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SML2192

A-485

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

Synonym(s):

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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Pack SizeSKUAvailabilityPrice
5 mg
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$210.00
25 mg
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$840.00

About This Item

Empirical Formula (Hill Notation):
C25H24F4N4O5
CAS Number:
Molecular Weight:
536.48
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder

$210.00


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Product Name

A-485, ≥98% (HPLC)

Quality Segment

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

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.[1]

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.[2]
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

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This Item
SML2588SML1315D1946
assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥97% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

-

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 20 mg/mL, clear

solubility

-

color

white to beige

color

white to beige

color

white to beige

color

colorless to yellow


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Global Trade Item Number

SKUGTIN
SML2192-25MG04061842559817
SML2192-5MG04061842559824

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