INCB-057643

SKU: orb1301806

Description

INCB057643 is a potent, selective, and orally available small molecule inhibitor of BET proteins. It is utilized in oncology research to investigate epigenetic mechanisms in cancers such as AML and solid tumors, demonstrating activity in both cellular and animal models.

Research Area

Cell Biology, Epigenetics & Chromatin

Images & Validation

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Key Properties

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CAS Number	1820889-23-3
MW	415.46
Purity	99.58% (May vary between batches)
Formula	C₂₀H₂₁N₃O₅S
SMILES	CN1C(=O)C(C)(C)Oc2c1cc(cc2-c1cn(C)c(=O)c2[nH]ccc12)S(C)(=O)=O
Target	Epigenetic Reader Domain,Apoptosis
Solubility	DMSO:65 mg/mL (156.45 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.81 mM)

Bioactivity

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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 .

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 .

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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INCB057643, INCB-057643, INCB 057643, inhibit, EpigeneticReaderDomain, Epigenetic Reader Domain, Inhibitor, Apoptosis, BET

Quality Guarantee

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Compound Identifiers

PubChem CID

118467751 ↗

Key Properties

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No computed properties available.

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INCB-057643 (orb1301806)

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Purity:	>98% (HPLC)
CAS Number:	1820889-23-3
MW:	415.464
Formula:	C₂₀H₂₁N₃O₅S

INCB-057643

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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