| Size | Price | Stock | Qty |
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| Targets |
The primary target of AKT-IN-23 is the AKT kinase (AKT1, AKT2, AKT3). AKT is a serine/threonine protein kinase that plays a central role in cell survival, proliferation, and metabolism. AKT-IN-23 acts as an ATP-competitive inhibitor, binding to the ATP-binding pocket of AKT and preventing its activation. This inhibition reduces the phosphorylation of downstream substrates (e.g., GSK-3beta, PRAS40, FOXO), leading to decreased cell proliferation, induction of apoptosis, and suppression of tumor growth.
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| ln Vitro |
In vitro, AKT-IN-23 effectively inhibits AKT activity, leading to decreased cell proliferation and survival in various cancer cell models. It inhibits pAKT phosphorylation in cells with IC50 values in the 1 nM-500 nM range in T-47D breast cancer cells, and >15 uM in SKBR3 cells, demonstrating variable potency across cell lines. It can inhibit cell proliferation with EC50 values of 500 nM-2 uM (T-47D) and 2 uM-15 uM (SKBR3). The compound also reduces colony formation and induces apoptosis. A standard in vitro protocol for assessing AKT-IN-23 activity involves measuring pAKT levels by Western blot. Cells (e.g., T-47D) are seeded in 6-well plates and treated with AKT-IN-23 (0-10 uM) for 2-6 hours. Cell lysates are probed with antibodies against pAKT (Ser473) and total AKT. The IC50 is calculated by densitometry. For cell proliferation assays, cells are treated for 72 hours and viability measured by CellTiter-Glo. IC50 is determined from dose-response curves.
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| ln Vivo |
In vivo, AKT-IN-23 can be used in cancer research. A standard xenograft model: Female athymic nude mice are injected subcutaneously with PTEN-deficient cancer cells (e.g., PC-3 prostate or T-47D breast). When tumors reach 100-150 mm3, AKT-IN-23 is administered orally or intraperitoneally at doses of 10, 30, 100 mg/kg daily for 21-28 days. Tumor volume is measured by calipers twice weekly. Endpoints include tumor growth inhibition (TGI), pAKT levels in tumor lysates (Western blot), and survival. A vehicle control group and a positive control (e.g., capivasertib) are included.
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| ADME/Pharmacokinetics |
AKT-IN-23 is an AKT inhibitor with molecular formula C25H27F4N7O and molecular weight 517.52 g/mol. The compound has a calculated logP of 2.8. It is soluble in DMSO (up to 25 mg/mL). In vivo, it can be formulated in a mixture of DMSO, PEG300, Tween 80, and saline (e.g., 10:40:5:45). The compound should be stored as powder at -20degC for up to 3 years and in DMSO solution at -80degC for up to 6 months. The plasma half-life in rodents is estimated at 2-4 hours.
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| Toxicity/Toxicokinetics |
The toxicological profile of AKT-IN-23 has not been fully disclosed. As an AKT inhibitor, potential toxicities include metabolic disturbances (hyperglycemia, hyperinsulinemia), skin rash, gastrointestinal effects, and immunosuppression. At supra-therapeutic doses, body weight loss may occur. Standard safety precautions for research chemicals apply: use fume hood, wear nitrile gloves, lab coat, and safety goggles. Not for human consumption.
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| References | |
| Additional Infomation |
A critical component of the PI3K/AKT/mTOR signaling pathway, AKT is hyperactivated in many human cancers (e.g., breast, prostate, ovarian, glioblastoma). AKT-IN-23 (LY2780301) is a research compound that has been investigated as a potential therapeutic for AKT-driven cancers. It is not an FDA-approved drug. The compound is for research use only and not for human consumption.
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| Molecular Formula |
C25H27F4N7O
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|---|---|
| Molecular Weight |
517.52
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| Exact Mass |
517.221
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| CAS # |
1226801-23-5
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| PubChem CID |
46186926
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| Appearance |
Typically exists as solids at room temperature
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| Density |
1.45±0.1 g/cm3(Predicted)
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| Boiling Point |
723.4±60.0 °C(Predicted)
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| LogP |
0
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
793
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(=CC=1C(F)(F)F)C1=CN(CCN(C)C)C(C2CCN(C3C4=C(N=CN=3)NC(C4)=O)CC2)=N1
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| InChi Key |
YDFKZIGAUIKZGP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27F4N7O/c1-34(2)9-10-36-13-20(16-3-4-19(26)18(11-16)25(27,28)29)32-23(36)15-5-7-35(8-6-15)24-17-12-21(37)33-22(17)30-14-31-24/h3-4,11,13-15H,5-10,12H2,1-2H3,(H,30,31,33,37)
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| Chemical Name |
4-[4-[1-[2-(dimethylamino)ethyl]-4-[4-fluoro-3-(trifluoromethyl)phenyl]imidazol-2-yl]piperidin-1-yl]-5,7-dihydropyrrolo[2,3-d]pyrimidin-6-one
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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 | 1.9323 mL | 9.6615 mL | 19.3229 mL | |
| 5 mM | 0.3865 mL | 1.9323 mL | 3.8646 mL | |
| 10 mM | 0.1932 mL | 0.9661 mL | 1.9323 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.
Link: https://clinicaltrials.gov/ct2/show/NCT01980277
Conditions:Breast CancerLink: https://clinicaltrials.gov/ct2/show/NCT02018874
Conditions:Solid Tumors and Non-Hodgkin's LymphomaLink: https://clinicaltrials.gov/ct2/show/NCT01115751
Conditions:Metastases, NeoplasmProducts are for research use only; We do not sell to patients
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