Sotorasib (Synonyms: 索托拉西布; AMG-510)

目录号: HY-114277 纯度: 99.75%: Data Sheet SDS COA 产品使用指南
FAQs
技术支持

Sotorasib (AMG-510) 是一种有效的，口服生物可利用的，选择性的 KRAS G12C 共价抑制剂。Sotorasib 将 KRAS G12C 锁定在非活跃的 GDP 约束状态。Sotorasib 导致 KRAS G12C 突变的局部晚期或转移性非小细胞肺癌 (NSCLC) 的消退。

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CAS No. : 2296729-00-3

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1727	In-stock
1 mg	￥500	In-stock
2 mg	￥700	In-stock
5 mg	￥1400	In-stock
10 mg	￥2400	In-stock
25 mg	￥3840	In-stock
50 mg	￥5500	In-stock
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Customer Review

Other Forms of Sotorasib:

MCE 顾客使用本产品发表的 89 篇科研文献

Cell Viability Assay

: Sotorasib purchased from MCE. Usage Cited in: Mol Cancer. 2023 May 20;22(1):86. [Abstract]; Sotorasib (20 nM; 48 h) in combination with Fedratinib (1 μM; 48 h) inhibits KRASG12C in H358 and MiaPaca2 cells, activates STAT3, and induces specific apoptosis, indicating cytotoxic effects.

: Sotorasib purchased from MCE. Usage Cited in: Mol Cancer. 2023 May 20;22(1):86. [Abstract]; Sotorasib (5-100 nM; 48 h) can inhibit the proliferation of H1792, H2030, H358, H23, and MiaPaca2 cells. The inhibitory effect is more significant when combined with Fedratinib (HY-10409) (0.25-1 μM).

: Sotorasib purchased from MCE. Usage Cited in: J Biol Chem. 2023 Feb;299(2):102842.; Sotorasib (1 μM) strongly downregulates survival protein Survivin in MIA PaCa-2 cells.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC)^[1]^[2]^[3]^[4]^[5]^[6].

IC₅₀ & Target^[1]

