INCB057643
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $1650 | Check With Us |
| 250mg | $2650 | Check With Us |
| 500mg | $3975 | Check With Us |
: Cat #: V3764 CAS #: 1820889-23-3 Purity ≥ 98%
Description: INCB057643 is a novel, orally bioavailable BET inhibitor that has been tested in preclinical models of hematologic malignancies.
Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products
Product Promise
- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 415.46 |
|---|---|
| Molecular Formula | C20H21N3O5S |
| CAS No. | 1820889-23-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: >60 mg/mLr |
| Water: N/Ar | |
| Ethanol: N/A | |
| 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 |
| Synonyms | INCB057643; INCB-057643; INCB 057643 |
| Protocol | 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. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.4070 mL | 12.0349 mL | 24.0697 mL | 48.1394 mL |
| 5mM | 0.4814 mL | 2.4070 mL | 4.8139 mL | 9.6279 mL |
| 10mM | 0.2407 mL | 1.2035 mL | 2.4070 mL | 4.8139 mL |
| 20mM | 0.1203 mL | 0.6017 mL | 1.2035 mL | 2.4070 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.