.001 μM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.0082 μM Compound: LOXO-195	Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.013 μM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.013 μM Compound: LOXO-195	Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.018 μM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay	[PMID: 35080890]
BaF3	IC₅₀	0.018 μM Compound: LOXO-195	Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
BaF3	IC₅₀	0.041 μM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	1 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	1.1 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKA assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKA assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	1.2 nM Compound: 3; LOXO-195	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	1.35 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.36 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.4 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKB assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKB assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	1.6 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKC assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKC assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	1.7 nM Compound: 3; LOXO-195	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	10.28 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	10.5 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	10.7 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	10.98 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	109 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	113.1 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
BaF3	IC₅₀	12 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
BaF3	IC₅₀	12.6 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA F589L mutant assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA F589L mutant assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	13 nM Compound: 3	Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA G595R mutant assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA G595R mutant assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	15 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	15.2 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
BaF3	IC₅₀	16.7 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	16.7 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
BaF3	IC₅₀	17 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	17.2 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	18 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	2.32 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.4 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	2.7 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	22.23 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	23.2 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
BaF3	IC₅₀	24.4 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA G667A mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA G667A mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	25.4 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	26.11 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	26.38 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	27.8 nM Compound: selitrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition	[PMID: 36395392]
BaF3	IC₅₀	28.2 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	3.2 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	3.39 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	30 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	30.66 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	31.5 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	35.79 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	36.7 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	37 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	4.15 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	4.9 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	41.06 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	41.4 nM Compound: 3; LOXO-195	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	42.04 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	423.15 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	48.16 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.08 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.2 nM Compound: 3; LOXO-195	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	5.7 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	50 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	6.8 nM Compound: LOXO-195	Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay	[PMID: 34253025]
BaF3	IC₅₀	7.48 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	72.6 nM Compound: 3	Antiproliferative activity aganist mouse BAF3 cells transfected with LMNA-TRKA G667C mutant assessed as cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity aganist mouse BAF3 cells transfected with LMNA-TRKA G667C mutant assessed as cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34668694]
BaF3	IC₅₀	8.2 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	8.5 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	84.5 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
BaF3	IC₅₀	9 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	95.6 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
BaF3	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	> 10000 nM Compound: 3	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	> 10000 nM Compound: LOX0195	Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay	[PMID: 35080890]
BaF3	IC₅₀	> 20000 nM Compound: Selitrectinib	Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
KM12	IC₅₀	0.0028 μM Compound: LOXO-195	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35617855]
KM12	IC₅₀	1.7 nM Compound: Selitrectinib	Antiproliferative activity against human KM12 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
KM12	IC₅₀	2.9 nM Compound: Selitrectinib	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 37030091]
KM12	IC₅₀	6.8 nM Compound: Selitrectinib	Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
KM12	IC₅₀	<= 5 nM Compound: LOXO-195	Inhibition of cell proliferation in TPM3-NTRK1 fusion positive human KM12 cells incubated for 72 hrs by DAPI staining based analysis Inhibition of cell proliferation in TPM3-NTRK1 fusion positive human KM12 cells incubated for 72 hrs by DAPI staining based analysis	[PMID: 28578312]
KM12	IC₅₀	<= 5 nM Compound: LOXO-195	Antiproliferative activity against TrK fused human KM12 cells Antiproliferative activity against TrK fused human KM12 cells	[PMID: 34253025]
MCF7	IC₅₀	> 10000 nM Compound: Selitrectinib	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 39033612]
MCF7	IC₅₀	> 20000 nM Compound: Selitrectinib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 38029466]
NIH3T3	GI₅₀	1.6 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells transfected with wild type TRKA assessed as cell growth inhibition Antiproliferative activity against mouse NIH3T3 cells transfected with wild type TRKA assessed as cell growth inhibition	[PMID: 38389874]
NIH3T3	GI₅₀	17.5 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	2 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells expressing wild type TRKC mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing wild type TRKC mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]
NIH3T3	GI₅₀	25 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells expressing TRKA G667S mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing TRKA G667S mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]
NIH3T3	GI₅₀	29 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells harbouring TRKA V573M mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells harbouring TRKA V573M mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	45.5 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells expressing TRKC G623R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing TRKC G623R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]
NIH3T3	GI₅₀	64 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells transfected with TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells transfected with TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	7 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells harbouring TRKC G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method Antiproliferative activity against mouse NIH3T3 cells harbouring TRKC G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method	[PMID: 38389874]
NIH3T3	GI₅₀	9 nM Compound: 19; LOXO-195	Antiproliferative activity against mouse NIH3T3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38389874]

体外研究
(In Vitro)

Selitrectinib (LOXO-195) 显示出与野生型 TRKA、TRKB 和 TRKC 激酶结构域的强结合力。Selitrectinib (LOXO-195) 在激酶活性测定中表现出强效 (IC₅₀<1 nM) 抑制活性。值得注意的是，Selitrectinib (LOXO-195) 对 TRKA G595R、TRKC G623R 和 TRKA G667C 具有低纳摩尔抑制活性，IC₅₀ 范围为 2.0-9.8 nM。在 Selitrectinib (LOXO-195) 浓度为 1 μM 时，对 228 种体外激酶进行了分析，该浓度比其对 TRKA 的 IC₅₀ (0.6 nM) 高约 1667 倍。 Selitrectinib (LOXO-195) 对 98% 的非 TRK 激酶的选择性高出 1000 倍以上。Selitrectinib (LOXO-195) 在含有 TRK 融合基因的 KM12、CUTO-3 和 MO-91 细胞系中表现出强效的细胞增殖抑制作用 (IC₅₀≤5 nM)^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

