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Cytoskeletal Signaling Akt A-674563 2HCl(552325-73-2(fb-2hcl))

A-674563 2HCl(552325-73-2(fb-2hcl))

Catalog No. T6139L   CAS T6139L

A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

A-674563 2HCl(552325-73-2(fb-2hcl)), CAS T6139L
Pack Size Availability Price/USD Quantity
1 mg In stock 87.00
5 mg In stock 157.00
10 mg In stock 221.00
25 mg In stock 394.00
50 mg In stock 592.00
100 mg In stock 888.00
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Purity 99.57%
Biological Description
Chemical Properties
Storage & Solubility Information
Description A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
Animal Research
A-674563 is formulated in 5% dextrose.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.
Animal Model:
Cell Research
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. The analysis is done using a fmax Fluorescence Microplate Reader, set at the excitation wavelength of 544 nm and the emission wavelength of 595 nm. Data are analyzed using SOFTmax PRO software.
Cell lines:
Molecular Weight 431.36
Formula C22H24Cl2N4O
CAS No. T6139L

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Luo Y, Shoemaker A R, Liu X, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.[J]. Molecular Cancer Therapeutics, 2005, 4(6):977. 2. Zhu Q S, Ren W, Korchin B, et al. Soft Tissue Sarcoma Are Highly Sensitive to AKT Blockade: A Role for p53 Independent Up-regulation of GADD45α[J]. Cancer Research, 2008, 68(8):2895-2903. 3. Zou Y, Zhu Y R, Fan G, et al. Pre-clinical assessment of A-674563 as an anti-melanoma agent[J]. Biochemical & Biophysical Research Communications, 2016, 477(1):1-8.

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