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

More

Less

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

More

Less

Hazard and Precautionary Statements (GHS)

More

Less

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

More

Less

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

Target	Value
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

More

Less

INCB-54329 Suppliers

China 43 United States 3 Global 46

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4769
Advantage: 55

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
Advantage: 60

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
Advantage: 62

Beijing Solarbio Science & Tecnology Co., Ltd.

Tel: 010-50973130 18101056239
Email: 3193328036@qq.com
Country: China
ProdList: 29760
Advantage: 68

Shanghai Anyinuo Biomedical Technology Co., Ltd.

Tel: 021-34625901 18018851262;
Email: 420970979@qq.com
Country: China
ProdList: 5894
Advantage: 58

TargetMol Chemicals Inc.

Tel: +1-781-999-5354; +17819995354
Email: marketing@targetmol.com
Country: United States
ProdList: 32435
Advantage: 58

InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6391
Advantage: 58

HANGZHOU CLAP TECHNOLOGY CO.,LTD

Tel: 86-571-88216897,88216896 13588875226
Fax: 86-571-88216895
Email: sales@hzclap.com
Country: CHINA
ProdList: 6312
Advantage: 58

ChemeGen(Shanghai) Biotechnology Co.,Ltd.

Tel: 18818260767
Fax: QQ 3610331285
Email: sales@chemegen.com
Country: China
ProdList: 11218
Advantage: 58

Shanghai hongqu biomedical technology co. LTD

Tel: 88888888888
Email: hongquchem@qq.com
Country: China
ProdList: 5132
Advantage: 58

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