| 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 |
