Free shipping on all orders over $ 500

Molibresib besylate

Cat. No. M13825
Molibresib besylate Structure
Synonym:

GSK 525762C; I-BET 762 besylate

Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

Chemical Information
Molecular Weight 582.07
CAS Number 1895049-20-3
Solubility (25°C) DMSO 25 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Anu Shilpa Krishnatry, et al. CPT Pharmacometrics Syst Pharmacol. Population pharmacokinetic modeling of molibresib and its active metabolites in patients with solid tumors: A semimechanistic autoinduction model

[2] Kylie Riddell, et al. J Clin Pharmacol. An Adaptive Physiologically Based Pharmacokinetic-Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers

[3] Xiangpeng Dai, et al. Nat Med. Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4

[4] Jake E Delmore, et al. Cell. BET bromodomain inhibition as a therapeutic strategy to target c-Myc

[5] Edwige Nicodeme, et al. Nature. Suppression of inflammation by a synthetic histone mimic

Related Epigenetic Reader Domain Products
Phoenixin-20

Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals.

Menin-MLL inhibitor 31

Menin-MLL inhibitor 31 is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM.

OPN-2853

OPN-2853 is a bromodomain protein-4 (BRD4) inhibitor that can be used in studies related to hematologic and lymphatic disorders.

HDAC/JAK/BRD4-IN-1

HDAC/JAK/BRD4-IN-1 is a potent HDAC/JAK/BRD4 triple inhibitor.

VYN-201

VYN-201 is a novel pan-BET inhibitor for studies related to idiopathic pulmonary fibrosis.

  Catalog
Abmole Inhibitor Catalog




Keywords: Molibresib besylate, GSK 525762C; I-BET 762 besylate supplier, Epigenetic Reader Domain, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.