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BFH772

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Chemical Structure| 890128-81-1 同义名 : -
CAS号 : 890128-81-1
货号 : A694724
分子式 : C23H16F3N3O3
纯度 : 98%
分子量 : 439.387
MDL号 : MFCD30534392
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(238.97 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
靶点

  • VEGFR2

    VEGFR2, IC50:3 nM
描述 BFH772 is an effective oral inhibitor of VEGFR2, targeting the kinase with an IC50 value of 3 nM. BFH772 exhibits high selectivity; it inhibits VEGFR2 with an IC50 of 3 nM and also targets B-RAF, RET, and TIE-2, though with a potency at least 40 times lower. BFH772 is inactive (IC50 > 10 μM; > 2 μM for cKIT) against all other tested tyrosine-specific and serine/threonine-specific protein kinases. In CHO cells, BFH772 inhibits VEGFR2 with an IC50 of 4.6±0.6 nM, and in HUVEC cells, it does so with an IC50 of 3 nM. It also inhibits the ligand-induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging from 30 to 160 nM. BFH772 is selective (IC50 values > 0.5 μM) against the kinases of EGFR, ERBB2, INS-R, and IGF-1R, as well as against the cytoplasmic BCR-ABL kinase.[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.38mL

2.28mL

1.14mL

22.76mL

4.55mL

2.28mL
参考文献

[1]Bold G, et al. A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis. J Med Chem. 2016 Jan 14;59(1):132-46.