Home Epigenetics Epigenetic Reader Domain inhibitor - Akt modulator - ERK modulator - Myc modulator - NF-κB inhibitor - Apoptosis related activator Alobresib (GS-5829) For research use only.

Alobresib (GS-5829)

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

Alobresib (GS-5829) Chemical Structure

Alobresib (GS-5829) Chemical Structure

CAS: 1637771-14-2

Purity & Quality Control

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

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Biological Activity

Description Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
Targets
BET [1] BLK [2] Akt [2] ERK1/2 [2] MYC [2] Click to View More Targets
In vitro
In vitro

In-vitro experiments demonstrates high sensitivity of USC cell-lines to the exposure to GS-5829 causing a dose-dependent decrease in the phosphorylated levels of c-Myc and a dose-dependent increase in caspase activation (apoptosis).[1] GS-5829 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 GS-5829 also inhibits NF-κB signaling. GS-5829-induced apoptosis results from an imbalance between positive (BIM) and negative regulators (BCL-XL) of the intrinsic apoptosis pathway.[2]
Cell Research Cell lines PBMC, MEC-1
Concentrations 100 nM, 200 nM, 400 nM, 800 nM
Incubation Time 72 h, 24 h
Method

TACS XTT cell proliferation/viability assay (Trevigen) is performed according to the manufacturer’s instructions on MEC-1 cells treated with GS-5829 or the BCR signaling inhibitors for 72 h. Half-maximal inhibitory concentrations (IC50) are calculated using Prism 6 or 7 based on technical triplicate measurements.
In Vivo
In vivo

GS-5829 has impressive activity against USC primary tumors as well as USC xenografts. Assessment of c-Myc expression in tumors exposed to the GS-5829 demonstrates down-regulation of both total and phospho c-Myc proteins. GS-5829 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 GS-5829 in USC patients harboring disease resistant to standard salvage chemotherapy are warranted.[1]
Animal Research Animal Models female CB17/lcrHsd-Prkd/scid mice bearing USC-ARK1 or USC-ARK2 xenograft
Dosages 20 mg/kg, 10 mg/kg
Administration Oral gavage
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

Chemical lnformation & Solubility

Molecular Weight 437.49 Formula

C26H23N5O2
CAS No. 1637771-14-2 SDF --
Smiles CC1=C(C(=NO1)C)C2=CC(=C3C(=C2)NC(=N3)C4CC4)C(C5=CC=CC=N5)(C6=CC=CC=N6)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (198.86 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : ˂1 mg/mL


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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