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INCB057643

SKU: orb1225873

Description

INCB057643 is a novel potent, selective, orally bioavailable BET inhibitor; shows more effectivity against androgen-dependent (VCaP and LNCaP) than androgen-independent (DU145 and PC3) cells with IC50 of 500 nM, respectively; significantly causes inhibition of tumor growth in mice bearing 22Rv1 tumor xenografts.Solid Tumors Phase 2 Clinical.

Images & Validation

Key Properties

CAS Number1820889-23-3
MW415.464
Purity>98% (HPLC)
FormulaC20H21N3O5S
SMILESCN(C(C(C)(C)O1)=O)C2=C1C(C(C3=C4NC=C3)=CN(C)C4=O)=CC(S(C)(=O)=O)=C2
TargetBromodomain
SolubilityDMSO : 62.5 mg/mL 150.44 mM

Bioactivity

In Vivo
Production of several cytokines, including IL-6, IL-10 and MIP-1α, is repressed by INCB-057643 in human and mouse whole blood stimulated ex vivo with LPS. Oral administration of INCB-057643 results in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL. Additionally, combining INCB-057643 with standard of care agents used for the treatment of DLBCL including rituximab and bendamustine results in enhanced anti-tumor efficacy relative to that achieved with single agent therapies at doses that are well tolerated.
In Vitro
INCB-057643 is a novel, orally bioavailable BET inhibitor. INCB-057643 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 INCB-057643 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 INCB-057643.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

INCB 057643

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  • INCB-057643 [orb1301806]

    99.58% (May vary between batches)

    1820889-23-3

    415.46

    C20H21N3O5S

    10 mg, 25 mg, 50 mg, 100 mg, 1 mg, 1 ml x 10 mM (in DMSO), 200 mg, 5 mg
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Protocol Information

INCB057643 (orb1225873)

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Available Sizes

Select a size below

2 mg
¥ 2,080.00
5 mg
¥ 3,250.00
10 mg
¥ 5,200.00
25 mg
¥ 9,490.00
50 mg
¥ 13,390.00
100 mg
¥ 17,940.00
500 mg
¥ 35,620.00