Description
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc.
Product information
CAS Number: 1637771-14-2
Molecular Weight: 437.49
Formula: C26H23N5O2
Chemical Name: [2-cyclopropyl-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-1,3-benzodiazol-7-yl]bis(pyridin-2-yl)methanol
Smiles: CC1ON=C(C)C=1C1=CC(=C2NC(=NC2=C1)C1CC1)C(O)(C1=CC=CC=N1)C1=CC=CC=N1
InChiKey: CMSUJGUHYXQSOK-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 83.33 mg/mL (190.47 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Alobresib (0.1 nM-100 μM; 72 hours) inhibits cell proliferation in primary uterine serous carcinoma (USC) lines.
In Vivo:
Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) impaires USC-ARK2 xenograft tumor growth in female CB17/lcrHsd-Prkd/scid mice. Alobresib exhibits a significantly slower rate of tumor growth in mice, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.). Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) is well tolerated with no clear impact on body weight compared with vehicle control.
Products are for research use only. Not for human use.
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