溶解性 | Soluble in water (<1 mg/ml) at 25 °C, DMSO (~20 mg/ml), DMF (~20 mg/ml), 1:5 DMSO:PBS (pH 7.2) (~0.2 mg/ml), ethanol (5 mg/ml) at 25 °C, and methanol. |
存贮条件 | 储存温度-20°C |
应用 | A VEGF (Flk/Flt) and PDGFR inhibitor. |
产品介绍 | Linifanib (ABT-869)是一种新型,有效,ATP竞争性VEGFR/PDGFR抑制剂,同时抑制KDR, CSF-1R, Flt-1/3和PDGFRβ,其IC50分别为4 nM, 3 nM, 3 nM/4 nM和66 nM ,对具有突变激酶依赖性的癌细胞(即FLT3)最有效。Phase 3。 |
备注 | Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent canc |
生化机理 | ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (Flt/Flk) and PDGFR families (e.g., KDR, Flt1, Flt3, Flt4, CSF-1R, and KIT) demonstrating IC50 values ranging from 4-190 nM. ABT-869 shows little activity against unrelated RTKs, cytoplasmic tyrosine kinases, or Ser/Thr kinases (IC50 > 1 μM). ABT-869 inhibits proliferation in MV-4-11 and MOLM-13 cells (acute myeloid leukemia cell lines harboring RTK mutations; IC50 = 4 and 6 nM, respectively), inducing apoptosis as evidenced by an increased sub-G0/G1 phase cell population, caspase activation, and PARP cleavage. In murine xenograft models, as well as in a phase 1 clinical trial, ABT-869 demonstrated respectable efficacy in solid tumors including lung and hepatocellular carcinomas. |
别名 | N-[4-(3-氨基-1H-吲唑-4-基)苯基]-N'-(2-氟-5-甲基苯基)脲;ABT-869; AL-39324; ABT 869; ABT869; AL 39324; AL39324;1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea;N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)urea |
利尼伐尼 (ABT-869)
Linifanib (ABT-869) (订货以英文为准)
编号:L126993
CAS号:796967-16-3
分子式:C21H18FN5O
分子量:375.40
产品名称 | Linifanib (ABT-869) |
中文名称 | 利尼伐尼 (ABT-869) |
CAS号 | 796967-16-3 |
分子式(M.F.) | C21H18FN5O |
分子量(M.W.) | 375.40 |
储存条件 | -20°C储存 |
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