A p300/CBP inhibitor
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A-485

Item No. 24119

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(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
CAS Number
1889279-16-6
Molecular Formula
C25H24F4N4O5
Formula Weight
536.5
Purity
≥98% (mixture of isomers)
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 16 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
253 nm
SMILES
O=C(NC)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
InChi Code
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-/m1/s1
InChi Key
VRVJKILQRBSEAG-PYFQUHSISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $209

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    10 mg

    $367

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    25 mg

    $783

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    Cayman Chemical
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    Product Description

    A-485 is an inhibitor of the histone acetyltransferase p300/CBP (IC50 = 60 nM).1 It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin's, and acute myeloid leukemia cell lines. It inhibits expression of prostate specific antigen (PSA) and H3K27Ac occupancy at the PSA enhancer without inhibiting androgen receptor occupancy in LNCaP-FGC cells. A-485 reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100 mg twice per day for 21 days. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lasko, L.M., Jakob, C.G., Edalgi, R.P., et al. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature 550(7674), 128-132 (2017).