| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
AKT-IN-1 has an IC50 of 0.422 and 0.322 μM, respectively, which allows it to effectively block the phosphorylation of AKT Thr308 and Ser473 sites in cells. Because ribosomal protein S6 is a downstream effector of the PI3K-AKT pathway, AKT-IN-1 prevents it from becoming phosphorylated. PRAS40 phosphorylation is efficiently inhibited by AKT-IN-1 [1].
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| ln Vivo |
Compound 26 (AKT-IN-1) in vivo effects were evaluated by assessing the compound's pharmacodynamic efficacy in the BT474c breast cancer xenograft model. AKT-IN-1 efficiently prevented the phosphorylation of AKT (Ser473) and its downstream substrate GSK3β after acute dosages of 100 and 200 mg/kg. Its effectiveness was in line with its pharmacokinetic properties. By assessing the impact on the growth of tumor cell xenografts, the in vivo activity of AKT-IN-1 was further described. AKT-IN-1 (100 and 200 mg/kg) given orally, continuously, and daily to nude mice containing BT474c mammary adenocarcinoma xenografts suppresses tumor growth in a dose-dependent manner. At a daily dosage of 200 mg/kg, AKT-IN-1 significantly inhibits the growth of tumors [1].
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| References |
| Molecular Formula |
C22H21N3O
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|---|---|
| Molecular Weight |
343.43
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| Exact Mass |
343.168
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| CAS # |
1357158-81-6
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| PubChem CID |
56953649
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
496.4±45.0 °C at 760 mmHg
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| Flash Point |
254.0±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.643
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| LogP |
2.87
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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 |
4
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| Heavy Atom Count |
26
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| Complexity |
490
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GIRZDHCBMNHMEH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21N3O/c23-21(26)17-13-19(15-5-2-1-3-6-15)20(25-14-17)16-7-9-18(10-8-16)22(24)11-4-12-22/h1-3,5-10,13-14H,4,11-12,24H2,(H2,23,26)
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| Chemical Name |
6-[4-(1-aminocyclobutyl)phenyl]-5-phenylpyridine-3-carboxamide
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| Synonyms |
AZD-26 AZD26 AZD 26
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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 : ~75 mg/mL (~218.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.28 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 25.0 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: ≥ 2.5 mg/mL (7.28 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 25.0 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: ≥ 2.5 mg/mL (7.28 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 | 2.9118 mL | 14.5590 mL | 29.1180 mL | |
| 5 mM | 0.5824 mL | 2.9118 mL | 5.8236 mL | |
| 10 mM | 0.2912 mL | 1.4559 mL | 2.9118 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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