PeptideDB

FGFR-IN-10

CAS: 2847092-41-3 F: C28H30FN9O2 W: 543.60

FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mut
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Bioactivity FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively[1].
Invitro FGFR-IN-10 (compound 115) (5 μM; 0-240 min) 在 SD 大鼠和人血液中具有稳定性,其全血半衰期均 (t1/2) >600 min[1]。 FGFR-IN-10 (0-10 μM; 72 h) 抑制 SNU-16 和 JMSU-1 细胞的生长,GI50 分别为 6 nM 和 24 nM[1]。
In Vivo FGFR-IN-10 (10 mg/kg; 口服; 单剂量) 在 SD 大鼠中表现出较强的口服活性,生物利用度为 60.7%[1]。在 SD 大鼠中的药代动力学分析[1]Route
Name FGFR-IN-10
CAS 2847092-41-3
Formula C28H30FN9O2
Molar Mass 543.60
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]. Zhu Wei, et al. Heterocyclic compound serving as FGFR inhibitor and application thereof: World Intellectual Property Organization, WO2022206939. 2022-10-06.