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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Alobresib (GS-5829) is a novel and potent BET bromodomain inhibitor with anticancer activity. IIt may be used to treat USCs that are recurrent or chemotherapy-resistant and overexpress c-Myc.
| Targets |
BET; BLK; Akt; ERK1/2; MYC
|
|---|---|
| ln Vitro |
In-vitro research shows that USC cell lines are highly sensitive to the drug GS-5829, which results in a dose-dependent reduction in the level of phosphorylated c-Myc and an increase in caspase activation (apoptosis).[1] Through the deregulation of important signaling pathways like BLK, AKT, ERK1/2, and MYC, GS-5829 reduces CLL cell proliferation and triggers leukemia cell apoptosis. According to IκBα modulation, GS-5829 also suppresses NF-κB signaling. An imbalance between the positive (BIM) and negative (BCL-XL) regulators of the intrinsic apoptosis pathway causes GS-5829-induced apoptosis.[2]
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| ln Vivo |
GS-5829 has impressive activity against USC primary tumors as well as USC xenografts. In tumors exposed to GS-5829, analysis of the expression of c-Myc shows that both the total and phosphorylated forms of the protein are downregulated. When compared to JQ1 at the doses used in in vivo experiments against USC xenografts, GS-5829 significantly outperforms it in terms of bioavailability after oral administration. There is a need for clinical studies with the drug GS-5829 in USC patients who have disease that is resistant to conventional salvage chemotherapy. [1]
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| Cell Assay |
Following the manufacturer's instructions, MEC-1 cells treated for 72 hours with GS-5829 or the BCR signaling inhibitors are subjected to the TACS XTT cell proliferation/viability assay (Trevigen). Using technical triplicate measurements, half-maximal inhibitory concentrations (IC50) are computed.
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| Animal Protocol |
female CB17/lcrHsd-Prkd/scid mice bearing USC-ARK1 or USC-ARK2 xenograft
20 mg/kg, 10 mg/kg Oral gavage |
| References |
| Molecular Formula |
C26H23N5O2
|
|---|---|
| Molecular Weight |
437.5
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| Exact Mass |
437.1852
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| Elemental Analysis |
C, 71.38; H, 5.30; N, 16.01; O, 7.31
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| CAS # |
1637771-14-2
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| Related CAS # |
1637771-14-2
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C(=NO1)C)C2=CC(=C3C(=C2)NC(=N3)C4CC4)C(C5=CC=CC=N5)(C6=CC=CC=N6)O
|
| InChi Key |
CMSUJGUHYXQSOK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H23N5O2/c1-15-23(16(2)33-31-15)18-13-19(24-20(14-18)29-25(30-24)17-9-10-17)26(32,21-7-3-5-11-27-21)22-8-4-6-12-28-22/h3-8,11-14,17,32H,9-10H2,1-2H3,(H,29,30)
|
| Chemical Name |
[2-cyclopropyl-6-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-benzimidazol-4-yl]-dipyridin-2-ylmethanol
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| Synonyms |
Alobresib; GS 5829; GS5829; GS-5829
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| HS Tariff Code |
2934.99.9001
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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: 83.3~87 mg/mL (~198.9 mM)
Water: ˂1 mg/mL Ethanol: ~11 mg/mL (~25.1 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2857 mL | 11.4286 mL | 22.8571 mL | |
| 5 mM | 0.4571 mL | 2.2857 mL | 4.5714 mL | |
| 10 mM | 0.2286 mL | 1.1429 mL | 2.2857 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 |
| NCT02607228 | Terminated | Drug: Alobresib Drug: Enzalutamide |
Metastatic Castrate-Resistant Prostate Cancer |
Gilead Sciences | December 8, 2015 | Phase 1 Phase 2 |
| NCT02392611 | Completed | Drug: Alobresib Drug: Exemestane |
Solid Tumors and Lymphomas | Gilead Sciences | March 16, 2015 | Phase 1 |
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