store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-674563 是一种口服有效,选择性的Akt1抑制剂,Ki=11 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 699 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,920 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,280 | 现货 |
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 | Akt1:11 nM(Ki) |
体外活性 | A-674563 is achieved from A-443654 by replacing the indole with a phenyl moiety and getting oral activity. A-674563 slows proliferation of tumor cells with EC50 of 0.4 μM. [1] A-674563 does not inhibit Akt phosphorylation per se, but blocks the phosphorylation of Akt downstream targets in a dose-dependent manner. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 induces G2 cell cycle arrest and apoptosis in STS cells. [2] |
体内活性 | 20 mg/kg A-674563 increases plasma insulin in an oral glucose tolerance test. A-674563 shows no significant monotherapy tumor inhibitory activity; the efficacy of the combination therapy is significantly improved compared to paclitaxel monotherapy. [1] A674563-treated (20 mg/kg/bid, p.o.) mice exhibits slower tumor growth and more than 50% decrease in the tumor volume at the termination of the study compared with that in control group. [2] A-674563 is identified to have drastically improved PK profile with oral bioavailability of 67% in mouse, but is 70-fold less active than A-443654. [3] |
激酶实验 | Akt Kinase Assay: The kinase assay uses His-Akt1 and a biotinylated mouse Bad peptide as substrate. The kinase assay is carried out at room temperature for 30 minutes in 50 μL of reaction buffer [20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.1% (w/v) Triton X-100, 5 μM ATP (Km = 40 μM), 5 μM peptide (Km = 15 μM), 1 mM DTT, 60 ng of Akt1, and 0.5 μCi of [γ-33P]ATP] in the presence of different concentrations of A-674563. Each reaction is stopped by adding 50 μL of termination buffer (0.1 M EDTA, pH 8.0, and 4 M NaCl). The biotinylated Bad peptides are immobilized on streptavidin-coated FLASH plates. After being washed with PBS-Tween 20 (0.05%), the 33P phosphopeptide captured on the FLASH plates is measured with a TopCount Packard Instruments γ counter. |
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 M) is added to each well on the 96-well plates and incubated until the reaction is complete as per manufacturer's instructions. Analysis is done using an fmax Fluorescence Microplate Reader, set at the excitation wavelength of 544 nm and emission wavelength of 595 nm. Data are analyzed using SOFTmax PRO software provided by the manufacturer. (Only for Reference) |
别名 | A674563 |
分子量 | 358.44 |
分子式 | C22H22N4O |
CAS No. | 552325-73-2 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 66 mg/mL (184.1 mM)
DMSO: 67 mg/mL (186.9 mM)
Ethanol: 15 mg/mL (41.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO / Ethanol | 1 mM | 2.7899 mL | 13.9493 mL | 27.8987 mL | 69.7467 mL |
5 mM | 0.558 mL | 2.7899 mL | 5.5797 mL | 13.9493 mL | |
10 mM | 0.279 mL | 1.3949 mL | 2.7899 mL | 6.9747 mL | |
20 mM | 0.1395 mL | 0.6975 mL | 1.3949 mL | 3.4873 mL | |
H2O / DMSO | 50 mM | 0.0558 mL | 0.279 mL | 0.558 mL | 1.3949 mL |
100 mM | 0.0279 mL | 0.1395 mL | 0.279 mL | 0.6975 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
A-674563 552325-73-2 Cell Cycle/Checkpoint Cytoskeletal Signaling MAPK PI3K/Akt/mTOR signaling Stem Cells Tyrosine Kinase/Adaptors GSK-3 ERK Akt PKA CDK Protein kinase B PKB inhibit A674563 A 674563 Inhibitor inhibitor