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FGFR1/DDR2 inhibitor 1

CAS No. : 2308497-58-5

MCE 国际站：FGFR1/DDR2 inhibitor 1

产品活性：FGFR1/DDR2 inhibitor 1 是具有口服活性的成纤维细胞生长因子受体 1 (FGFR1) 和盘状蛋白域受体 2 (DDR2) 的抑制剂，其对 FGFR1 和 DDR2 的IC₅₀ 值分别为 31.1 nM、3.2 nM。具有抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR  |  Discoidin Domain Receptor

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 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).

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%.

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