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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, 10 mM in DMSO;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)
form 
Solid
color 
Light yellow to yellow
InChI
InChI=1S/C19H16N4O3/c1-10-16(11(2)26-22-10)12-6-7-14-17-18(12)25-9-15(23(17)19(24)21-14)13-5-3-4-8-20-13/h3-8,15H,9H2,1-2H3,(H,21,24)/t15-/m1/s1
InChIKey
XYLPKCDRAAYATL-OAHLLOKOSA-N
SMILES
O1C2=C(C3=C(C)ON=C3C)C=CC3NC(=O)N(C2=3)[C@@H](C2=NC=CC=C2)C1
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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

Uses

INCB054329 is a potent BET inhibitor.

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

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

References

[1] Pérez-Salvia M, et al. Bromodomain inhibitors and cancer therapy: From structures to applications. Epigenetics. 2017 May 4;12(5):323-339. DOI:10.1080/15592294.2016.1265710
[2] Phillip CC Liu, et al. Abstract 3523: Discovery of a novel BET inhibitor INCB054329.

INCB-54329 Preparation Products And Raw materials

Raw materials

Preparation Products

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INCB-54329 Suppliers

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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
  • INCB054329, 10 mM in DMSO
  • 1628607-64-6