Akti-1/2 (AKT inhibitor VIII)

Alias: Sigma-A6730; AKT inhibitor VIII; AKT inhibitor-8; AKT-inhibitor-VIII; AKT-inhibitor-8; Akt-I 1,2; Akti-1/2
Cat No.:V0173 Purity: ≥98%
Akti-1/2 (known also as AKT inhibitor VIII), aquinoxaline-based compound,is a novel, potent, selective,cell-permeable and allosteric inhibitor of Akt1/2 with potential anticancer activity.
Akti-1/2 (AKT inhibitor VIII) Chemical Structure CAS No.: 612847-09-3
Product category: Akt
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Akti-1/2 (AKT inhibitor VIII):

  • PF-AKT400
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Akti-1/2 (known also as AKT inhibitor VIII), a quinoxaline-based compound, is a novel, potent, selective, cell-permeable and allosteric inhibitor of Akt1/2 with potential anticancer activity. It has an IC50 of 58 nM for Akt1 and 210 nM for Akt2, respectively, and is about 36-fold more selective for Akt1 than Akt3. AKTi-1/2. Akts, PKA, PKC, and SGK lacking the pleckstrin homology (PH) domain did not exhibit any inhibition.

Biological Activity I Assay Protocols (From Reference)
Targets
Akt1 (IC50 = 58 nM); Akt2 (IC50 = 210 nM); Akt3 (IC50 = 2119 nM)
ln Vitro
Akti-1/2 inhibits Akt1 and Akt2 with an IC50 of 305 nM and 2086 nM, respectively, in a cell-based IPKA (C33A) assay. Akti-1/2 causes cell apoptosis in HT29, MCF7, and A2780 cells by significantly raising caspase-3 activity. [1]
Akti-1/2 prevents insulin from controlling the expression of PEPCK, G6Pase, and FOXO1 in liver cells. [2]
Akti-1/2 also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. [3]
Akti-1/2 inhibits cell growth in HCC827, NCI-H522, NCI-1651, and PC-9 cells with IC50 values of 4.7 μM, 7.25 μM, and 9.5 μM; when combined with gefitinib, Akti-1/2 results in enhanced inhibition of cell growth and apoptosis. [4]
ln Vivo
Akti-1/2 (50 mg/kg, i.p.) inhibits lung Akt1 and Akt2 phosphorylation in mice at both basal and IGF-stimulated levels.AKT inhibitor VIII (50 mpk, 3 doses, ip, every 90 min) is administered to mice to achieve plasma concentrations of 1.5–2.0 μM. IGF is then administered intravenously to the animals' tail veins to promote Akt phosphorylation. Both basal and IGF-stimulated Akt1 and Akt2 phosphorylation are inhibited by IP Western in mouse lung, but Akt3 phosphorylation is unaffected.
Enzyme Assay
Briefly, a Biomek 2000 Laboratory Automation Workstation in a 96-well format is used to carry out all assays (25.5 μl at 21°C for 30 min). The addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-33P]-, 800 cpm/pmol) initiates reactions that contain 5–20 mU purified kinase and substrate protein or peptide.
Cell Assay
Using the 96-hour sulforhodamine B assay (SRB), it is possible to determine how AKTi-1/2 inhibits cell growth. The sigmoidal dose-response (variable slope) equation and non-linear regression analysis are used in GraphPad Prism 6.0 to calculate the drug concentrations that inhibited 50% of cell growth (IC50) for each compound.
Animal Protocol
C57BL/6 J mice
50 mg/kg
i.p.
References

[1]. Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4.

[2]. Diabetes. 2007 Sep;56(9):2218-27.

[3]. J Thromb Haemost. 2008 Nov;6(11):1923-32.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C34H29N7O
Molecular Weight
551.6404
Exact Mass
551.24336
Elemental Analysis
C, 74.03; H, 5.30; N, 17.77; O, 2.90
CAS #
612847-09-3
Appearance
Solid powder
SMILES
C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=C(N=C6C=C7C(=NC=N7)C=C6N5)C8=CC=CC=C8
InChi Key
BIWGYFZAEWGBAL-UHFFFAOYSA-N
InChi Code
InChI=1S/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42)
Chemical Name
3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
Synonyms
Sigma-A6730; AKT inhibitor VIII; AKT inhibitor-8; AKT-inhibitor-VIII; AKT-inhibitor-8; Akt-I 1,2; Akti-1/2
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~22 mg/mL (~39.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8128 mL 9.0639 mL 18.1278 mL
5 mM 0.3626 mL 1.8128 mL 3.6256 mL
10 mM 0.1813 mL 0.9064 mL 1.8128 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Status Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00897663 Completed Genetic: microarray analysis
Genetic: gene expression
analysis
Brain and Central Nervous
System Tumors
Alliance for Clinical
Trials in Oncology
November 2006 Phase 3
NCT00671970 Completed Drug: Bevacizumab and
Erlotinib
Glioblastoma
Gliosarcoma
Duke University February 2007 Phase 2
Biological Data
  • Akti-1/2

  • Akti-1/2
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