| Identification | Back Directory | [Name]
A-485 | [CAS]
1889279-16-6 | [Synonyms]
A-485
A-486
A485;A 485
(1R)-N-[(4-Fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide
Spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide, N-[(4-fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]-, (1R)- | [Molecular Formula]
C25H24F4N4O5 | [MDL Number]
MFCD31619258 | [MOL File]
1889279-16-6.mol | [Molecular Weight]
536.48 |
| Chemical Properties | Back Directory | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO:97.41(Max Conc. mg/mL);181.57(Max Conc. mM)
DMF:10.0(Max Conc. mg/mL);18.64(Max Conc. mM)
Ethanol:57.88(Max Conc. mg/mL);107.89(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.47(Max Conc. mM) | [form ]
A crystalline solid | [pka]
14.07±0.46(Predicted) | [color ]
White to off-white | [optical activity]
[α]/D +40 to +50°, c =0.5 in methanol |
| Hazard Information | Back Directory | [Uses]
A-485 is potent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC50 values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively). Displays > 1000-fold selectivity over closely related HATs. Suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines in vitro. Inhibits tumor growth in a castration-resistant prostate cancer xenograft model. Orally bioavailable. | [Biological Activity]
A-485 exhibits an anti-tumor effect and may show therapeutic effects against the growth hormone pituitary adenoma (GHPA). It can specifically block the acetylation of histone H3 lysine 27 (H3K27) and lysine 18 (H3K18) sites catalyzed by p300.''A-485 is a potent and selective catalytic inhibitor of the p300 and CREB-binding protein (CBP) histone acetyltransferases (HATs) with an IC50 value of 60 nM. A-485 was most active against haematological malignancies including most multiple myeloma cell lines as well as androgen receptor-positive prostate cancer. It was also shown to inhibit the proliferation of castration-resistant prostate cancer cells and in vivo tumour growth in SCID mice. | [storage]
Store at -20°C |
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