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MedChemExpress - Model FGFR1/DDR2 ...

MedChemExpress - Model FGFR1/DDR2 inhibitor 1 - 2308497-58-5

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity[1].

FGFR1/DDR2 inhibitor 1

MCE China：FGFR1/DDR2 inhibitor 1

Brand：MedChemExpress (MCE)

Cat. No.HY-114311

CAS：2308497-58-5

Purity：98.26%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 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[1]. FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC50s 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)[1].

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[1]. 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%[1].

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

References：

[1]. Wang Q, et al. Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. Eur J Med Chem. 2019 Feb 1;163:671-689. [Content Brief]

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