| Bioactivity | FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively[1]. |
| Invitro | FGFR-IN-9 (Compound 19) (0-2 mM; 72 h) 抑制 HUH7 细胞，IC50 为 94.7±28.6 nM，抑制 Ba/F3 FGFR4WT 和 Ba/F3 FGFR4V550L 细胞增殖，IC50 分别为 82.5 ± 19.2 nM 和 260.0 ± 50.2 nM[1]。FGFR-IN-9 (0-400 nM; 4 h) 抑制 FGFR 信号通路[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | FGFR-IN-9 (Compound 19) (30 and 45 mg/kg; i.g.; daily for 3 weeks) 在 HUH7 异种移植小鼠模型中显示出抗肿瘤活性[1]。In Vivo Pharmacokinetic Profile Data for FGFR-IN-9 (Compound 19) [1] FGFR-IN-9 |
| Name | FGFR-IN-9 |
| Formula | C25H28N6O3S |
| Molar Mass | 492.59 |
| 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]. Xie W, et al. Discovery of 2-Amino-7-sulfonyl-7 H-pyrrolo [2, 3-d] pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation. Journal of Medicinal Chemistry, 2022. |