TRK II-IN-1 是一种有效的 II 型TRK抑制剂，抑制TRKA/B/CandTRKAG667C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。
| 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) |
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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. |
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| 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. |
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