| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Akt1 Akt2 Akt3
AKT1, AKT2, and AKT3 (protein kinase B family). AKT-IN-6 is a potent inhibitor of all three AKT isoforms, with IC50 values of less than 500 nM for each isoform. |
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| ln Vitro |
In cell signaling, Akt functions as a key node after growth factors, cytokines, and other cellular stimuli. Type-2 diabetes and cancer are two examples of complicated disorders whose pathophysiological characteristics are caused by aberrant loss or gain of Akt activation[2].
AKT-IN-6 is a potent inhibitor of AKT1, AKT2, and AKT3 with IC50 values of less than 500 nM for each isoform. As a potent AKT inhibitor, it blocks the phosphorylation and activation of AKT, thereby inhibiting downstream signaling pathways. The compound's ability to inhibit all three AKT isoforms makes it a valuable tool for studying the role of AKT signaling in various cellular processes, including cell survival, proliferation, and metabolism. |
| ln Vivo |
No detailed in vivo activity data are publicly available for AKT-IN-6. As a potent AKT inhibitor, its in vivo effects would be expected to be related to the inhibition of AKT signaling, which could lead to reduced tumor growth, increased apoptosis, and improved responses to other therapies.
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| Enzyme Assay |
In vitro enzyme assays for AKT-IN-6 are performed to evaluate its inhibitory activity against AKT1, AKT2, and AKT3. The kinases are incubated with peptide substrates and ATP in the presence of varying concentrations of AKT-IN-6. The inhibition of kinase activity is measured by assessing the phosphorylation of the substrate, and IC50 values are calculated from the concentration-response curves.
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| Cell Assay |
In vitro cell-based assays are conducted to evaluate the effects of AKT-IN-6 on AKT signaling and cell viability. Cells are treated with AKT-IN-6, and AKT phosphorylation and the phosphorylation of downstream targets such as GSK3β, PRAS40, and FOXO are measured by Western blotting. Cell viability and proliferation are assessed using standard assays such as MTT or CCK-8. The compound's ability to induce apoptosis is evaluated by measuring caspase activity or by flow cytometry.
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| Animal Protocol |
No detailed in vivo animal study protocols are publicly available for AKT-IN-6. In vivo studies would be conducted in animal models, such as tumor xenograft models, to evaluate the antitumor efficacy of AKT-IN-6. The compound could be administered via oral or intraperitoneal routes, and its effects on tumor growth, survival, and biomarkers of AKT signaling would be assessed.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for AKT-IN-6. As a small molecule inhibitor, its ADME properties would be characterized in standard preclinical studies. The compound is soluble in DMSO at 125 mg/mL.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for AKT-IN-6. As a potent AKT inhibitor, its toxicity profile would be expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
AKT-IN-6 (Example 13, INCB-047775) is a potent inhibitor of AKT1, AKT2, and AKT3 with IC50 values of less than 500 nM. It is a valuable research tool for studying the role of AKT signaling in cancer and other diseases. The compound is not approved for human therapeutic use and is strictly for research purposes. It is described in patent WO2013056015A1.
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| Molecular Formula |
C22H20FN5O
|
|---|---|
| Molecular Weight |
389.43
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| Exact Mass |
389.165
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| CAS # |
1430056-54-4
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| PubChem CID |
89499684
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| Appearance |
Yellow to brown solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
662.5±55.0 °C at 760 mmHg
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| Flash Point |
354.5±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.671
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| LogP |
1.38
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
650
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1C(=C(C=N1)C#N)C2=CC3=C(C=C2)C(=O)N(C3)[C@@H](CC4=CC(=CC=C4)F)CN
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| InChi Key |
QXRHOURHCGFDIM-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C22H20FN5O/c1-27-21(17(10-24)12-26-27)15-5-6-20-16(9-15)13-28(22(20)29)19(11-25)8-14-3-2-4-18(23)7-14/h2-7,9,12,19H,8,11,13,25H2,1H3/t19-/m0/s1
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| Chemical Name |
5-[2-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-1-oxo-3H-isoindol-5-yl]-1-methylpyrazole-4-carbonitrile
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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) |
DMSO: 125 mg/mL (320.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5679 mL | 12.8393 mL | 25.6786 mL | |
| 5 mM | 0.5136 mL | 2.5679 mL | 5.1357 mL | |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5679 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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