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| 5mg |
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| Targets |
INY-05-040 targets AKT (protein kinase B), a serine/threonine protein kinase that plays a central role in cell survival, proliferation, and metabolism. As an AKT degrader, it induces the degradation of AKT protein rather than simply inhibiting its catalytic activity. This approach may overcome limitations of catalytic AKT inhibitors and provide more complete suppression of AKT-dependent phenotypes.
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| ln Vitro |
In vitro studies demonstrate that INY-05-040 is a second-generation AKT degrader that outperforms catalytic AKT inhibition in suppressing AKT-dependent phenotypes in breast cancer cell lines. A growth inhibition screen with 288 cancer cell lines confirmed that INY-05-040 had substantially higher potency than the first-generation AKT degrader INY-03-041. Both compounds outperformed catalytic AKT inhibition by GDC-0068. Detailed IC50 values and degradation kinetics are not extensively documented.
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| ln Vivo |
In vivo activity of INY-05-040 is inferred from its superior potency in cellular assays and its mechanism as an AKT degrader. By inducing degradation of AKT, the compound is expected to have anti-tumor activity in vivo. Detailed in vivo efficacy data from animal models, including tumor growth inhibition studies, are not extensively documented in the available literature. The compound is intended for research use only.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for INY-05-040 is not applicable in the traditional sense, as the compound is a degrader rather than a classical enzyme inhibitor. However, binding studies may be performed to assess its interaction with AKT and the E3 ubiquitin ligase complex. Cellular degradation assays measure AKT protein levels by Western blot after compound treatment. Standard protocols include appropriate positive controls such as catalytic AKT inhibitors and vehicle controls.
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| Cell Assay |
In vitro cell-based assays for INY-05-040 are conducted using breast cancer cell lines and a panel of 288 cancer cell lines. Cells are treated with the compound at various concentrations, and AKT protein levels are measured by Western blot to assess degradation. Cell viability and proliferation are assessed using growth inhibition assays. AKT-dependent phenotypes are evaluated to compare the compound's efficacy with catalytic AKT inhibitors.
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| Animal Protocol |
In vivo animal studies for INY-05-040 would typically be conducted using xenograft mouse models of breast cancer. Tumor-bearing mice would be administered the compound via appropriate routes, and tumor growth inhibition would be monitored. AKT degradation in tumor tissues would be confirmed by Western blot. Pharmacokinetic parameters would be determined from plasma samples. However, detailed protocols and efficacy data are not available from the search results.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of INY-05-040 are not extensively documented in the available literature. As a second-generation AKT degrader, it has been optimized for potency compared to first-generation compounds. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not available from the search results. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicity information for INY-05-040 is limited. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
INY-05-040 is a second-generation AKT degrader that outperforms catalytic AKT inhibition in breast cancer cell lines. It has substantially higher potency than first-generation AKT degrader INY-03-041 in a screen of 288 cancer cell lines. Both compounds outperform catalytic AKT inhibition by GDC-0068. It is intended for research use only.
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| Molecular Formula |
C55H76CLN9O6S
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|---|---|
| Molecular Weight |
1026.77
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| CAS # |
2503018-29-7
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| Appearance |
White to off-white solid powder
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| Density |
1.235±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
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| Boiling Point |
1153.8±65.0 °C(predicted)
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| LogP |
0
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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) |
DMSO :≥ 100 mg/mL (~97.39 mM)
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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 | 0.9739 mL | 4.8696 mL | 9.7393 mL | |
| 5 mM | 0.1948 mL | 0.9739 mL | 1.9479 mL | |
| 10 mM | 0.0974 mL | 0.4870 mL | 0.9739 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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