将稳定转染的 NIH-3T3 ΔTRKA 和 ΔTRKA-G595R 细胞皮下植入裸鼠侧腹。Selitrectinib 能有效降低ΔTRKA驱动的肿瘤中的磷酸化TRKA。在四种 TRKA 依赖性肿瘤模型 (ΔTRKA、ΔTRKA-G595R、ΔTRKAG667C 和 TPM3-NTRK1 融合阳性 KM12 结直肠癌细胞) 中，所有剂量的 Selitrectinib (LOXO-195) 均能抑制肿瘤生长 (相对于载体)。Larotrectinib 对 KM12 和 NIH 3T3-ΔTRKA 肿瘤的抑制程度相似。任何药物治疗后，组内平均体重减轻均不超过 5%。Selitrectinib (LOXO-195) 对 TRK 蛋白表现出高选择性^[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

380.42

Formula

C₂₀H₂₁FN₆O

CAS 号

2097002-61-2

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 62.5 mg/mL (164.29 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6287 mL	13.1434 mL	26.2867 mL
5 mM	0.5257 mL	2.6287 mL	5.2573 mL
10 mM	0.2629 mL	1.3143 mL	2.6287 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.47 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.47 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.47 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.90% ee.: 99.77%

选择批次：

Data Sheet (651 KB) SDS (393 KB)

COA (288 KB) HNMR (207 KB) LCMS (121 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Drilon A, et al. A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors. Cancer Discov. 2017 Sep;7(9):963-972. [Content Brief]

Cell Assay ^[1]	For assessment of cellular inhibition potency, cells are harvested per a standard protocol, counted and added to flat-bottom, collagen I-coated 96-well assay plates at 3×10⁴ cells/well (wild-type cell line) or 5×10⁴ cells/well (mutant cell lines) in 100 μL/well of DMEM growth medium containing 10% FBS. Plates are then incubated at room temperature for 30 minutes prior to an overnight incubation at 37°C with 5% CO₂. Next, cells are treated for 1 hour at 37°C, 5% CO₂ with TRK inhibitor compounds (e.g., Selitrectinib (LOXO-195)). Control wells contain either 0.25% DMSO alone or 1 μM larotrectinib or LOXO-195. Following compound incubation, growth medium is discarded and cells are lysed by addition of 60 μL/well of ice-cold lysis buffer containing protease and phosphatase inhibitors^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] The ΔTRKA, ΔTRKA-G595R, and ΔTRKA -G667C NIH-3T3 tumor cell lines (~2-3x10⁶ cells) and KM12 cells (5x10⁶ cells) are injected subcutaneously into the right flank of female nu/nu NCr mice. Tumors are allowed to grow to ~100-200 mm³ or ~500 mm³, and animals are randomized by tumor size into dosing groups of 5 (KM12), 7 (NIH 3T3 ΔTRKA variants) or 3-4 (for PK-PD) animals. Animals are dosed by oral gavage with vehicle, Selitrectinib (LOXO-195) in 1% carboxymethylcellulose/0.5% Tween-80 or larotrectinib in 100% Labrafac lipophile. All animals are obtained at 6-8 weeks of age, housed in groups of 5 and allowed a one-week acclimation period before cancer cell injection. Animals are dosed with vehicle twice daily, Selitrectinib (LOXO-195) at 30 mg/kg, 100 mg/kg and 300 mg/kg twice daily and larotrectinib at 60 mg/kg daily for 9-12 days. Body weight and tumor size are monitored after cell implantation and at regular intervals during dosing^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Drilon A, et al. A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors. Cancer Discov. 2017 Sep;7(9):963-972. [Content Brief]

Selitrectinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6287 mL	13.1434 mL	26.2867 mL	65.7168 mL
	5 mM	0.5257 mL	2.6287 mL	5.2573 mL	13.1434 mL
	10 mM	0.2629 mL	1.3143 mL	2.6287 mL	6.5717 mL
	15 mM	0.1752 mL	0.8762 mL	1.7524 mL	4.3811 mL
	20 mM	0.1314 mL	0.6572 mL	1.3143 mL	3.2858 mL
	25 mM	0.1051 mL	0.5257 mL	1.0515 mL	2.6287 mL
	30 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1906 mL
	40 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6429 mL
	50 mM	0.0526 mL	0.2629 mL	0.5257 mL	1.3143 mL
	60 mM	0.0438 mL	0.2191 mL	0.4381 mL	1.0953 mL
	80 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8215 mL
	100 mM	0.0263 mL	0.1314 mL	0.2629 mL	0.6572 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Selitrectinib2097002-61-2LOXO-195LOXO195LOXO 195Trk ReceptorTropomyosin related kinase receptorInhibitorinhibitorinhibit

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Selitrectinib (Synonyms: LOXO-195)

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