Cas No.: | |
Chemical Name: | (S)-1-(4-(1-aminopropan-2-yl)phenyl)-2-hydroxy-4-methylphenanthridin-6(5H)-one hydrochloride |
SMILES: | C(C1=CC=C([C@@H](C)CN)C=C1)1=C2C(NC(=O)C3=C2C=CC=C3)=C(C)C=C1O.[H]Cl |
Formula: | C23H23ClN2O2 |
M.Wt: | 394.899 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | SKLB-C05 is a novel selective, orally active TOPK inhibitor with IC50 of 0.5 nM, shows excellent cytotoxicity and anti-migration and invasion activity on TOPK high-expressing CRC cells and induces cell apoptosis; exhibits markedly prioritized inhibitory activity on TOPK-positive CRC cells than TOPK-negative cells (HCT116 cell IC50=96 nM); inhibits TOPK downstream signaling including ERK1/2, p38, and JNK1/2/3, as well as downregulation of FAK/Src- MMP signaling; dramatically attenuates CRC tumor xenograft growth and completely suppressed hepatic metastasis of HCT116 cells (20 and 10 mg/kg/day). |