KRAS(G12C)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	36.5 μM Compound: (R)-38; AMG-510	Antiproliferative activity against human A549 cells harboring KRAS G12S point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human A549 cells harboring KRAS G12S point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31820981]
A549	IC₅₀	50 μM Compound: 2; AMG510	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant measured after 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant measured after 72 hrs by CCK-8 assay	[PMID: 35007863]
A549	IC₅₀	> 10 μM Compound: 2; AMG510	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as growth inhibition measured after 72 hrs by SRB assay	[PMID: 33309163]
ASPC1	IC₅₀	> 10 μM Compound: AMG510	Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
HEK-293T	IC₅₀	> 10 μM Compound: AMG510	Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
HepG2	IC₅₀	> 10 μM Compound: AMG510	Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
MIA PaCa-2	IC₅₀	0.005 μM Compound: (R)-38; AMG-510	Antiproliferative activity against human MIAPaCa2 cells harboring KRAS G12C point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human MIAPaCa2 cells harboring KRAS G12C point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31820981]
MIA PaCa-2	IC₅₀	0.018 μM Compound: AMG510	Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
MIA PaCa-2	IC₅₀	0.022 μM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell growth Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell growth	[PMID: 36621179]
MIA PaCa-2	IC₅₀	0.029 μM Compound: 2; AMG510	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 33309163]
MIA PaCa-2	IC₅₀	13 nM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay	[PMID: 38316747]
MIA PaCa-2	IC₅₀	37 nM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days by CCK8 assay	[PMID: 38316747]
MIA PaCa-2	IC₅₀	6 nM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay	[PMID: 38316747]
MIA PaCa-2	IC₅₀	> 10 nM Compound: AMG510	Cytotoxicity against human MIA PaCa-2 cells incubated for 48 hrs by CCK-8 assay Cytotoxicity against human MIA PaCa-2 cells incubated for 48 hrs by CCK-8 assay	[PMID: 38593589]
MIA PaCa-2	IC₅₀	> 40 μM Compound: AMG510	Cytotoxicity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
NCI-H1373	IC₅₀	355.7 nM Compound: AMG-510	Cytotoxicity against human NCI-H1373 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1373 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1373	IC₅₀	> 10000 nM Compound: AMG-510	Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1792	IC₅₀	3000 nM Compound: AMG-510	Cytotoxicity against human NCI-H1792 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1792 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1792	IC₅₀	> 10000 nM Compound: AMG-510	Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1975	IC₅₀	> 10 μM Compound: 2; AMG510	Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as growth inhibition measured after 72 hrs by SRB assay	[PMID: 33309163]
NCI-H2122	IC₅₀	530.3 nM Compound: AMG-510	Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H2122	IC₅₀	90.5 nM Compound: AMG-510	Cytotoxicity against human NCI-H2122 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H2122 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H23	IC₅₀	111.5 nM Compound: 2; AMG510	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay	[PMID: 35007863]
NCI-H23	IC₅₀	1500 nM Compound: AMG-510	Cytotoxicity against human NCI-H23 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H23 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H23	IC₅₀	> 10000 nM Compound: AMG-510	Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H358	EC₅₀	6 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 Antiproliferative activity against human NCI-H358	[PMID: 36300829]
NCI-H358	EC₅₀	6.4 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay	[PMID: 36300829]
NCI-H358	IC₅₀	0.001 μM Compound: 1	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay	[PMID: 37395055]
NCI-H358	IC₅₀	0.012 μM Compound: AMG510	Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
NCI-H358	IC₅₀	1 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay	[PMID: 38316747]
NCI-H358	IC₅₀	10 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells incubated for 6 days by CCK8 assay Antiproliferative activity against human NCI-H358 cells incubated for 6 days by CCK8 assay	[PMID: 38316747]
NCI-H358	IC₅₀	213 nM Compound: AMG-510	Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H358	IC₅₀	3 nM Compound: AMG-510	Cytotoxicity against human NCI-H358 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H358 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H358	IC₅₀	4 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay	[PMID: 38316747]
NCI-H358	IC₅₀	8.4 nM Compound: 2; AMG510	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay	[PMID: 35007863]
NCI-H358	IC₅₀	< 0.016 μM Compound: 2; AMG510	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by SRB assay	[PMID: 33309163]
NCI-H358	IC₅₀	< 0.03 μM Compound: 16, AMG510	Antiproliferative activity against human NCI-H358 cells Antiproliferative activity against human NCI-H358 cells	[PMID: 32910655]
NCM460	IC₅₀	> 40 μM Compound: AMG510	Cytotoxicity against human NCM460 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human NCM460 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
PANC-1	IC₅₀	> 40 μM Compound: AMG510	Cytotoxicity against human PANC-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human PANC-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
PANC-1	IC₅₀	> 40 μM Compound: AMG510	Cytotoxicity against human PANC-1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human PANC-1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
SW837	IC₅₀	2 nM Compound: AMG-510	Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay	[PMID: 38316747]
SW837	IC₅₀	3 nM Compound: AMG-510	Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay	[PMID: 38316747]
SW837	IC₅₀	9 nM Compound: AMG-510	Antiproliferative activity against human SW837 cells incubated for 6 days by CCK8 assay Antiproliferative activity against human SW837 cells incubated for 6 days by CCK8 assay	[PMID: 38316747]

体外研究
(In Vitro)

在细胞测定中，Sotorasib (AMG-510) 共价修饰 KRAS G12C 并抑制 KRAS G12C 信号传导，通过所有 KRAS p.G12C 突变细胞系中的 ERK1/2 (p-ERK) 磷酸化来测量^[2]。
Sotorasib (AMG-510；1-10 μM；72 小时) 也有效损害 NCI-H358 和 MIA PaCa-2 中的细胞活力，IC₅₀ 分别为 0.006 μM 和 0.009 μM。非 KRASG12C 细胞系对 Sotorasib (IC₅₀>7.5 μM) 不敏感^[3]。
Sotorasib (AMG-510) (0-50 μM，72 小时) 可抑制细胞生长，并与 Cisplatin (HY-17394) 在 H23 和 H358 细胞中产生协同作用^[5]。
Sotorasib (AMG-510) (100 nM，4-72 小时) 对活性 KRAS 具有持续抑制作用，但仍能观察到 RAS-MAPK 的自适应反馈再激活^[6]。

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

Cell Viability Assay^[3]

Cell Line:	NCI-H358 and MIA PaCa-2 cells
Concentration:	1-10 μM
Incubation Time:	72 hours
Result:	Potently impaired cellular viability in both NCI-H358 and MIA PaCa-2 (IC₅₀=~0.006 μM and ~0.009 μM respectively).

Cell Viability Assay^[5]

Cell Line:	NCI-H23 (H23) and NCI-H358 (H358) cells (Lung adenocarcinoma cell lines harbor KRAS G12C mutations)
Concentration:	0-50 μM
Incubation Time:	72 h
Result:	The IC₅₀ values in H358 and H23 cell lines were 0.0818 μM, 0.6904 μM, respectively. Had a synergistic effect with Cisplatin (HY-17394).

