FGFR1/DDR2 inhibitor 1 - 99%, high purity , CAS No.2308497-58-5

Item Number

F651919

• Synonyms: 3-(3-(1-Cyclopropyl-1H-pyrazol-4-yl)-1H-indazol-6-yl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide
• Specifications & Purity: ≥98%
• Biochemical and Physiological Mechanisms: FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2) , with IC 50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads

Product Description

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2) , with IC 50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity

In Vitro

FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 μM; 2 hours) significant inhibition of DDR2 phosphorylation in a dose-dependent manner in H2286 cells. FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC 50 s of 108.4, 93.4, 31.8 and 306.6 nM against KG-1, SNU-16, NCI-H716 and UMUC14 respectively. FGFR1/DDR2 inhibitor 1 demonstrates substantially activity against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

FGFR1/DDR2 inhibitor 1 (10-20 mg/kg; p.o.; once daily for 7 days) has profound anti-tumor efficacy in NCI-H1581 tumor model . SCID mice bearing NCI-H2286 tumors were randomized and treated with FGFR1/DDR2 inhibitor 1 at doses of 10 mg/kg for 10 consecutive days. FGFR1/DDR2 inhibitor 1 could suppress tumor growth with tumor growth inhibition rates (TGI) of 82.8% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice bearing NCI-H1581 tumors Dosage: 10 or 20 mg/kg Administration: P.o.; once daily for 7 days Result: Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition rates (TGI) of 59.7% and 98.1% at doses of 10 and 20 mg/kg, respectively.

Form:Solid

IC50& Target:FGFR1 31.1 nM (IC 50 ) DDR2 3.2 nM (IC 50 )