Molibresib (I-BET762; GSK-525762A)
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 |
|---|---|---|
| 250mg | $990 | Check With Us |
| 500mg | $1550 | Check With Us |
| 1g | $2325 | Check With Us |
: Cat #: V0414 CAS #: 1260907-17-2 Purity ≥ 98%
Description: Molibresib (also known as GSK525762A, I-BET-762, GSK-525762) is a novel and potent inhibitor for BET (Bromodomain and Extra-Terminal) family of proteins with potential anti-inflammatory and anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 423.9 |
|---|---|
| Molecular Formula | C22H22ClN5O2 |
| CAS No. | 1260907-17-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1 |
| Synonyms | GSK525762; GSK525762; GSK525762; GSK525762A; GSK525762A; GSK 525762A; IBET762; IBET762; IBET 762; molibresib. |
| Protocol | In Vitro | Molibresib (I-BET 762) shows the highest affinity interaction with BET. Molibresib binds to the tandem bromodomains of BET with high affinity (dissociation constant Kd of 50.5-61.3 nM). Molibresib displaces, with high efficacy (half-maximum inhibitory concentration IC50 of 32.5-42.5 nM), a tetra-acetylated H4 peptide that had been pre-bound to tandem bromodomains of BET. |
|---|---|---|
| In Vivo | The antimyeloma activity of Molibresib (I-BET 762) is tested dosed orally in an in vivo systemic xenograft model generated by injecting OPM-2 cells into NOD-SCID mice. Daily oral doses of Molibresib up to 10 mg/kg and 30 mg/kg given every other day are well tolerated with no clear impact on body weight compared with vehicle control. The plasma hLC concentration is significantly reduced in mice treated with Molibresib. |
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 | 2.3590 mL | 11.7952 mL | 23.5905 mL | 47.1809 mL |
| 5mM | 0.4718 mL | 2.3590 mL | 4.7181 mL | 9.4362 mL |
| 10mM | 0.2359 mL | 1.1795 mL | 2.3590 mL | 4.7181 mL |
| 20mM | 0.1180 mL | 0.5898 mL | 1.1795 mL | 2.3590 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
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Volume(start)
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Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
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Volume(start)
V1
=
Concentration(final)
C2
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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.