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Mivebresib

Catalog No. T3712 CAS 1445993-26-9

Synonyms: ABBV-075

Mivebresib (ABBV-075), also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.

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Mivebresib, CAS 1445993-26-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
2 mg	In stock	$ 75.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 162.00
25 mg	In stock	$ 270.00
50 mg	In stock	$ 486.00
100 mg	In stock	$ 695.00
1 mL * 10 mM (in DMSO)	In stock	$ 100.00

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Purity: 98.74%

Purity: 97.17%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Mivebresib (ABBV-075), also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.
Targets&IC50	BET:1.5 nM(ki)
In vitro	ABBV-075 exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit[1].
In vivo	ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia[1].

Synonyms	ABBV-075
Molecular Weight	459.47
Formula	C22H19F2N3O4S
CAS No.	1445993-26-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 84 mg/mL (183 mM)

References and Literature

1. Aparna Sarthy, et al. Experimental and Molecular Therapeutics. 2016, Abstract 4718.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Human Metabolite Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Fluorochemical Library

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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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Mivebresib 1445993-26-9 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain ABBV-075 ABBV 075 ABBV075 Inhibitor inhibit inhibitor

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