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FGFR1/DDR2 inhibitor 1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
FGFR1/DDR2 inhibitor 1图片
CAS NO:2308497-58-5
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
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。
Cas No.2308497-58-5
分子式C28H22F3N5O
分子量501.5
溶解度DMSO : 250 mg/mL (498.50 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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

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].

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].

[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.