ChemicalBook > CAS DataBase List > A-485

A-485

Product Name: A-485
CAS No.: 1889279-16-6
Chemical Name: A-485
Synonyms: A-486;A-485;A485;A 485;A-485, 10 mM in DMSO;inhibit,HATs,A 485,Inhibitor,Epigenetic Reader Domain,Histone Acetyltransferase,HAT,A-485,A485;N-(4-Fluorobenzyl)-2-[(R)-5-(3-methylureido)-2’,4’-dioxo-2,3-dihydrospiro[indene-1,5’-oxazolidin]-3’-yl]-N-[(S)-1,1,1-trifluoro-2-propyl]acetamide;N-(4-Fluorobenzyl)-2-[(R)-5-(3-methylureido)-2’,4’-dioxo-2,3-dihydrospiro[indene-1,5’-oxazolidin]-3’-yl]-N-[(S)-1,1,1-trifluoro-2-propyl]acetamide;N-(4-Fluorobenzyl)-2-((R)-5-(3-methylureido)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-3'-yl)-N-((S)-1,1,1-trifluoropropan-2-yl)acetamide;(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)-
CBNumber: CB63386444
Molecular Formula: C25H24F4N4O5
Formula Weight: 536.48
MOL File: 1889279-16-6.mol

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A-485 Property

Density: 1.46±0.1 g/cm3(Predicted)
storage temp.: 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
InChIKey: VRVJKILQRBSEAG-LFPIHBKWSA-N
SMILES: [C@@]12(C(=O)N(CC(N(CC3=CC=C(F)C=C3)[C@@H](C)C(F)(F)F)=O)C(=O)O1)C1=C(C=C(NC(NC)=O)C=C1)CC2

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 24119
Product name: A-485
Packaging: 1mg
Price: $49
Updated: 2024/03/01

Cayman Chemical

Product number: 24119
Product name: A-485
Packaging: 25mg
Price: $711
Updated: 2024/03/01

Cayman Chemical

Product number: 24119
Product name: A-485
Packaging: 5mg
Price: $190
Updated: 2024/03/01

Cayman Chemical

Product number: 24119
Product name: A-485
Packaging: 10mg
Price: $333
Updated: 2024/03/01

Tocris

Product number: 6387
Product name: A485
Purity: ≥98%(HPLC)
Packaging: 5
Price: $257
Updated: 2021/12/16

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A-485 Chemical Properties,Usage,Production

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.

in vivo

After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (P<0.005 as compare to vehicle control). In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16 hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3 hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen^[1].

IC 50

CBP/p300

storage

Store at -20°C

A-485 Preparation Products And Raw materials

Raw materials

Preparation Products

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A-485 Suppliers

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1889279-16-6, A-485Related Search:

(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

A-485

A485;A 485

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)-

A-486

N-(4-Fluorobenzyl)-2-((R)-5-(3-methylureido)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-3'-yl)-N-((S)-1,1,1-trifluoropropan-2-yl)acetamide

inhibit,HATs,A 485,Inhibitor,Epigenetic Reader Domain,Histone Acetyltransferase,HAT,A-485,A485

N-(4-Fluorobenzyl)-2-[(R)-5-(3-methylureido)-2’,4’-dioxo-2,3-dihydrospiro[indene-1,5’-oxazolidin]-3’-yl]-N-[(S)-1,1,1-trifluoro-2-propyl]acetamide

A-485, 10 mM in DMSO

N-(4-Fluorobenzyl)-2-[(R)-5-(3-methylureido)-2’,4’-dioxo-2,3-dihydrospiro[indene-1,5’-oxazolidin]-3’-yl]-N-[(S)-1,1,1-trifluoro-2-propyl]acetamide

1889279-16-6

C25H24F4N4O5

intermediate