| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
The primary targets of Akt-I-1,2 are Akt1 and Akt2, two isoforms of the serine/threonine protein kinase Akt (also known as protein kinase B). Akt-I-1,2 acts as a selective, non-ATP-competitive inhibitor. This means it does not compete with ATP for binding to the kinase active site, but rather binds to an allosteric site or otherwise inhibits kinase activity through a non-ATP-competitive mechanism. By inhibiting Akt1 and Akt2, the compound blocks downstream signaling pathways involved in cell survival and proliferation.
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| ln Vitro |
In vitro, Akt-I-1,2 demonstrates selective inhibition of Akt1 and Akt2. The compound's activity is assessed in kinase assays using recombinant Akt1 and Akt2 enzymes and peptide substrates. The compound's non-ATP-competitive mechanism of action is confirmed by performing the assay at different ATP concentrations. The compound's effects on cell viability and apoptosis are assessed in cancer cell lines. However, detailed IC50 values are not extensively reported.
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| ln Vivo |
In vivo data for Akt-I-1,2 are not extensively reported in the available literature. As a selective inhibitor of Akt1 and Akt2, the compound has potential for in vivo applications in cancer models. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical.
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| Enzyme Assay |
In vitro enzyme assays for Akt-I-1,2 typically involve measuring its inhibition of Akt1 and Akt2 kinase activity. Recombinant Akt1 or Akt2 enzymes are incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. The incorporation of phosphate into the substrate is measured, and the IC50 for inhibition is calculated. The non-ATP-competitive nature of the inhibition is confirmed by performing the assay at different ATP concentrations.
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| Cell Assay |
Cellular assays for Akt-I-1,2 are performed in cancer cell lines to assess its effects on Akt signaling and cell viability. Cells are treated with the compound, and the phosphorylation of Akt substrates (e.g., GSK3β, PRAS40) is measured by Western blotting. Cell viability is assessed using assays such as MTT or resazurin reduction. Apoptosis is measured by flow cytometry using Annexin V staining or by measuring caspase activity.
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| Animal Protocol |
In vivo animal studies with Akt-I-1,2 are not extensively documented in the available literature. Based on its inhibition of Akt1 and Akt2, potential in vivo models could include xenograft models for cancer. In such studies, Akt-I-1,2 would be administered systemically, and tumor growth would be monitored. However, specific protocols are not detailed in the available sources.
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| ADME/Pharmacokinetics |
Akt-I-1,2 has a molecular weight of 375.89 and a molecular formula of C23H22ClN3. It is typically dissolved in DMSO for in vitro studies. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Akt-I-1,2 are not extensively reported. The compound is classified as a research-use-only chemical and is not intended for human consumption. As an inhibitor of Akt signaling, it may have effects on normal cell survival and proliferation that could contribute to toxicity. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References |
: Yamaji M, Ota A, Wahiduzzaman M, Karnan S, Hyodo T, Konishi H, Tsuzuki S, Hosokawa Y, Haniuda M. Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. doi: 10.1002/cam4.1179. Epub 2017 Sep 27. PubMed PMID: 28960945; PubMed Central PMCID: PMC5673922.
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| Additional Infomation |
Akt-I-1,2 is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying the Akt signaling pathway in cancer biology. The compound is used to investigate the role of Akt1 and Akt2 in tumorigenesis, cell survival, and proliferation. Its non-ATP-competitive mechanism of action makes it a valuable tool for studying the structure and function of Akt kinases and for validating Akt as a therapeutic target.
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| Molecular Formula |
C23H22CLN3
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|---|---|
| Molecular Weight |
375.9
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| Exact Mass |
375.15
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| CAS # |
473382-50-2
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| Related CAS # |
473382-50-2
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| PubChem CID |
73014064
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
6.659
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
448
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].N([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C1C([H])=C([H])C(C2C(C3C([H])=C([H])C([H])=C([H])C=3[H])=NC3=C([H])C([H])=C([H])C([H])=C3N=2)=C([H])C=1[H]
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| InChi Key |
NXSKOEXUDZHMAL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H21N3.ClH/c1-23(2,24)18-14-12-17(13-15-18)22-21(16-8-4-3-5-9-16)25-19-10-6-7-11-20(19)26-22/h3-15H,24H2,1-2H31H
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| Chemical Name |
2-[4-(3-Phenylquinoxalin-2-yl)phenyl]propan-2-aminehydrochloride
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| Synonyms |
Akt-I-1,2 Akt I 1,2 AktI1,2
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6603 mL | 13.3014 mL | 26.6028 mL | |
| 5 mM | 0.5321 mL | 2.6603 mL | 5.3206 mL | |
| 10 mM | 0.2660 mL | 1.3301 mL | 2.6603 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.
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.
(2) Be sure to add the solvent(s) in order.
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