Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
Akt3[1].
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ln Vitro |
With an IC50 of 0.972 µM, Akt3 degrader 1 (0.001-100 µM; 24 h) exhibits antiproliferative effects in H1975OR cells[1]. In NSCLC cell lines, Akt3 degrader 1 (1.6, 8, 40, 200, and 1000 nM; 24 h) causes Akt3 degradation via the ubiquitin proteasome-mediated proteolysis process[1]. In H1975OR cells, Akt3 degrader 1 (10, 100 nM) preferentially and dose-dependently degrades exogenous Akt3 protein that only contains the PH domain, but not the Akt3 del PH mutant[1]. By interfering with Akt3's noncatalytic activities, Akt3 degrader 1 prevents H1975OR NSCLC cells from developing osimertinib-induced resistance[1].
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ln Vivo |
In mice, Akt3 degrader 1 (10, 20 mg/kg; ip; every 3 days for 5 weeks) significantly inhibits tumor growth (TGI), with a TGI value of almost 75%[1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: H1975OR cells Tested Tested Concentrations: 0.001-100 µM Incubation Duration: 24 h Experimental Results: Inhibited growth of H1975OR cells with an IC50 of 0.972 µM. Western Blot Analysis[1] Cell Types: A549, HCC827, H1975, H1975OR, PC9, H1299, and H460 cells Tested Tested Concentrations: 1.6, 8, 40, 200, 1000 nM Incubation Duration: 24 h Experimental Results: Selectively induced Akt3 degradation in all of these cell lines in a dose-dependent manner, whereas had minimal influence on Akt1 and Akt2 protein levels. |
Animal Protocol |
Animal/Disease Models: NOD-SCID-IL2Rg -/-(NSI) mice (H1975OR xenograft model)[1].
Doses: 10, 20 mg/kg Route of Administration: intraperitoneal (ip) administration; every 3 days for 5 weeks Experimental Results: Inhibited tumor growth without causing obvious body weight loss or other signs of toxicity. |
References |
[1]. Xu F, et al. Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells. J Med Chem. 2022 Oct 27;65(20):14032-14048.
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Molecular Formula |
C53H72N8O4
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Molecular Weight |
885.19
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CAS # |
2836342-69-7
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.1297 mL | 5.6485 mL | 11.2970 mL | |
5 mM | 0.2259 mL | 1.1297 mL | 2.2594 mL | |
10 mM | 0.1130 mL | 0.5649 mL | 1.1297 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.