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INCB-057643 

Cat. No.: HY-111485 Purity: 98.91%
Handling Instructions

INCB-057643 is a novel, orally bioavailable BET inhibitor.

For research use only. We do not sell to patients.

INCB-057643 Chemical Structure

INCB-057643 Chemical Structure

CAS No. : 1820889-23-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 242 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

INCB-057643 is a novel, orally bioavailable BET inhibitor.

IC50 & Target

BET[1]

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[1].

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[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (150.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4070 mL 12.0349 mL 24.0697 mL
5 mM 0.4814 mL 2.4070 mL 4.8139 mL
10 mM 0.2407 mL 1.2035 mL 2.4070 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

References
Molecular Weight

415.46

Formula

C₂₀H₂₁N₃O₅S

CAS No.

1820889-23-3

SMILES

O=C1C(C)(C)OC2=C(C3=CN(C)C(C4=C3C=CN4)=O)C=C(S(=O)(C)=O)C=C2N1C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
INCB-057643
Cat. No.:
HY-111485
Quantity:

INCB-057643

Cat. No.: HY-111485