FGFR1/DDR2 inhibitor 1
规格
| Cas Number | 2308497-58-5 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 10mg 或 1mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 250 mg/mL (498.50 mM; Need ultrasonic) |
| 过滤标签 | FGFR,Discoidin Domain Receptor,Protein Tyrosine Kinase/RTK |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 物理形态 | 固体 |
| 生化和生理学机理 | FGFR1/DDR2 抑制剂 1 是一种具有口服活性的成纤维细胞生长因子受体 1（FGFR1）和 Discoindin 结构域受体 2（DDR2）抑制剂，其 IC 50 值分别为 31.1 nM 和 3.2 nM。抗肿瘤活性。 |
| 英文描述 |
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 ) |