Akt3 degrader 1
Based on 1 Customer Validation
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomesOsimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 95.10%
- CAS No.: 2836342-69-7
- Formula: C53H72N8O4
- Molecular Weight:885.19
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Akt3[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
0.007 μM
Compound: 12l
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Antiproliferative activity against human osimertinib resistant NCI-H1975 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay
Antiproliferative activity against human osimertinib resistant NCI-H1975 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay
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[PMID: 36173763] |
Akt3 degrader 1 (0.001-100 μM; 24 h) shows antiproliferative effects on H1975OR cells with an IC50 of 0.972 μM[1].
Akt3 degrader 1 (1.6, 8, 40, 200, 1000 nM; 24 h) induces degradation of Akt3 through the ubiquitin proteasome-mediated proteolysis process in NSCLC cell lines[1].
Akt3 degrader 1 (10, 100 nM) selectively and dose-dependently degrades exogenous PH domain-only Akt3 protein but not the Akt3 del PH mutant in H1975OR cells[1].
Akt3 degrader 1 overcomes osimertinib-induced resistance in H1975OR NSCLC cells via disrupting the noncatalytic functions of Akt3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975OR cells
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Concentration:0.001-100 µM
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Incubation Time:24 h
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Result:Inhibited growth of H1975OR cells with an IC50 of 0.972 µM.
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Cell Line:A549, HCC827, H1975, H1975OR, PC9, H1299, and H460 cells
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Concentration:1.6, 8, 40, 200, 1000 nM
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Incubation Time:24 h
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Result: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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID-IL2Rg-/-(NSI) mice (H1975OR xenograft model)[1].
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Dosage:10, 20 mg/kg
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Administration:Intraperitoneal administration; every 3 days for 5 weeks
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Result:Inhibited tumor growth without causing obvious body weight loss or other signs of toxicity.
Chemical Information
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CAS No. 2836342-69-7
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Appearance Solid
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Molecular Weight 885.19
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Formula C53H72N8O4
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Color Light yellow to yellow
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SMILES
COC1=C(C=CC(N2CCN(CC2)CCCCCCCCCCCCNC(CC34CC5CC(C4)CC(C3)C5)=O)=C1)NC6=NC=C7C(C)=CC(N(C7=N6)C8=CC=CC(NC(C9CC9)=O)=C8)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Akt3 degrader 1 Related Classifications
HY-151606 Related Classifications
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