Afuresertib hydrochloride|1047645-82-8|(GSK2110183 hydrochloride; LAE002 hydrochloride)-陌孚医药/Medlife

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Afuresertib hydrochloride (Synonyms: GSK2110183 hydrochloride; LAE002 hydrochloride)

目录号: PL04513 纯度: ≥99%

CAS No. :1047645-82-8

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中文名称	Afuresertib hydrochloride
英文名称	Afuresertib hydrochloride
英文别名	GSK 2110183 hydrochloride;Afuresertib hydrochloride;GSK2110183B;N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide,hydrochloride;N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride;Afuresertib HCl;GSK-2110183 hydrochloride;UNII-0FC27E442O;GSK 2110183B;GSK-2110183B;GSK2110183 hydrochloride;Afuresertib (hydrochloride);Afuresertib HCl (GSK2110183);Afuresertib HCl salt, GSK-2110183 HCl salt, GSK-2110183B HCl salt;Afuresertib hydrochloride [USAN];0FC27E442O;Afuresertib hydrochloride (USAN);AK171367;YFQJOPFTGMHYNV-YDALLXLXSA-N;GSK2110183B; Afuresertib HCl;N-((S)-1-Amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide hydrochloride;BCP19741
Cas No.	1047645-82-8
分子式	C₁₈H₁₈Cl₃FN₄Os
分子量	463.78
包装储存	-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

产品详情

Afuresertib hydrochloride (GSK 2110183 hydrochloride) 是一个口服有效的，ATP 竞争性的选择性 pan-Akt 抑制剂，作用于 Akt1/Akt2/Akt3，K_i 值分别为 0.08/2/2.6 nM。

生物活性

Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K i s of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.

性状

Solid

IC50 & Target[1][2]

Akt1 0.08 nM (Ki) Akt2 2 nM (Ki)

体外研究(In Vitro)

Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase.
Western blotting analysis shows that Afuresertib increases the expression of p21 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC , which are associated with fibroblast core serum response. has not independently confirmed the a

体内研究(In Vivo)

Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts. 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

-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

ClinicalTrial

参考文献

[1]. Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659.
[2]. Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880

溶解度数据	In Vitro: DMSO : 100 mg/mL (215.62 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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