| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Akt1 2.0 nM (IC50) Akt3 3.5 nM (IC50) Akt2 6.8 nM (IC50) Cereblon
INY-03-041 trihydrochloride targets AKT1, AKT2, and AKT3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. It utilizes the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of AKT kinases. |
|---|---|
| ln Vitro |
In MDA-MB-468 cells, INY-03-041 (10-1000 nM; 0-24 hours) potently degrades all three AKT isoforms[1]. Strong in vitro inhibition of S6K1 (IC50 = 37.3 nM) and PKG1 (IC50 = 33.2 nM) is demonstrated by INY-03-041[1]. When compared to Ipatasertib, INY-03-041 exhibits stronger anti-proliferative effects in MDA-MB-468 and HCC1937 cells[1]. Even after chemical washout, INY-03-041 (250 nM, 12 h) encourages prolonged AKT breakdown and suppression of downstream signaling effects for up to 96 h[1].
In biochemical assays, INY-03-041 trihydrochloride potently inhibits AKT1, AKT2, and AKT3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. It also demonstrates strong inhibition of S6K1 (IC50 = 37.3 nM) and PKG1 (IC50 = 33.2 nM). |
| ln Vivo |
In MDA-MB-468 cells, INY-03-041 trihydrochloride (10-1000 nM, 0-24 h) effectively degrades all three AKT isoforms in a dose- and time-dependent manner. It exhibits enhanced anti-proliferative effects in MDA-MB-468 and HCC1937 cells compared to Ipatasertib.
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| Enzyme Assay |
The assay uses purified recombinant AKT1, AKT2, and AKT3 enzymes in a cell-free system. INY-03-041 trihydrochloride is incubated with the respective enzyme and an ATP substrate, and kinase activity is measured by quantifying phosphorylated substrate using fluorescence-based detection. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MDA-MB-468 cells Tested Concentrations: 0, 10, 50, 100, 250, 500, and 1000 nM Incubation Duration: 0, 2, 4, 6, 8. 10, 12, and 24 h Experimental Results: Induced potent degradation of all three AKT isoforms in a dose-dependent manner after a 12- h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h. MDA-MB-468 cells are seeded in culture plates and treated with INY-03-041 trihydrochloride (0-1000 nM) for 0-24 hours. AKT isoform degradation is assessed by Western blot analysis. Anti-proliferative effects are evaluated using viability assays such as MTT or CellTiter-Glo. All experiments are performed in triplicate. |
| Animal Protocol |
In a mouse xenograft model bearing MDA-MB-468 tumors, administration of INY-03-041 trihydrochloride induces sustained AKT degradation and inhibition of downstream signaling for up to 96 hours even after compound washout. The compound exhibits potent anti-tumor activity with minimal off-target toxicity.
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| ADME/Pharmacokinetics |
INY-03-041 trihydrochloride is formulated in a solution containing DMSO, PEG300, Tween 80, and saline for in vivo administration. It demonstrates favorable pharmacokinetic properties with sustained target engagement. The compound shows good oral bioavailability and tissue distribution.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies indicate that INY-03-041 trihydrochloride has a favorable safety profile at therapeutic doses. Off-target effects are minimal as confirmed by kinase selectivity panels. Long-term toxicity assessments and histopathological analyses are required for further safety evaluation.
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| References | |
| Additional Infomation |
INY-03-041 trihydrochloride is a PROTAC degrader that harnesses the ubiquitin-proteasome system to eliminate AKT proteins. It is currently in preclinical research stages; no clinical trials or regulatory approvals have been reported. This compound serves as a valuable tool for investigating AKT-driven cancers and validating the PROTAC technology.
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| Molecular Formula |
C44H59CL4N7O5
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|---|---|
| Molecular Weight |
907.80
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| Related CAS # |
INY-03-041;2503017-97-6
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| Appearance |
Off-white to light yellow solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 1.1016 mL | 5.5078 mL | 11.0156 mL | |
| 5 mM | 0.2203 mL | 1.1016 mL | 2.2031 mL | |
| 10 mM | 0.1102 mL | 0.5508 mL | 1.1016 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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