| Identification | Back Directory | [Name]
GS5829,alobresib | [CAS]
1637771-14-2 | [Synonyms]
GS5829
GS5829,alobresib
Alobresib (GS-5829)
1H-Benzimidazole-7-methanol, 2-cyclopropyl-5-(3,5-dimethyl-4-isoxazolyl)-α,α-di-2-pyridinyl- | [Molecular Formula]
C26H23N5O2 | [MDL Number]
MFCD32174263 | [MOL File]
1637771-14-2.mol | [Molecular Weight]
437.49 |
| Chemical Properties | Back Directory | [Boiling point ]
718.9±60.0 °C(Predicted) | [density ]
1.349±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:83.33(Max Conc. mg/mL);190.47(Max Conc. mM) | [form ]
A solid | [pka]
10.43±0.30(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research[1][2]. | [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.). |
| [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. DOI:10.1158/1078-0432.CCR-18-0864
[2] Rahul Aggarwal, et al. Phase Ib Study of the BET Inhibitor GS-5829 as Monotherapy and Combined with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer. Clin Cancer Res. 2022 Sep 15;28(18):3979-3989. DOI:10.1158/1078-0432.CCR-22-0175 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|