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SML2192

A-485

Name: A-485
Brand: SIGMA

≥98% (HPLC), catalytic p300/CBP inhibitor, powder

别名:

N-(4-fluorobenzyl)-2-((R)-5-(3-methylureido)-2′,4′-dioxo-2,3-dihydrospiro[indene-1,5′-ozazolidine]-3′-7 yl)-N-((S)-1,1,1-trifluoropropan-2-yl)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)-

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关于此项目

经验公式（希尔记法）:

C₂₅H₂₄F₄N₄O₅

化学文摘社编号:

1889279-16-6

分子量:

536.48

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD31619258

Assay:

≥98% (HPLC)

Form:

powder

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属性

产品名称

A-485, ≥98% (HPLC)

Quality Segment

100

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +40 to +50°, c = 0.5 in methanol

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

CNC(NC1=CC=C2C(CC[C@]23C(N(CC(N(CC4=CC=C(F)C=C4)[C@@H](C)C(F)(F)F)=O)C(O3)=O)=O)=C1)=O

InChI

1S/C25H24F4N4O5/c1-14(25(27,28)29)32(12-15-3-5-17(26)6-4-15)20(34)13-33-21(35)24(38-23(33)37)10-9-16-11-18(7-8-19(16)24)31-22(36)30-2/h3-8,11,14H,9-10,12-13H2,1-2H3,(H2,30,31,36)/t14-,24+/m0/s1

InChI key

VRVJKILQRBSEAG-LFPIHBKWSA-N

说明

Application

A-485 has been used as a p300 regulated RelA acetylation inhibitor to study the effect of fatty acid oxidation (FAO) derived cytoplasmic acetyl-CoA on CD47 transcription and protein stability via citrate/acetyl-CoA mediated RelA acetylation in glioblastoma.

Biochem/physiol Actions

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.

Selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c