INCB-54329

Product Name: INCB-54329
CAS No.: 1628607-64-6
Chemical Name: INCB-54329
Synonyms: INCB-54329;INCB-054329,INCB-54329;INCB054329（INCB-054329;INCB054329（INCB-054329,INCB-54329）;Inhibitor,inhibit,INCB 054329,Epigenetic Reader Domain;(S)-6-(3,5-Dimethylisoxazol-4-yl)-3-(pyridin-2-yl)-3,4-dihydro-5-oxa-1,2a-diazaacenaphthylen-2(1H)-one;Imidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, 7-(3,5-dimethyl-4-isoxazolyl)-4,5-dihydro-4-(2-pyridinyl)-, (4S)-;(11S)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-11-pyridin-2-yl-9-oxa-1,3-diazatricyclo[6.3.1.0^{4,12}]dodeca-4(12),5,7-trien-2-one
CBNumber: CB24672573
Molecular Formula: C19H16N4O3
Formula Weight: 348.36
MOL File: 1628607-64-6.mol

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INCB-54329 Property

Density: 1.46±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : ≥ 100 mg/mL (287.06 mM)
pka: 12.48±0.40(Predicted)

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0046160
Product name: INCB054329
Purity: 98.21%
Packaging: 5mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-0046160
Product name: INCB054329
Purity: 98.21%
Packaging: 10mg
Price: $850
Updated: 2021/12/16

ChemScene

Product number: CS-0046160
Product name: INCB054329
Purity: 98.21%
Packaging: 25mg
Price: $1750
Updated: 2021/12/16

ChemScene

Product number: CS-0046160
Product name: INCB054329
Purity: 98.21%
Packaging: 50mg
Price: $2750
Updated: 2021/12/16

ChemScene

Product number: CS-0046160
Product name: INCB054329
Purity: 98.21%
Packaging: 100mg
Price: $3950
Updated: 2021/12/16

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INCB-54329 Chemical Properties,Usage,Production

Biological Activity

INCB054329 (INCB-054329, INCB-54329) is a BET inhibitor with IC50 for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively Available in 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM.

in vitro

3 μM of INCB054329 had no significant inhibitory activity against 16 non-BET bromodomains. It had a mean GI50 of 152 nM in a group of 32 hematologic cancer cell lines isolated from acute myeloid leukemia, non-Hodgkin's lymphoma, and multiple myeloma. In T cells isolated from normal volunteers, stimulated with IL2 in vitro, the GI50 value of it was 2.435 μM. Its growth inhibitory effect on cells is related to the arrest of cells in G1 phase. INCB054828 is also a selective inhibitor of FGFR1,2,3. In myeloma cell lines, treatment with it inhibited c-myc expression and induced HEXIM1. In AML and lymphoma cell lines, INCB054329 induced apoptosis and increased expression of pro-apoptotic regulators. It reduces the expression of homologous recombination components, reduces cell growth, and enhances PARPi and cisplatin-induced DNA damage and apoptosis.

in vivo

In mice, INCB-54329 has high clearance and short half-life. At exposures sufficient to effectively inhibit c-myc, it was effective and well tolerated in KMS-12-BM and MM1.S xenograft models. In vivo, oral administration of it inhibited tumor growth in multiple hematological cancer models.

target

Target	Value
BRD3-BD2 ()	1 nM
BRD4 -BD2 ()	3 nM
BRD2-BD2 ()	5 nM
BRD3-BD1 ()	9 nM
BRD4-BD1 ()	28 nM

INCB-54329 Preparation Products And Raw materials

Raw materials

Preparation Products

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INCB-54329 Suppliers

China 24 United States 3 Global 27

Shanghai Lollane Biological Technology Co.,Ltd.

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1628607-64-6, INCB-54329Related Search:

INCB39110 3-Pyrrolidinecarboxylic acid, 1-[[7-cyano-2-[3'-[[3-[[(3R)-3-hydroxy-1-pyrrolidinyl]methyl]-1,7-naphthyridin-8-yl]amino]-2,2'-dimethyl[1,1'-biphenyl]-3-yl]-5-benzoxazolyl]methyl]-, (3R)- 4-tert-Butylcyclohexanone ADOGEN 464

INCB-54329

(11S)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-11-pyridin-2-yl-9-oxa-1,3-diazatricyclo[6.3.1.0^{4,12}]dodeca-4(12),5,7-trien-2-one

INCB054329（INCB-054329,INCB-54329）

Imidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, 7-(3,5-dimethyl-4-isoxazolyl)-4,5-dihydro-4-(2-pyridinyl)-, (4S)-

INCB054329（INCB-054329

INCB-054329,INCB-54329

Inhibitor,inhibit,INCB 054329,Epigenetic Reader Domain

(S)-6-(3,5-Dimethylisoxazol-4-yl)-3-(pyridin-2-yl)-3,4-dihydro-5-oxa-1,2a-diazaacenaphthylen-2(1H)-one

1628607-64-6