Cas No.: | 1404231-34-0 |
Chemical Name: | 5H-Pyrimido[4,5-b][1,4]thiazin-6(7H)-one, 2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-7-[(4-nitrophenyl)methylene]- |
Synonyms: | ON-146040;ON146040 |
SMILES: | O=[N+](C1=CC=C(/C=C2\SC3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C3NC\2=O)C=C1)[O-] |
Formula: | C24H23N7O3S |
M.Wt: | 489.5495 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | ON 146040 is a potent, dual PI3K/BCR-ABL inhibitor with IC50 of 14/20 nM for PI3Kα/δ , IC50 of 20 nM for BCR/ABL; displaysno significant effect on PI3Kβ/γ isoforms (IC50=3/1 uM), also inhibits Abl1 and several mutant versions of Abl (IC50<150 nM) but not the T315I mutant; abrogates the oncogenic signaling of STAT3 and STAT5, ON 146040 is highly potent in killing hematologic tumor cells with IC50 values of 150-1,000 nM, down-regulates STAT3 and STAT5 phosphorylation in leukemia and myeloma cells. |