A-674563 hydrochloride|98%|abs818558-爱必信(上海)生物科技有限公司

A-674563 hydrochloride

参考价：¥2016

供货周期：

一周

品牌：

爱必信

规格：

98%

货号：

abs818558

CAS号：

552325-73-2(free base)

产品详情

公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!

抑制剂描述：

产品名称：A-674563 hydrochloride

产品别名：见爱必信官网

英文别名：A-674563 hydrochloride

靶点：Akt

CAS：552325-73-2(free base)

纯度：98%

外观：见爱必信官网

保存方法：Store at -20°C

描述：

A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM.

溶解性：DMSO : ≥ 30 mg/mL (75.97 mM)

体外研究：

A-674563 slows proliferation of tumor cells with an EC50 of 0.4 μM. A563 (0-10 μM) significantly decreases GSK3 and MDM2 phosphorylation in STS cells. A563 shows inhibitory effect on all STS cell lines, with IC50 values at 48 hours ranging from 0.22±0.034 μM (SW684) to 0.35 ±0.06 μM (SKLMS1). A563 induces G2 cell cycle arrest and apoptosis in STS cells. A563 (1 μM/12 hr) upregulates the expression of GADD45A independent of p53. A-674563 (10-1000 nM) is anti-proliferative and cytotoxic in cultured human melanoma cells, induces melanoma cell apoptotic death, inhibited by caspase inhibitors, and inhibits melanoma cells via Akt-dependent and -independent mechanisms. A-674563 is cytotoxic and anti-proliferative when added to U937 and AmL progenitor cells, activates caspase-3/9 and apoptosis in U937 and AmL progenitor cells, and manipulates other signalings in AmL cells whiling blocking Akt.

体内研究：A-674563 (40 mg/kg/d, p.o.) shows no significant monotherapy activity, but the efficacy of the combination therapy (A-674563+paclitaxel) is significantly improved in the PC-3 prostate cancer xenograft model. A-674563 (20, 100 mg/kg) increases plasma insulin in an oral glucose tolerance test. A563 (20 mg/kg/bid; p.o.) exhibits slow tumor growth and a significant difference in tumor volume without significant weight loss of mice. A563-treated tumors express increased levels of GADD45α and decreased levels of PCNA (a nuclear marker for proliferation). Additionally, TUNEL assay staining levels (marker for apoptosis) increase in the A563-treated specimens. A-674563 (25, 100 mg/kg, lavage daily) potently inhibits A375 xenograft growth in mice. A-674563 (15, 40 mg/kg) injection inhibits U937 xenograft in vivo growth, and improves mice survival.

产品信息订购：

产品货号	产品名称	规格	价格	大包装及货期
abs818558	A-674563 hydrochloride	2mg	2016.00	立即咨询
abs818558	A-674563 hydrochloride	5mg	3528.00	立即咨询

产品更多信息请进入爱必信网站咨询