Information BFH772 is a novel potent oralVEGFR2inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM. Targets VEGFR2 (Cell-free assay) 3 nM In vitro BFH772 was highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 was highly selective, In addition to VEGFR2, it also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM. In vivo BFH772 all at 3 mg/kg orally dosed once per day potently inhibited melanoma growth (by 54−90% for primary tumor and 71−96% for metastasis growth). Cell Research(from reference) Cell lines:HUVEC endothelial cells Concentrations:0-10 nM Incubation Time:48 h
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BFH772
Dangerous GoodsCAS number:890128-81-1 molecular formula:C23H16F3N3O3
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | BCP18910 | MFCD30534392 | HMS3649L19 | T1IV236CVP | 6-[[6-(hydroxymethyl)-4-pyrimidinyl]oxy]-N-[3-(trifluoromethyl)phenyl]-1-naphthalenecarboxamide | AKOS032945111 | HY-100419 | s8188 | A915077 | BDBM50270425 | EX-A1157 | UNII-T1IV236CVP | SCHEMBL987715 | | ||
| CAS number | 890128-81-1 | molecular formula | C23H16F3N3O3 |
| molecular weight | 439.39 g/mol | Exact mass | 10mM in DMSO |
| PSA | 84.300 Ų | logp | 4.396 |
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Safety information
Signal word:
Warning
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。
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