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].

Product Specifications

CAS Number

[1970149-05-3]

UNSPSC

12352005

Target

P38 MAPK; Raf; Src; VEGFR

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sklb646.html

Smiles

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

Molecular Formula

C28H26F3N7O

Molecular Weight

533.55

References & Citations

[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.