INCB057643

Catalog No.S8714 Batch:S871402

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Technical Data

Formula

C20H21N3O5S
Molecular Weight 415.46 CAS No. 1820889-23-3
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.77 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Add solvents to the product individually and in order.)
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 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 4.15mg/ml (9.99mM) Taking the 1 mL working solution as an example, add 50 μL of 83 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 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.59mg/ml (1.42mM) Taking the 1 mL working solution as an example, add 50 μL of 11.8 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between this compound and acetylated lysines on histones.
Targets
BET
In vitro

INCB057643 inhibits binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range, and is selective against other bromodomain containing proteins. In vitro analyses show that this compound inhibits proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicate that G1 arrest and a concentration-dependent increase in apoptosis are seen within 48 hours of treatment with this chemical. Production of several cytokines, including IL-6, IL-10 and MIP-1α, was repressed by this compound in human and mouse whole blood stimulated ex vivo with LPS. It inhibits proliferation of prostate cancer cell lines. In short-term cell proliferation assays, this chemical appears more effective against androgen-dependent (VCaP and LNCaP) than androgen-independent (DU145 and PC3) cells.
In Vivo

Oral administration of INCB057643 resulted in significant anti-tumour efficacy in xenograft models of AML, myeloma, and DLBCL. Treatment of mice bearing 22Rv1 tumour xenografts with this compound (3 mg/kg) led to significant inhibition of tumour growth (T/C%:45%) and consistent reduction of tumour weight relative to vehicle-treated mice.

Protocol (from reference)

References

  • http://cancerres.aacrjournals.org/content/77/13_Supplement/5071#
  • http://cancerres.aacrjournals.org/content/77/13_Supplement/5080

Sellecks INCB057643 Has Been Cited by 1 Publication

The synergy of the XPO1 inhibitors combined with the BET inhibitor INCB057643 in high-grade B-cell lymphoma via downregulation of MYC expression [ Sci Rep, 2023, 13(1):18554] PubMed: 37899423

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.