Synonyms: 4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone; TKI-258; CHIR 258; CHIR-258; CHIR258; TKI 258; TKI258
Molecular Formula: C21H21FN6O
Molecular Weight: 392.43
Linear Structural Formula: C21H21FN6O
MDL Number: MFCD10565680
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: Dovitinib (CHIR-258) is an orally active and potent receptor tyrosine kinase (RTK) inhibitor against class III (FLT3/KIT/PDGFR1/CSFR/PDGFR2 IC50 = 1/2/27/36/200 nM), class IV (FGFR1/3 IC50 = 8/9 nM), and class V (VEGFR1/2/3 IC50 = 10/13/8 nM) RTKs, but not INSR, EGFR1, ErbB2 or Raf (IC50 = 2.1, 2.2, >20, >25 μM, respectively). Dovitinib inhibits target RTKs phosphorylation in cultured cells (pVEGFR1 and pPDGFRβ IC90<50 nm; km12l4a) and exhibits in vivo anti-tumor efficacy in mice bearing km12l4a or hct116 human cancer xenografts (10-120 mg g ay p.o.).<>