1. PI3K/Akt/mTOR
  2. Akt
  3. A-674563 hydrochloride

A-674563 hydrochloride 

Cat. No.: HY-13254A Purity: 99.78%
Handling Instructions

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

For research use only. We do not sell to patients.

A-674563 hydrochloride Chemical Structure

A-674563 hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1212 In-stock
Estimated Time of Arrival: December 31
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Description

A-674563 hydrochloride is a potent and selective Akt1 inhibitor with 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)

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±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].

In Vivo

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].

Molecular Weight

394.90

Formula

C₂₂H₂₃ClN₄O

SMILES

N[[email protected]@H](CC1=CC=CC=C1)COC2=CC(C3=CC4=C(C=C3)NN=C4C)=CN=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (253.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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 μL) is added to each well on the 96-well plates and incubated until the reaction is complete. 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.

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

Animal Administration
[1]

Immunocompromised male scid mice are at 6 to 8 weeks of age. The 1×106 3T3-Akt1 or 2×106 MiaPaCa-2 and PC-3 cells in 50% Matrigel are inoculated s.c. into the flank. For early treatment studies, mice are randomLy assigned to treatment groups and therapy is initiated the day after inoculation. Ten animals are assigned to each group, including controls. For established tumor studies, tumors are allowed to reach a designated size and mice are assigned to treatment groups of equal tumor size (n=10 mice per group). Tumor size is evaluated by twice weekly measurements with digital calipers. Tumor volume is estimated using the formula: V=L×W2/2. A-443654 is given s.c. in a vehicle of 0.2% HPMC. A-674563 is given orally in a vehicle of 5% dextrose. Gemcitabine and paclitaxel are added to the assay.

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

References
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Keywords:

A-674563A674563A 674563AktPKBProtein kinase BInhibitorinhibitorinhibit

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Product Name:
A-674563 hydrochloride
Cat. No.:
HY-13254A
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