A 485 is a 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), which displays > 1000-fold selectivity over closely related HATs. A 485 suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines
in vitro
, and also inhibits tumor growth in a castration-resistant prostate cancer xenograft model. A 485 is orally bioavailable.
To request the negative control for A 485, please fill out the A 486 request form on the SGC website.
Caractéristiques techniques
| Marque | Tocris |
| Réf. B-LABO | BL-RE-125018 |
| Réf. fabricant | 18738649 |
| CAS | 1889279-16-6 |
|---|
| Synonyme | (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 |
|---|
| Quantité | 25 mg |
|---|
| Formule moléculaire | C<sub>25</sub>H<sub>24</sub>F<sub>4</sub>N<sub>4</sub>O<sub>5</sub> |
|---|
| Poids de la formule | 536.48 |
|---|
| Pureté | 98% |
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