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INCB054329 BET inhibitor

Name: INCB054329
Brand: Selleck Chemicals
SKU: S8753
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S8753

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

Chemical Structure

Molecular Weight: 348.36

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Quality Control

Batch: Purity: 98.97%

98.97

Related Targets	HDAC JAK Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other BET Inhibitors	Pelabresib (CPI-0610) ZEN-3694 (BET-IN-19) Molibresib (I-BET-762) Mivebresib (ABBV-075) Birabresib (OTX015) I-BET151 (GSK1210151A) Apabetalone (RVX-208) AZD5153 6-hydroxy-2-naphthoic acid CPI-203 I-BRD9

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (200.94 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 70 mg/mL

Water : ˂1 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.500mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.430mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	348.36	Formula	C₁₉H₁₆N₄O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1628607-64-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	BRD3-BD2 1 nM BRD4-BD2 3 nM BRD2-BD2 5 nM BRD3-BD1 9 nM BRD4-BD1 28 nM BRD2-BD1 44 nM BRDT-BD2 63 nM BRDT-BD1 119 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 median 50% growth inhibition (GI50) value of this compound is 152 nM (range, 26-5000 nM). In contrast to tumor cell lines, the GI50 value 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. This compound is also a selective kinase inhibitor of the FGFR 1, 2, and 3. In myeloma cell lines, treatment with this chemical inhibits expression of c-MYC and induced HEXIM1. In both AML and lymphoma cell lines, it induces apoptosis consistent with increased expression of pro-apoptotic regulators.
In vivo	INCB054329 exhibits high clearance in mice resulting in a short half-life. At exposures that effectively suppressed c-MYC, this compound is found to be efficacious and well tolerated in both the KMS-12-BM and MM1.S xenograft models. In vivo, oral administration of this chemical inhibits tumor growth in several models of hematologic cancers.
References	[1] https://pubmed.ncbi.nlm.nih.gov/30206163/ [2] http://cancerres.aacrjournals.org/content/75/15_Supplement/3523 [3] https://pubmed.ncbi.nlm.nih.gov/29567272/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02431260	Terminated	Solid Tumors and Hematologic Malignancy	Incyte Corporation	April 14 2015	Phase 1\|Phase 2

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