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A-674563

カタログ番号GC11875

A-674563 は、Ki が 11 nM の経口活性の選択的 Akt1 阻害剤です。

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A-674563 化学構造

Cas No.: 552325-73-2

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$116.00
在庫あり
5mg
$102.00
在庫あり
10mg
$152.00
在庫あり
50mg
$447.00
在庫あり
100mg
$733.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

soft tissue sarcoma (STS) cell lines

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-10 μM; 24, 48, and 72 h

Applications

In STS cell lines, A-674563 significantly decreased GSK3 and MDM2 phosphorylation in a dose-dependent way. A-674563 induced growth inhibition in a dose-dependent and time-dependent manner, and induced G2 cell cycle arrest and apoptosis.

Animal experiment [1]:

Animal models

Mice with human fibrosarcoma (HT1080) subcutaneous xenografts

Dosage form

20 mg/kg/bid, p.o.

Application

In mice with human fibrosarcoma (HT1080) subcutaneous xenografts, A-674563 inhibited tumor growth and significantly reduced tumor volume at the termination of the study (320.76 ± 86.8) compared with that in control group (667.92 ± 97.41; P < 0.01).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Zhu QS, Ren W, Korchin B et al. Soft tissue sarcoma cells are highly sensitive to AKT blockade: a role for p53-independent up-regulation of GADD45 alpha. Cancer Res. 2008 Apr 15;68(8):2895-903.

Background

A-674563 is a potent and selective Akt1 inhibitor with IC50 value of 14 nM. A-67453 also inhibited PKA and Cdk2 with IC50 value of 16 nM and 46 nM.

Akt, also known as protein kinase B, is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.

In MiaPaCa-2 cells treated with A-674563 for 48 hour, it slowed the tumor cell proliferation (EC50 = 0.4 μm). In STS cells, phosphorylation of GSK3 and MDM2 was prominently reduced by A-674563 treatment. [1] Akt inhibition-induced G2 cells cycle arrest and apoptosis were also observed in A563-treated STS cells. [2]

In scid mice carrying established PC-3 tumors, administration of A-674563 at 40 mg/kg per day for 21 days, combined with administration of paclitaxel at 15 mg/kg per day on days 20.24.28, increased the efficacy of paclitaxel compared with paclitaxel monotherapy. [1] A563 also significantly blocked HT1080 xenograft growth in nude mice. [2]

References:
1.  Luo Y, Shoemaker AR, Liu X et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005 Jun;4(6):977-86.
2.  Zhu QS, Ren W, Korchin B et al. Soft tissue sarcoma cells are highly sensitive to AKT blockade: a role for p53-independent up-regulation of GADD45 alpha. Cancer Res. 2008 Apr 15;68(8):2895-903.

Chemical Properties

Cas No. 552325-73-2 SDF
Chemical Name (2S)-1-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxy-3-phenylpropan-2-amine
Canonical SMILES CC1=C2C=C(C=CC2=NN1)C3=CC(=CN=C3)OCC(CC4=CC=CC=C4)N
Formula C22H22N4O M.Wt 358.44
溶解度 ≥ 4.9mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.7899 mL 13.9493 mL 27.8987 mL
5 mM 0.558 mL 2.7899 mL 5.5797 mL
10 mM 0.279 mL 1.3949 mL 2.7899 mL
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**ストックソリューションを準備する際には、常にバイアルラベルおよび MSDS/CoA(オンラインで利用可能)で掲載された製品のロット固有分子量を使用してください。

計算

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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