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Alobresib (GS-5829) BET inhibitor

Name: Alobresib (GS-5829)
Brand: Selleck Chemicals
SKU: S8961
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8961

Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. This compound inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. It also inhibits NF-κB signaling.

Chemical Structure

Molecular Weight: 437.49

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Quality Control

Batch: S896101 DMSO]87 mg/mL]false]Ethanol]11 mg/mL]false]Water]˂1 mg/mL]false Purity: 98.15%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

98.15

Related Targets	HDAC JAK Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other BET Products	Molibresib (I-BET-762) AZD5153 6-hydroxy-2-naphthoic acid Mivebresib (ABBV-075) Pelabresib (CPI-0610) INCB054329 ZEN-3694 (BET-IN-19) Birabresib (OTX015) I-BET151 (GSK1210151A) Apabetalone (RVX-208) CPI-203

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (198.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 11 mg/mL

Water : ˂1 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	437.49	Formula	C₂₆H₂₃N₅O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1637771-14-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C(=NO1)C)C2=CC(=C3C(=C2)NC(=N3)C4CC4)C(C5=CC=CC=N5)(C6=CC=CC=N6)O

Mechanism of Action

Targets/IC₅₀/Ki	BET BLK Akt ERK1/2 MYC NF-κB
In vitro	In-vitro experiments demonstrates high sensitivity of USC cell-lines to the exposure to this compound causing a dose-dependent decrease in the phosphorylated levels of c-Myc and a dose-dependent increase in caspase activation (apoptosis). It inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. IκBα modulation indicates that this agent also inhibits NF-κB signaling. Its-induced apoptosis results from an imbalance between positive (BIM) and negative regulators (BCL-XL) of the intrinsic apoptosis pathway.
In vivo	Alobresib (GS-5829) has impressive activity against USC primary tumors as well as USC xenografts. Assessment of c-Myc expression in tumors exposed to this compound demonstrates down-regulation of both total and phospho c-Myc proteins. This chemical demonstrates excellent bioavailability after oral administration and is significantly more effective than JQ1 at the doses used in comparative experiments in vivo against USC xenografts. Clinical studies with this compound in USC patients harboring disease resistant to standard salvage chemotherapy are warranted.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29941483/ [2] https://pubmed.ncbi.nlm.nih.gov/31862959/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02983604	Terminated	Advanced Estrogen Receptor Positive HER2- Breast Cancer	Gilead Sciences	January 10 2017	Phase 1\|Phase 2
NCT02607228	Terminated	Metastatic Castrate-Resistant Prostate Cancer	Gilead Sciences	December 8 2015	Phase 1\|Phase 2
NCT02392611	Completed	Solid Tumors and Lymphomas	Gilead Sciences	March 16 2015	Phase 1

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