Reagents and instruments for immunology, cell biology and molecular biology.
 
> A-674563 [552325-73-2]

A-674563 [552325-73-2]

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Cat# HY-13254-10mg

Size : 10mg

Brand : MedChemExpress

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Phone : +1 850 650 7790

Description

A-674563 is an orally active Akt1 inhibitor with a Ki of 11 nM.

IC50 & Target[1]

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)

Cellular Effect
Cell Line Type Value Description References
MIA PaCa-2 EC50
0.4 μM
Compound: 11g
Antiproliferative activity against human MiaPaCa2 cell line
Antiproliferative activity against human MiaPaCa2 cell line
[PMID: 16678413]
MOLM-13 EC50
0.17 μM
Compound: 17; A674563
Cytotoxicity against human MOLM13 cells
Cytotoxicity against human MOLM13 cells
[PMID: 31207462]
MOLM-14 EC50
0.06 μM
Compound: 17; A674563
Cytotoxicity against human MOLM14 cells
Cytotoxicity against human MOLM14 cells
[PMID: 31207462]
MV4-11 EC50
0.092 μM
Compound: 17; A674563
Cytotoxicity against human MV4-11 cells
Cytotoxicity against human MV4-11 cells
[PMID: 31207462]
Sf9 IC50
>100 μM
Compound: A674563
Inhibition of Akt1 (1 to 480) expressed in Sf9 cells by indirect affinity mass spectrometry assay
Inhibition of Akt1 (1 to 480) expressed in Sf9 cells by indirect affinity mass spectrometry assay
[PMID: 22533986]
In Vitro

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 μM (SW684) to 0.35 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A-674563 Related Antibodies

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (232.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7899 mL 13.9493 mL 27.8987 mL
5 mM 0.5580 mL 2.7899 mL 5.5797 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 5.75 mg/mL (16.04 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Purity & Documentation
References

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