2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor FLT3 VEGFR RET
  4. TRK II-IN-1

TRK II-IN-1 是一种有效的 II 型 TRK 抑制剂，抑制 TRKA/B/C and TRKAG667C 的 IC50 值分别为3.3，6.4，4.3 和 9.4 nM。TRK II-IN-1还可以抑制 FLT3，RET 和 VEGFR2，IC50 值分别为 1.3，9.9 和 71.1 nM。TRK II-IN-1 可用于研究 TRK 驱动的癌症。

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TRK II-IN-1 Chemical Structure

TRK II-IN-1 Chemical Structure

CAS No. : 2904690-41-9

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TRK II-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Trk Receptor 亚型特异性产品:

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TrkA TrkB TrkC Trk

查看 VEGFR 亚型特异性产品:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRK II-IN-1 is a potent type II TRK inhibitor, with IC50s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKAG667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC50s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers[1].

IC50 & Target[1]

TrkA

3.3 nM (IC50)

TrkB

6.4 nM (IC50)

TrkC

4.3 nM (IC50)

TRKAG667C

9.4 nM (IC50)

FLT3

1.3 nM (IC50)

RET

9.9 nM (IC50)

VEGFR2

71.1 nM (IC50)

体外研究
(In Vitro)

TRK II-IN-1 (compound 12d) (1 μM) demonstrates over 90% of kinase inhibition towards VEGFR2, RET, FLT3 and nearly 70% inhibition against Kit, CSF1R, DDR1 and DDR2[1].
TRK II-IN-1 (72 h) inhibits Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB and Ba/F3-ETV6-TRKC cells, with IC50s of 26.1, 44.7 and 15.7 nM, respectively[1].
TRK II-IN-1 (72 h) suppresses proliferation of a panel of Ba/F3 cells stably transformed with wild type, xDFG as well as solvent-front (SF) mutant TRK fusion proteins, with IC50s ranging from 2.6 to 143.3 nM[1].
TRK II-IN-1 (0.4-500 nM; 48 h) induces apoptosis of Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells[1].
TRK II-IN-1 (0.4-500 nM; 24 h) arrests cell cycle progression in the G0/G1 phase in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells[1].
TRK II-IN-1 (0.8-500 nM; 6 h) suppresses the phosphorylation of TRKA, TRKAG667C kinases, and their downstream AKT, ERK and PLCγ1 in a dose-dependent manner[1].

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

TRK II-IN-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions
Concentration: 0.4, 2, 10, 50 nM for Ba/F3-CD74-TRKA cells; 4, 20, 100, 500 nM for Ba/F3-CD74-TRKAG667C cells
Incubation Time: 48 hours
Result: Notable apoptotic cells (18.74% in 100 nM and 35.65% in 500 nM) were observed in Ba/F3-CD74-TRKA cells.
Induced Ba/F3-CD74-TRKAG667C cell apoptosis with 11.22% and 56.25% at the concentration of 10 nM and 50 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions
Concentration: 0.4, 2, 10, 50 nM for Ba/F3-CD74-TRKA cells; 4, 20, 100, 500 nM for Ba/F3-CD74-TRKAG667C cells
Incubation Time: 24 hours
Result: Arrested cell cycle progression in the G0/G1 phase.

Western Blot Analysis[1]

Cell Line: Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions
Concentration: 0.8, 4, 20, 100, 500 nM
Incubation Time: 6 hours
Result: Inhibited the activation of TRKA and downstream signaling.
分子量

564.60

Formula

C29H31F3N8O
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 II-IN-1 相关分类

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  • 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 II-IN-12904690-41-9Trk ReceptorFLT3VEGFRRETTropomyosin related kinase receptor Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Vascular endothelial growth factor receptorTRKAG667Csolvent-frontxDFGInhibitorinhibitorinhibit

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