SKLB646 

SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC₅₀ values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC₅₀ values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines^[1].

533.55

C₂₈H₂₆F₃N₇O

1970149-05-3

CC1=CC=C(NC(C2=CC(C(F)(F)F)=CC=C2)=O)C=C1C#CC3=NN(C4CCN(C)CC4)C5=C3C(N)=NC=N5

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Mingwu Zhang, et al. "Preclinical evaluation of a novel orally available SRC/Raf/VEGFR2 inhibitor, SKLB646, in the treatment of triple-negative breast cancer." Molecular Cancer Therapeutics 15.3 (2016): 366-378.  [Content Brief]