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A-674563 hydrochloride

Catalog No.GC35212

A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM.

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A-674563 hydrochloride Chemical Structure

Cas No.: 2070009-66-2

Size Price Stock Qty
10mM (in 1mL DMSO)
$128.00
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2mg
$84.00
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5mg
$147.00
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10mg
$231.00
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50mg
$697.00
In stock
100mg
$1,050.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM. Akt1|11 nM (Ki)|PKA|16 nM (Ki)|CDK2|46 nM (Ki)|GSK3β|110 nM (Ki)|ERK2|260 nM (Ki)|PKCδ|360 nM (Ki)|RSK2|580 nM (Ki)|MAPK-AP2|1.1 μM (Ki)|PKCγ|1.2 μM (Ki)|Chk1|2.6 μM (Ki)|CK2|5.4 μM (Ki)|SRC|13 μM (Ki)

A-674563 slows proliferation of tumor cells with an EC50 of 0.4 μM[1]. A563 (0-10 µM) significantly 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±0.034 µM (SW684) to 0.35 ±0.06 µM (SKLMS1). 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, activates caspase-3/9 and apoptosis in U937 and AmL progenitor cells, and manipulates other signalings in AmL cells whiling blocking Akt[4].

A-674563 (40 mg/kg/d, p.o.) shows no significant monotherapy activity, but the efficacy of the combination therapy (A-674563+paclitaxel) is significantly improved in the PC-3 prostate cancer xenograft model. A-674563 (20, 100 mg/kg) increases plasma insulin in an oral glucose tolerance test[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) potently 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].

[1]. Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther, 2005, 4(6), 977-986. [2]. Zhu QS, 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, 68(8), 2895-2903. [3]. Zou Y, et al. Pre-clinical assessment of A-674563 as an anti-melanoma agent. Biochem Biophys Res Commun. 2016 Aug 12;477(1):1-8. [4]. Xu L, et al. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells. Biochem Biophys Res Commun. 2016 Apr 15;472(4):662-8.

Chemical Properties

Cas No. 2070009-66-2 SDF
Canonical SMILES N[C@@H](CC1=CC=CC=C1)COC2=CC(C3=CC4=C(C=C3)NN=C4C)=CN=C2.[H]Cl
Formula C22H23ClN4O M.Wt 394.9
Solubility H2O:100 mg/mL (253.23 mM; Need ultrasonic); DMSO:62.5 mg/mL (158.27 mM; Need ultrasonic) Storage -20°C, stored under nitrogen
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

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1 mg 5 mg 10 mg
1 mM 2.5323 mL 12.6614 mL 25.3229 mL
5 mM 0.5065 mL 2.5323 mL 5.0646 mL
10 mM 0.2532 mL 1.2661 mL 2.5323 mL
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