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INCB054329

Catalog No. T22345 CAS 1628607-64-6

Synonyms: INCB-054329,INCB-54329, INCB-54329

INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2 with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM respectively.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

INCB054329, CAS 1628607-64-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 64.00
5 mg	In stock	$ 155.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 497.00
50 mg	In stock	$ 723.00
100 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 169.00

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Purity: 98.03%

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Storage & Solubility Information

Description	INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2 with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM respectively.
Targets&IC50	BRD2 BD2:5 nM, BRD3 BD2:1 nM, BRD4 BD1:28 nM, BRD4 BD2:3 nM, BRD3 BD1:9 nM
In vitro	INCB054329 shows no significant inhibitory activity against 16 non-BET bromodomains at 3 μM. In a panel of 32 hematologic cancer cell lines derived from acute myeloid leukemia, non-Hodgkin lymphoma, and multiple myeloma, the GI50 of INCB054329 is 152 nM (range, 26-5000 nM). In contrast to tumor cell lines, the GI50 against T cells isolated from non-diseased donors stimulated ex vivo with IL-2 is 2.435 μM. Growth inhibition correlates with a concentration-dependent accumulation of cells in the G1 phase of the cell cycle. INCB054828 is also a selective kinase inhibitor of the FGFR 1, 2, and 3[1]. Treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1 in myeloma cell lines. In both lymphoma and AML cell lines, INCB054329 induces apoptosis consistent with increased expression of pro-apoptotic regulators[2]. INCB054329 reduces expression of Homologous recombination (HR) components and co-operatively reduces cell growth and increases DNA damage and apoptosis induced by cisplatin and PARPi [3].
In vivo	INCB054329 exhibits high clearance in mice leading to a short half-life. At exposures that effectively suppressed c-MYC, INCB054329 is found to be efficacious and well tolerated in both the MM1.S and KMS-12-BM xenograft models[1]. In vivo, oral administration of INCB054329 inhibits tumor growth in several hematologic cancers models[2].
Cell Research	Cell lines: DLBCL, AML, Myeloma cells. Incubation Time: 72 h. Method: Cell viability assay
Animal Research	Animal Models: KMS-12-BM tumors established in female Nu/Nu mice. Dosages: 3, 10, 30, or 100 mg/kg. Administration: oral gavage.

Synonyms	INCB-054329,INCB-54329, INCB-54329
Molecular Weight	348.36
Formula	C19H16N4O3
CAS No.	1628607-64-6

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (287.06 mM)

References and Literature

1. Stubbs MC, et al. Clin Cancer Res. 2019, 25(1):300-311. 2. Phillip CC Liu, et al. AACR Cancer Res. 2015, 75(15 Suppl):Abstract nr 3523. 3. Wilson AJ, et al. Gynecol Oncol. 2018, 149(3):575-584.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Epigenetics Compound Library Clinical Compound Library PPI Inhibitor Library Anti-Cancer Compound Library Histone Modification Compound Library

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Keywords

INCB054329 1628607-64-6 Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor inhibit INCB 54329 INCB-054329,INCB 54329 INCB-054329,INCB-54329 INCB54329 INCB-054329,INCB54329 INCB-054329 INCB-54329 INCB 054329 inhibitor

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