INCB057643 ( INCB 057643 )

Catalog No. M12807 CAS No. 1820889-23-3

COA

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HNMR

HPLC

MSDS

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Product Name

INCB057643
Note

Research use only, not for human use.
Brief Description

INCB057643 is a novel potent, selective, orally bioavailable BET inhibitor.
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 <100 nM and >500 nM, respectively; significantly causes inhibition of tumor growth in mice bearing 22Rv1 tumor xenografts.Solid Tumors Phase 2 Clinical
Synonyms

INCB 057643
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

BET
Research Area

Cancer
Indication

Solid Tumors

CAS Number

1820889-23-3
Formula Weight

415.46
Molecular Formula

C20H21N3O5S
Purity

>98% (HPLC)
Solubility

DMSO : 62.5 mg/mL 150.44 mM
SMILES

CN(C(C(C)(C)O1)=O)C2=C1C(C(C3=C4NC=C3)=CN(C)C4=O)=CC(S(C)(=O)=O)=C2
Chemical Name

2,2,4-trimethyl-8-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-6-(methylsulfonyl)-2H-benzo[b][1,4]oxazin-3(4H)-one

1. Wilson AJ, et al. Gynecol Oncol. 2018 Mar 20. pii: S0090-8258(18)30229-4.

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