Alobresib|1637771-14-2|-陌孚医药/Medlife

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Alobresib

目录号: PL13451 纯度: ≥98%

CAS No. :1637771-14-2

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中文名称	Alobresib
英文名称	Alobresib
英文别名	Alobresib;3QBL0BLP3D;Alobresib [INN];BDBM249306;DB14970;(2-Cyclopropyl-6-(3,5-dimethyl-1,2-oxazol-4-yl)-1hbenzimidazol-4-yl)(dipyridin-2-yl)methanol;GS-5829
Cas No.	1637771-14-2
分子式	C₂₆H₂₃N₅O₂
分子量	437.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Alobresib (GS-5829) 是一种 BET 溴结构域抑制剂。Alobresib 可有效对抗复发且耐药的过表达 c-Myc 的子宫浆液性癌。Alobresib 可用于转移性去势抵抗性前列腺癌 (mCRPC) 研究。

生物活性

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.

性状

Solid

IC50 & Target[1][2]

BET bromodomain

体外研究(In Vitro)

Alobresib (0.1 nM-100 μM; 72 hours) inhibits cell proliferation in primary uterine serous carcinoma (USC) lines. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.
[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.

溶解度数据	In Vitro: DMSO : 83.33 mg/mL (190.47 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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