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A-674563 Akt1/PKA/CDK2 inhibitor,potent and selective

Catalog No.A8616
Size Price Stock Qty
10mM (in 1mL DMSO)
$154.00
In stock
5mg
$140.00
In stock
10mg
$210.00
In stock
50mg
$630.00
In stock
100mg
$980.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

A-674563

Biological Activity

Description A-674563 is an inhibitor of Akt1 with a Ki value of 11 nM.
Targets Akt1 PKA CDK2 GSK-3β ERK2  
IC50 11 nM(Ki) 16 nM(Ki) 46 nM(Ki) 110 nM(Ki) 260 nM(Ki)  

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.

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Chemical Properties

Cas No. 552325-73-2 SDF Download 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
Solubility >4.9mg/ml in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.