Bioactivity | FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models[1]. |
Invitro | FGFR-IN-11 (0.3 nM-20 μM, 72 h) 以纳摩尔活性抑制多种癌细胞生长[1]。 Cell Viability Assay[1] Cell Line: |
In Vivo | FGFR-IN-11 (60 mg/kg, 口服, 每天一次, 21 天) 在雌性裸鼠的 Huh-7 或 NCI-H1581 异种移植瘤模型中显著抑制肿瘤生长并且不影响小鼠体重。[1] Animal Model: |
Name | FGFR-IN-11 |
CAS | 2658488-68-5 |
Formula | C28H29ClN4O4 |
Molar Mass | 521.01 |
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]. Hu S, et al. Discovery and Structural Optimization of Novel Quinolone Derivatives as Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors. J Med Chem. 2023 Jul 13;66(13):8858-8875. |