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Alobresib (GS-5829)

  Cat. No.:  DC11887   Featured
Chemical Structure
1637771-14-2
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More than 5000 active chemicals with high quality for research!
Field of application
Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity..
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1637771-14-2
Chemical Name: [2-cyclopropyl-6-(3,5-dimethyl-1,2-oxazol-4-yl)- 1H-benzimidazol-4-yl]di(pyridin-2-yl)methanol
Synonyms: GS-5829;GS 5829;GS5829
SMILES: C(C1=C2C(=CC(C3=C(C)ON=C3C)=C1)NC(C1CC1)=N2)(C1=NC=CC=C1)(C1=NC=CC=C1)O
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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[1].
Target: BET bromodomain[1]
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.)[1]. 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[1]. Animal Model: Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors[1] Dosage: 10 and 20 mg/kg Administration: Oral; twice-daily; 28 days Result: Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).
In Vitro: Alobresib (0.1 nM-100 μM; 72 hours) inhibits cell proliferation in primary uterine serous carcinoma (USC) lines[1]. Cell Proliferation Assay[1] Cell Line: Primary uterine serous carcinoma (USC) lines ARK1 and ARK2 cell lines Concentration: 0.1 nM, 10 nM, 1 μM, 100 μM Incubation Time: 72 hours Result: A progressive, dose response decrease in cell proliferation. IC50s of 27 nM and 31 nM for ARK2 and ARK1 cells, respectively.
References: [1]. Bonazzoli E, et al. Inhibition of BET Bromodomain Proteins with GS-5829 and GS-626510 in Uterine Serous Carcinoma, a Biologically Aggressive Variant of Endometrial Cancer. Clin Cancer Res. 2018 Oct 1;24(19):4845-4853.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC11887 Alobresib (GS-5829) Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity..
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