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| 25mg |
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Purity: ≥98%
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. It inhibits BET with IC50 of ~35 nM in a cell-free assay. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, and is highly selective over other bromodomain-containing proteins. GSK525762 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides.
| ln Vitro |
Molibresib (I-BET 762) showed the strongest affinity interaction with BET. Molibresib binds to the tandem bromodomains of BET with great 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[1]. Molibresib exhibits high affinity for BD1/BD2 domain of BRD2/3/4 proteins. Molibresib therapy leads to a reduction in the recruitment of all three proteins to chromatin[2]. Molibresib inhibits OPM-2 cell growth with IC50 of 60.15 nM[3].
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| ln Vivo |
Molibresib (I-BET 762) is examined orally for its antimyeloma activity using an in vivo systemic xenograft model created by injecting OPM-2 cells into NOD-SCID mice. Molibresib oral dosages up to 10 mg/kg and 30 mg/kg administered every other day are well tolerated and do not significantly affect body weight when compared to vehicle control. When mice are given Molibresib, the concentration of hLC in their plasma is considerably decreased[3].
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| References |
[1]. Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23.
[2]. Asangani IA, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014 Jun 12;510(7504):278-82. [3]. Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705 |
| Molecular Formula |
C22H22CLN5O2
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|---|---|
| Molecular Weight |
423.895383358002
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| CAS # |
1260907-17-2
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| Related CAS # |
I-BET762 carboxylic acid;1300019-38-8;GSK 525768A;1260530-25-3;Molibresib besylate;1895049-20-3
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| SMILES |
O=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
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| InChi Key |
AAAQFGUYHFJNHI-SFHVURJKSA-N
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| InChi Code |
InChI=1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
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| Chemical Name |
(S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
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| Synonyms |
GSK-525762; GSK525762;IBET762; IBET 762; IBET-762; GSK 525762; GSK-525762A; GSK 525762A; GSK525762A;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~471.81 mM)
1M HCl : 100 mg/mL (~235.90 mM) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3590 mL | 11.7952 mL | 23.5905 mL | |
| 5 mM | 0.4718 mL | 2.3590 mL | 4.7181 mL | |
| 10 mM | 0.2359 mL | 1.1795 mL | 2.3590 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04116359 | Withdrawn | Drug: Cisplatin Drug: Etoposide |
Metastatic NUT Carcinoma Unresectable NUT Carcinoma |
National Cancer Institute (NCI) | September 18, 2020 | Phase 1 Phase 2 |
| NCT03925428 | Withdrawn | Drug: Entinostat Drug: Molibresib |
Advanced Lymphoma Advanced Malignant Solid Neoplasm |
National Cancer Institute (NCI) | September 18, 2020 | Phase 1 |
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