| Bioactivity | IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies[1]. |
| Invitro | IHMT-TRK-284 (Compound 34) (0-10 µM, 72 h) shows antiproliferative effects against BaF3 cells, a panel of kinase transformed BaF3 cells, and KM-12-LUC cells[1].IHMT-TRK-284 (0-10 µM, 24 h) induces apoptosis and arrests the cell cycle into G0/G1 phase in KM-12-LUC cells[1].IHMT-TRK-284 exerts its inhibitory effect to the colon cancer cells through on-target inhibition of TRK[1].IHMT-TRK-284 could overcome drug resistant mutants including V573M and F589L in the ATP binding pocket as well as G667C/S in the DFG region[1].IHMT-TRK-284 shows selectivity over VEGFR2 kinase[1]. Cell Proliferation Assay[1] Cell Line: |
| In Vivo | IHMT-TRK-284 (Compound 34) (40 and 80 mg/kg; p.o.; daily, 10 days) shows good in vivo PK and antitumor efficacy properties[1]. Animal Model: |
| Name | IHMT-TRK-284 |
| CAS | 2416844-79-4 |
| Formula | C25H27N7OS |
| Molar Mass | 473.59 |
| 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]. Beilei Wang, et al. Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistan |
IHMT-TRK-284
CAS: 2416844-79-4 F: C25H27N7OS W: 473.59
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.
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