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TRK II-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TRK II-IN-1图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
TRK II-IN-1 是一种有效的 II 型TRK抑制剂,抑制TRKA/B/CandTRKAG667CIC50值分别为3.3,6.4,4.3 和 9.4 nM。TRK II-IN-1还可以抑制FLT3RETVEGFR2IC50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。
生物活性

TRKII-IN-1 is a potent type IITRKinhibitor, withIC50s of 3.3, 6.4, 4.3 and 9.4 nM, forTRKA/B/CandTRKAG667C, respectively.TRKII-IN-1 also inhibitsFLT3,RET, andVEGFR2withIC50s of 1.3, 9.9, and 71.1 nM, respectively.TRKII-IN-1 can be used for the research ofTRKdriven 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 (化合物 12d) (1 μM) 显示出对 VEGFR2,RET,FLT3 激酶 90% 以上的抑制率,对 KIT,CSF1R,DDR1 和 DDR2 显示出接近 70% 左右的抑制率[1]
TRK II-IN-1 (72 h) 抑制 Ba/F3-CD74-TRKA,Ba/F3-ETV6-TRKB 和 Ba/F3-ETV6-TRKC 细胞增殖,IC50值分别为 26.1,44.7 和 15.7 nM[1]
TRK II-IN-1 (72 h) 抑制了 xDFG 和 SF 突变体 TRK 融合蛋白稳定转化的 Ba/F3 细胞的增殖,IC50值范围为 2.6 到 143.3 nM[1]
TRK II-IN-1 (0.4-500 nM; 48 h) 诱导 Ba/F3-CD74-TRKA 和 Ba/F3-CD74-TRKAG667C细胞凋亡[1]
TRK II-IN-1 (0.4-500 nM; 24 h) 可导致 Ba/F3-CD74-TRKA 和 Ba/F3-CD74-TRKAG667C细胞周期停滞在 G0/G1期[1]
TRK II-IN-1 (0.8-500 nM; 6 h) 以剂量依赖的方式抑制 TRKA,TRKAG667C激酶以及下游蛋白 AKT,ERK 和 PLCγ1的磷酸化[1]

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-TRKAG667Ccells
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-TRKAG667Ccell 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-TRKAG667Ccells
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

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.