Cas No.: | 1936421-41-8 |
Chemical Name: | 1-(3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethan-1-one |
Synonyms: | GNE049;GNE 049 |
SMILES: | FC(F)C1C=C2C(CCCN2C2C3CN(C(=O)C)CCC=3N(C3CCOCC3)N=2)=CC=1C1C=NN(C)C=1 |
Formula: | C27H32F2N6O2 |
M.Wt: | 510.59 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively; displays 3,850-fold selectivity over BRD4; shows excellent potency (12 nM) in a BRET cellular assay and inhibits the expression of MYC with EC50 of 14 nM in MV-4-11 cells; demonstrates significant dose-dependent inhibition of AR signaling and PC proliferation in vitro and in vivo. |