Cas No.: | 1801787-56-3 |
Chemical Name: | N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide |
Synonyms: | OICR 9429,OICR 9429 |
SMILES: | O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=CC(C3=CC=CC(CN4CCOCC4)=C3)=CC=C2N5CCN(C)CC5 |
Formula: | C29H32F3N5O3 |
M.Wt: | 555.59 |
Sotrage: | 4°C for 1 year, -20°C for more than 2 years |
Description: | OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation |
In Vitro: | OICR-9429 inhibit proliferation and induce differentiation in p30-expressing human AML cells. OICR-9429 cause a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene. OICR-9429 displays exquisite cellular selectivity and specificity in disrupting critical protein-protein interactions between WDR5. [1] reduce the viability of primary human AML cells with N-terminal C/EBPα mutations by about 50% (mean value, n = 8) at 5 μM[2]In vivo:The reference for OICR-9429 to mice (female NOD-SCID) is 3 mg/kg. |