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  • 化合物 AT7867 dihydrochloride|T21624|TargetMol

化合物 AT7867 dihydrochloride|T21624|TargetMol

AT7867 dihydrochloride
1431697-86-7
997 5mg 起订
591 2mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 AT7867 dihydrochloride
英文名称:
AT7867 dihydrochloride
CAS号:
1431697-86-7
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
产品类别:
抑制剂
货号:
T21624

Product Introduction

Bioactivity

NameAT7867 dihydrochloride
DescriptionAT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1 / Akt2 / Akt3 and p70S6K / PKA kinase with IC 50 s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively. AT7867 dihydrochloride is able to induce pharmacodynamic changes and inhibit human tumor xenograft growth.
In vitroAT7867 ATP-competitive inhibited AKT2 with the Ki of 18nM. AT7867 also shows potent activity against the structurally related AGC kinases p70S6K and PKA, but shows a clear window of selectivity against kinases from other kinase sub-families. In vitro growth inhibition studies show that AT7867 blocks proliferation in a number of human cancer cell lines. AT7867 appears to be most potent at inhibiting proliferation in MES-SA uterine, MDA-MB-468 and MCF-7 breast, and HCT116 and HT29 colon lines (IC 50 values range from 0.9-3 μM), and least effective in the two prostate lines tested (IC 50 values range from 10-12 μM) [1].
In vivoFollowing oral administration at 20 mg/kg, the elimination of AT7867 from plasma seems to be similar to that observed after i.v. administration. Plasma levels of AT7867 remain above 0.5 μM for at least 6 hours following an oral dose of 20 mg/kg. Assuming linear pharmacokinetics following i.v. administration, the bioavailability by the oral route is calculated to be 44%. In vivo pharmacodynamic (PD) biomarker studies are therefore performed with this model. Following pharmacokinetic and tolerability studies, doses of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) are administered to athymic mice bearing MES-SA tumors and the phosphorylation status of GSK3β and S6RP in tumors is monitored over time. Clear inhibition of phosphorylation of the two markers of pathway activity is seen at 2 and 6 hours following treatment with AT7867. By 24 hours, total levels of both GSK3β and S6RP are greatly reduced [1].
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
KeywordsAT 7867 | AT7867 | AT 7867 Dihydrochloride | AT-7867 Dihydrochloride | AT7867 dihydrochloride | AT7867 Dihydrochloride | AT-7867
AT7867 dihydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

化合物 AT7867 dihydrochloride相关厂家报价

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