2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. Trk-IN-20

Trk-IN-20 是一种 3- 乙烯基咪唑衍生物，是 Trk 抑制剂。Trk-IN-20 通过抑制磷酸化来抑制 Trk 激酶功能，抑制 TrkA/B/C 的 IC50s 分别为 1.6 nM、2.9 nM 和 2.0 nM。

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Trk-IN-20 Chemical Structure

Trk-IN-20 Chemical Structure

CAS No. : 2460924-63-2

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Trk-IN-20 相关抗体

Top Publications Citing Use of Products

查看 Trk Receptor 亚型特异性产品:

查看所有亚型
TrkA TrkB TrkC Trk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively[1].

IC50 & Target

TrkA

1.6 nM (IC50)

TrkB

2.9 nM (IC50)

TrkC

2.0 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
0.009 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.015 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.018 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.022 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.031 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.144 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.243 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.503 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
3.116 μM
Compound: 7mb
Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
体外研究
(In Vitro)

NTRK1 is a proto-oncogene in colon cancer, Trk inhibitors have been detected to against a variety of human cancers[1].
Trk-IN-20 (compound 7mb) (0.031, or 0.018 μM, respectively; 72 h) exhibits strong inhibition against the Larotrectinib-resistant cells with NTRK1-G667C or NTRK3-G696A mutations with IC50s of 0.031 and 0.018 μM, respectively[1].
Trk-IN-20 (compound 7mb) (9-22 nM; 72 h) inhibits BaF3 murine cells stably transformed with NTRK oncogenic fusions including CD74-NTRK1, ETV6-NTRK2 and ETV6-NTRK3 with IC50s of 15, 22, and 9 nM, respectively[1].
Trk-IN-20 (compound 7mb) (0.32, 1.6, 8, 40, 200; 6 h) inhibits activation of Trk and its downstream proteins in BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells[1].
Trk-IN-20 (compound 7mb) tightly bound to ATP-binding site of TrkA, TrkB, and TrkC with binding constant (Kd) values of 1.6, 3.1 and 4.9 nM, respectively[1].

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

Trk-IN-20 相关抗体:

Western Blot Analysis[1]

Cell Line: BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells
Concentration: 0, 0.32, 1.6, 8, 40, 200 nM
Incubation Time: 6 hours
Result: Inhibited the phosphorylation of TrkA/B/C and their downstream signaling molecules ERK, AKT, and PLC-γ1. And also induced partial degradation of Trk protein in BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells.
体内研究
(In Vivo)

Trk-IN-20 (compound 7mb) (p.o.; 10 mg/kg) shows short half-life of 1.39 hours and a low oral bioavailability of 8.79% in rats[1].

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

Animal Model: Pharmacokinetic Profile of Trk-IN-20 (Compound 7mb) in Rats[1]
Dosage:
Administration:
Result:
Route Dose (mg/kg) AUC0-∞ (μM.h) Cmax (μM) T1/2 (h) CL (L/h/kg) BA (%)
i.v. 2 3.69 6.77 1.39 1.44 /
p.o. 10 1.62 0.36 1.13 - 8.79
分子量

376.40

Formula

C22H18F2N4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Trk-IN-20 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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)
× = ×
C1   V1   C2   V2
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:

Trk-IN-202460924-63-2Trk ReceptorTropomyosin related kinase receptor3-Vinylindazoletropomyosin receptor kinaseTrkneurotrophic receptor tyrosine kinase geneNTRKfusioninhibitorresistancemutationInhibitorinhibit

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