MedKoo Cat#: 206955 | Name: INCB057643
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

INCB057643, also known INCB57643, is a BET inhibitor. INCB054329 reduces homologous recombination efficiency and augments PARP inhibitor activity in ovarian cancer. INCB057643 inhibited proliferation of prostate cancer cell lines. In short-term cell proliferation assays the BETi appeared more effective against androgen-dependent (VCaP and LNCaP) than androgen-independent (DU145 and PC3) cells (GI50 of ≤100 nM and ≥500 nM, respectively). 22Rv1 cells, which express androgen-independent AR splice variants, exhibited an intermediate level of sensitivity to both compounds (GI50: 150-250 nM).

Chemical Structure

INCB057643
INCB057643
CAS#1820889-23-3

Theoretical Analysis

MedKoo Cat#: 206955

Name: INCB057643

CAS#: 1820889-23-3

Chemical Formula: C20H21N3O5S

Exact Mass: 415.1202

Molecular Weight: 415.46

Elemental Analysis: C, 57.82; H, 5.10; N, 10.11; O, 19.25; S, 7.72

Price and Availability

Size Price Availability Quantity
10mg USD 285.00 2 Weeks
25mg USD 550.00 2 Weeks
50mg USD 900.00 2 Weeks
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Related CAS #
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Synonym
INCB057643; INCB-057643; INCB 057643; INCB57643; INCB-57643; INCB 57643;
IUPAC/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
InChi Key
VZSAMEOETVNDQH-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H21N3O5S/c1-20(2)19(25)23(4)15-9-11(29(5,26)27)8-13(17(15)28-20)14-10-22(3)18(24)16-12(14)6-7-21-16/h6-10,21H,1-5H3
SMILES Code
CN(C(C(C)(C)O1)=O)C2=C1C(C(C3=C4NC=C3)=CN(C)C4=O)=CC(S(C)(=O)=O)=C2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 415.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wilson AJ, Stubbs M, Liu P, Ruggeri B, Khabele D. The BET inhibitor INCB054329 reduces homologous recombination efficiency and augments PARP inhibitor activity in ovarian cancer. Gynecol Oncol. 2018 Mar 20. pii: S0090-8258(18)30229-4. doi: 10.1016/j.ygyno.2018.03.049. [Epub ahead of print] PubMed PMID: 29567272.