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FGFR1/DDR2 inhibitor 1

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Chemical Structure| 2308497-58-5 同义名 : -
CAS号 : 2308497-58-5
货号 : A1176996
分子式 : C28H22F3N5O
纯度 : 99%+
分子量 : 501.502
MDL号 : MFCD32067903
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(498.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 FGFR1/DDR2 inhibitor 1 is an orally active FGFR1 and DDR2 inhibitor with IC50 values of 31.1 nM and 3.2 nM, respectively. In the concentration range of 25-200 μM for 2 h, FGFR1/DDR2 inhibitor 1 significantly inhibited FGFR2 phosphorylation in SNU16 cells in a dose-dependent manner. In H2286 cells, FGFR1/DDR2 inhibitor 1 inhibited DDR2 phosphorylation in a dose-dependent manner at a concentration range of 60-250 μM for 2 h. FGFR1/DDR2 inhibitor 1 significantly inhibited the proliferation of FGFR-driven cancer cell lines, and the IC50 values of FGFR1/DDR2 inhibitor 1 were significantly lower than those of FGFR-driven cancer cell lines, and the IC50 values of FGFR2 inhibitor 1 were higher than those of FGFR-driven cancer cell lines, as KG-1, SNU-16, NCI-H716 and UMUC14 with IC50 values of 108.4, 93.4, 31.8 and 306.6 nM, respectively. FGFR1/DDR2 inhibitor 1 showed significant activity against the DDR2-driven cancer cell line NCI-H2286 (IC50=93.0 nM)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.94mL

3.99mL

1.99mL
参考文献

[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.