FGFR-IN-10

Names

[ Name ]:
FGFR-IN-10

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR

[Target]

CYP2C9:3.33 μM (IC50)

CYP2C19:18.75 μM (IC50)

CYP2D6:4.34 μM (IC50)

CYP3A4:0.69 μM (IC50)

FGFR2:104.1 nM (IC50)

V564F-FGFR2:43.6 nM (IC50)

[In Vitro]

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 Dose (mg/kg) Cmax (ng/mL) AUClast/D (h·mg/mL) T1/2 (h) Cl_obs (mL/min/kg) Vss_obs (L/kg) F (%) i.v. 5 / 664 1.02 26.0 1.2 / p.o. 10 2388 402 / / / 60.7

[References]

[1]. Zhu Wei, et al. Heterocyclic compound serving as FGFR inhibitor and application thereof: World Intellectual Property Organization, WO2022206939. 2022-10-06.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₃₀FN₉O₂

[ Molecular Weight ]:
543.60

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.