GS5829,alobresib
- CAS No.
- 1637771-14-2
- Chemical Name:
- GS5829,alobresib
- Synonyms
- GS5829;GS5829,alobresib;Alobresib (GS-5829);Alobresib, 10 mM in DMSO;Inhibitor,GS5829,Alobresib,GS 5829,Epigenetic Reader Domain,inhibit;1H-Benzimidazole-7-methanol, 2-cyclopropyl-5-(3,5-dimethyl-4-isoxazolyl)-α,α-di-2-pyridinyl-
- CBNumber:
- CB74815564
- Molecular Formula:
- C26H23N5O2
- Molecular Weight:
- 437.5
- MDL Number:
- MFCD32174263
- MOL File:
- 1637771-14-2.mol
| 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 |
| FDA UNII | 3QBL0BLP3D |
GS5829,alobresib price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0031496 | Alobresib 98.07% | 1637771-14-2 | 5mg | $180 | 2021-12-16 | Buy |
| ChemScene | CS-0031496 | Alobresib 98.07% | 1637771-14-2 | 10mg | $350 | 2021-12-16 | Buy |
| ChemScene | CS-0031496 | Alobresib 98.07% | 1637771-14-2 | 25mg | $680 | 2021-12-16 | Buy |
| ChemScene | CS-0031496 | Alobresib 98.07% | 1637771-14-2 | 50mg | $1150 | 2021-12-16 | Buy |
| ChemScene | CS-0031496 | Alobresib 98.07% | 1637771-14-2 | 100mg | $1800 | 2021-12-16 | Buy |
GS5829,alobresib Chemical Properties,Uses,Production
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
GS5829,alobresib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Hebei Mujin Biotechnology Co.,Ltd | +86 13288715578 +8613288715578 | sales@hbmojin.com | China | 12809 | 58 |
| CR Corporation Limited | +8613062833949 | fred.wen@crcorporation.cn | China | 8647 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38630 | 58 | |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 12952 | 65 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 021-61312847; 18021002903 | 3008007409@qq.com | China | 71829 | 60 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9729 | 58 |