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INCB-057643

🥰Excellent
Catalog No. T5417Cas No. 1820889-23-3

INCB057643 is a potent, selective and orally bioavailable BET inhibitor.

INCB-057643

INCB-057643

🥰Excellent
Purity: 99.50%
Catalog No. T5417Cas No. 1820889-23-3
INCB057643 is a potent, selective and orally bioavailable BET inhibitor.
Pack SizePriceAvailabilityQuantity
1 mg$35In Stock
5 mg$83In Stock
10 mg$143In Stock
25 mg$257In Stock
50 mg$387In Stock
100 mg$527In Stock
200 mg$725In Stock
1 mL x 10 mM (in DMSO)$92In Stock
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Purity:99.50%
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Product Introduction

Bioactivity
Description
INCB057643 is a potent, selective and orally bioavailable BET inhibitor.
In vitro
INCB057643 inhibited binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range and was selective against other bromodomain-containing proteins. INCB057643 inhibited proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicated that G1 arrest and a concentration-dependent increase in apoptosis were seen within 48 hours of treatment with INCB057643. BRD proteins also regulate the expression of many pro-inflammatory genes. Production of several cytokines, including IL-6, IL-10 and MIP-1α, was repressed by INCB057643 in human and mouse whole blood stimulated ex vivo with LPS [1].
In vivo
Oral administration of INCB057643 resulted in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL. Additionally, combining INCB057643 with the standard of care agents used for the treatment of DLBCL including rituximab and bendamustine resulted in enhanced anti-tumor efficacy relative to that achieved with single-agent therapies at doses that were well tolerated [1].
Chemical Properties
Molecular Weight415.46
FormulaC20H21N3O5S
Cas No.1820889-23-3
SmilesCN1C(=O)C(C)(C)Oc2c1cc(cc2-c1cn(C)c(=O)c2[nH]ccc12)S(C)(=O)=O
Relative Density.1.370 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 65 mg/mL (156.45 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4070 mL12.0349 mL24.0697 mL120.3485 mL
5 mM0.4814 mL2.4070 mL4.8139 mL24.0697 mL
10 mM0.2407 mL1.2035 mL2.4070 mL12.0349 mL
20 mM0.1203 mL0.6017 mL1.2035 mL6.0174 mL
50 mM0.0481 mL0.2407 mL0.4814 mL2.4070 mL
100 mM0.0241 mL0.1203 mL0.2407 mL1.2035 mL

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