TRK II-IN-1 是一种有效的 II 型
TRK抑制剂，抑制
TRKA/B/Cand
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。
| 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].
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| 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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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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