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A-674563 HCl (552325-73-2(free base))

产品编号 T4444 CAS 2070009-66-2

A-674563 HCl (552325-73-2(free base)) 是一种口服的、ATP 竞争性的、可逆的 Akt 抑制剂（Akt1 的 Ki：11 nM）。它对 PKA 和 Cdk2 具有抑制活性（IC50：16/46 nM），但对 Akt1 的选择性比 CMGC、CAMK 和 TK 家族中的其他激酶高 10 至 <1800 倍。

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A-674563 HCl (552325-73-2(free base)) Chemical Structure

A-674563 HCl (552325-73-2(free base)), CAS 2070009-66-2

规格	价格/CNY	货期
1 mg	￥ 750	现货
2 mg	￥ 1,080	现货
5 mg	￥ 1,360	现货
10 mg	￥ 1,900	现货
50 mg	特惠询价	现货
1 mL * 10 mM (in DMSO)	￥ 1,360	现货

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其他形式的 A-674563 HCl (552325-73-2(free base)):

A-674563
现货
A-674563 2HCl(552325-73-2(fb-2hcl))
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16/46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families [1].
靶点活性	ERK2:260 nM (Ki), PKCδ:360 nM (Ki), PKA:16 nM (Ki), CDK2:46 nM (Ki), Akt1:11 nM (Ki), GSK-3β:110 nM (Ki)
体外活性	A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro (EC50: 0.4 μM) [1]. A563 (0-10 μM) markedly 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 μM to 0.35 μM. A563 induces G2 cell cycle arrest and apoptosis in STS cells. A563 (1 μM/12 hr) upregulates the expression of GADD45A independent of p53[2]. 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[3]. A-674563 is cytotoxic and anti-proliferative when added to U937 and AmL progenitor cells activate caspase-3/9 and apoptosis in U937 and AmL progenitor cells and manipulate other signalings in AmL cells whiling blocking Akt[4].
体内活性	In the PC-3 prostate cancer xenograft model, A-674563 (40 mg/kg/d, p.o.) has no marked monotherapy activity, but the efficacy of the combination therapy (A-674563+paclitaxel) is significantly improved. In an oral glucose tolerance test, A-674563 (20, 100 mg/kg) can increase plasma insulin[1]. 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[2]. A-674563 (25, 100 mg/kg, lavage daily) effectively inhibits A375 xenograft growth in mice[3]. A-674563 (15, 40 mg/kg) injection inhibits U937 xenograft in vivo growth and improves mice survival[4].
细胞实验	The cells on 96-well plates are gently washed with 200 μL of PBS. Alamar Blue reagent is diluted 1:10 in normal growth media. The diluted Alamar Blue reagent (100 μL) is added to each well on the 96-well plates and incubated until the reaction is complete. The analysis is done using a fmax Fluorescence Microplate Reader, set at the excitation wavelength of 544 nm and the emission wavelength of 595 nm. Data are analyzed using SOFTmax PRO software.
动物实验	A-674563 is formulated in 5% dextrose.Immunocompromised male SCID mice are at 6 to 8 weeks of age. The 1×106 3T3-Akt1 or 2×106 MiaPaCa-2 and PC-3 cells in 50% Matrigel are inoculated s.c. into the flank. For early treatment studies, mice are randomly assigned to treatment groups and therapy is initiated the day after inoculation. Ten animals are assigned to each group, including controls. For established tumor studies, tumors are allowed to reach a designated size and mice are assigned to treatment groups of equal tumor size (n=10 mice per group). Tumor size is evaluated by twice-weekly measurements with digital calipers. Tumor volume is estimated using the formula: V=L×W2/2. A-443654 is given s.c. in a vehicle of 0.2% HPMC. A-674563 is given orally in a vehicle of 5% dextrose. Gemcitabine and paclitaxel are added to the assay.

分子量	394.9
分子式	C22H23ClN4O
CAS No.	2070009-66-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: >30 mg/mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Luo Y, Shoemaker A R, Liu X, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.[J]. Molecular Cancer Therapeutics, 2005, 4(6):977. 2. Zhu Q S, Ren W, Korchin B, et al. Soft Tissue Sarcoma Are Highly Sensitive to AKT Blockade: A Role for p53 Independent Up-regulation of GADD45α[J]. Cancer Research, 2008, 68(8):2895-2903. 3. Zou Y, Zhu Y R, Fan G, et al. Pre-clinical assessment of A-674563 as an anti-melanoma agent[J]. Biochemical & Biophysical Research Communications, 2016, 477(1):1-8. 4. Lin X, Zhang Y, Meng G, et al. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells[J]. Biochemical & Biophysical Research Communications, 2016, 472(4):662-668.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

A-674563 HCl (552325-73-2(free base)) 2070009-66-2 Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling MAPK PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors ERK PKA Akt CDK PKC A 674563 HCl (552325 73 2(free base)) A674563 HCl (552325732(free base)) Inhibitor inhibitor inhibit

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A-674563 HCl (552325-73-2(free base))

存储

溶解度

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输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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