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

产品编号 T6139L CAS T6139L

A-674563 2HCl(552325-73-2(fb-2hcl)) 是一种 Akt1 抑制剂，Ki 为 11 nM，对 PKA 有效，对 Akt1 的选择性比 PKC 高 30 倍以上。

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A-674563 2HCl(552325-73-2(fb-2hcl)) Chemical Structure

A-674563 2HCl(552325-73-2(fb-2hcl)), CAS T6139L

规格	价格/CNY	货期
1 mg	￥ 757	现货
5 mg	￥ 1,360	现货
10 mg	￥ 1,920	现货
25 mg	￥ 3,430	现货
50 mg	￥ 4,980	现货
100 mg	￥ 6,950	现货
1 mL * 10 mM (in DMSO)	￥ 1,490	现货

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其他形式的 A-674563 2HCl(552325-73-2(fb-2hcl)):

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

选择批次

纯度: 99.57%

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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 Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
靶点活性	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.
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.
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	431.36
分子式	C22H24Cl2N4O
CAS No.	T6139L

存储

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

溶解度

DMSO: 27.5 mg/mL (63.75 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3182 mL	11.5912 mL	23.1825 mL	57.9562 mL
	5 mM	0.4636 mL	2.3182 mL	4.6365 mL	11.5912 mL
	10 mM	0.2318 mL	1.1591 mL	2.3182 mL	5.7956 mL
	20 mM	0.1159 mL	0.5796 mL	1.1591 mL	2.8978 mL
	50 mM	0.0464 mL	0.2318 mL	0.4636 mL	1.1591 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.

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 2HCl(552325-73-2(fb-2hcl)) T6139L Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling MAPK PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors ERK CDK PKC Akt PKA A 674563 2HCl(552325 73 2(fb 2hcl)) A674563 2HCl(552325732(fb2hcl)) Inhibitor inhibitor inhibit

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

存储

溶解度

溶液配制表

计算器

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

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords