BT-869 is an TP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (VEGF) and platelet derived growth factor (PDGF) receptor families (e.g., KDR, Flt1, Flt3, Flt4, CSF-1R, and KIT) demonstrating IC50 values ranging from 4-190 nM.1 ABT-869 shows little activity against unrelated RTKs, cytoplasmic tyrosine kinases, or Ser/Thr kinases (IC50s > 1 μM. ABT-869 inhibits proliferation in MV-4-11 and MOLM-13 cells (acute myeloid leukemia cell lines harboring RTK mutations; IC50s = 4 and 6 nM, respectively), inducing apoptosis as evidenced by an increased sub-G0/G1 phase cell population, caspase activation, and PARP cleavage.
Линифаниб (ABT-869) - новый ингибитор ингибитор тирозин киназ - васкулярно-эндотелиальный фактор роста(VEGF) и тромбоцитарный фактора роста (PDGF), PDGF рецептора бета-(β-PDGFR), КДР, и колониестимулирующий фактора 1-рецепторов (CSF-1R), с IC50 0.2, 2, 4 и 7 нмоль для эндотелиальных клетках человека соответственно.
Name 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea
CAS 606143-52-6
Molecular Formula C21H18FN5O
WM 375.40
