| Bioactivity | 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]. |
| Invitro | 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: |
| Name | TRK II-IN-1 |
| Formula | C29H31F3N8O |
| Molar Mass | 564.60 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Xiang S, et, al. Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114899. |