Western Blot Analysis^[6]

Cell Line:	H358, MGH1088-1, MGH1062, MIA PaCa-2, B8182, LIM2099, SW837, SW1463 (KRAS-^G12C mutant cell lines)
Concentration:	100 nM
Incubation Time:	4, 24, 48, 72 h
Result:	Showed effective inhibition of the MAPK pathway at 4 h, comparable rapid and robust reactivation of RAS-MAPK signaling was observed, such that phospho-ERK levels returned to an average of ~75% of baseline levels by just 72 h. Adaptive feedback is likely to be a key driver of resistance.

体内研究
(In Vivo)

在临床前肿瘤模型中，Sotorasib (AMG-510) 快速且不可逆地结合 KRAS G12C，持久抑制丝裂原活化蛋白激酶 (MAPK) 信号通路。Sotorasib (口服；每天一次) 能够在 KRAS G12C 癌症小鼠模型中诱导肿瘤消退^[3]。
Sotorasib (AMG-510) (30 mg/kg；口服；每日一次，共持续 28 天) 可减小 NCI-H358 细胞衍生异种移植小鼠模型中的肿瘤大小，并与 Cisplatin 具有协同作用^[5]。

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

Animal Model:	Balb/C nude mice (injected with H358 cells under the skin)^[5]
Dosage:	30 mg/kg
Administration:	Oral gavage (p.o.); daily for 28 days
Result:	The mean tumor volume were 426.66mm³. Reduced tumor size, and had a synergistic effect with Cisplatin. Had little effects on body weight.

Clinical Trial

分子量

560.59

Formula

C₃₀H₃₀F₂N₆O₃

CAS 号

2296729-00-3

性状

固体

颜色

White to yellow

中文名称

索托拉西布

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (89.19 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)

H₂O 中的溶解度 : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7838 mL	8.9192 mL	17.8383 mL
5 mM	0.3568 mL	1.7838 mL	3.5677 mL
10 mM	0.1784 mL	0.8919 mL	1.7838 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, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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 (3.71 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 (3.71 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 (3.71 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。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： 20% HP-β-CD in Saline
Solubility: 10 mg/mL (17.84 mM); 悬浊液; 超声助溶

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

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

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

纯度 & 产品资料

纯度: 99.75%

选择批次：

Data Sheet (655 KB) SDS (393 KB)

COA (293 KB) HNMR (313 KB) RP-HPLC (206 KB) LCMS (93 KB) 元素分析报告 (215 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.

[2]. Karen Rex, et al. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.

[3]. Canon J, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223. [Content Brief]

[4]. Brian A. Lanman, et al.Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors. Cancer Chemistry.

[5]. Wu LL, et al. AMG-510 and cisplatin combination increases antitumor effect in lung adenocarcinoma with mutation of KRAS G12C: a preclinical and translational research. Discov Oncol. 2023 Jun 7;14(1):91. [Content Brief]

[6]. Ryan MB, et al. KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy. Cell Rep. 2022 Jun 21;39(12):110993. [Content Brief]

Sotorasib 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

H₂O / DMSO	1 mM	1.7838 mL	8.9192 mL	17.8383 mL	44.5959 mL
	5 mM	0.3568 mL	1.7838 mL	3.5677 mL	8.9192 mL
	10 mM	0.1784 mL	0.8919 mL	1.7838 mL	4.4596 mL
	15 mM	0.1189 mL	0.5946 mL	1.1892 mL	2.9731 mL
	20 mM	0.0892 mL	0.4460 mL	0.8919 mL	2.2298 mL
	25 mM	0.0714 mL	0.3568 mL	0.7135 mL	1.7838 mL
	30 mM	0.0595 mL	0.2973 mL	0.5946 mL	1.4865 mL
	40 mM	0.0446 mL	0.2230 mL	0.4460 mL	1.1149 mL
	50 mM	0.0357 mL	0.1784 mL	0.3568 mL	0.8919 mL
DMSO	60 mM	0.0297 mL	0.1487 mL	0.2973 mL	0.7433 mL
DMSO	80 mM	0.0223 mL	0.1115 mL	0.2230 mL	0.5574 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

Sotorasib2296729-00-3AMG-510索托拉西布AMG510AMG 510RasNSCLCKRASG12Canti-tumourcovalentregressionmutationGDP-boundphosphorylationInhibitorinhibitorinhibit

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Sotorasib (Synonyms: 索托拉西布; AMG-510)

Customer Review

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Sotorasib 相关抗体

MCE 顾客使用本产品发表的 89 篇科研文献

Sotorasib 相关产品

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