| Bioactivity | H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity[1]. | ||||||||||||
| Invitro | H3B-6527 inhibits TAOK2, JNK2, and CSF1R with IC50s of 690 nM, >10000 nM, and >10000 nM, respectively[1]. H3B-6527 (10-10000 nM; 72 hours) results in a GI50 value of 25 nM[1]. H3B-6527 (10-10000 nM; 72 hours) leads cell death in HCC cell lines[1]. H3B-6527 (0.1-1000 nM; 1 hour) decreases the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM[1]. H3B-6527 (1-1000 nM; 24 hours) causes a robust increase in CYP7A1 transcripts[1]. 0 --> H3B-6527 相关抗体: Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | H3B-6527 (10-300 mg/kg; orally; twice-daily; for 15 days) significantly inhibits tumor growth at the 300 and 100 mg/kg and does not inhibit tumor growth at 30 and 10 mg/kg[1]. Animal Model: | ||||||||||||
| Name | H3B-6527 | ||||||||||||
| CAS | 1702259-66-2 | ||||||||||||
| Formula | C29H34Cl2N8O4 | ||||||||||||
| Molar Mass | 629.54 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Joshi JJ, et al. H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven HepatocellularCarcinoma. Cancer Res. 2017 Dec 15;77(24):6999-7013. |