AKT1-IN-11
AKT1-IN-11, a Podophyllotoxin (HY-15552) derivative, is a AKT1/tubulin dual inhibitor. AKT1-IN-11 down-regulates the phosphorylation level of AKT kinase in tumor cells, disrupting cell proliferation, causeing G2/M phase arrest and inducing apoptosis. AKT1-IN-11 also promotes tubulin depolymerization. AKT1-IN-11 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 3087064-94-3
- Formula: C33H32N4O11S
- Molecular Weight:692.69
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
AKT1-IN-11 (Compound 2b) (48 h) inhibits HCT-116, HT-29, HCT-8 and NCM460 cell proliferation with IC50 values of 0.77, 0.48, 1.68 and 52.28 μM[1].
AKT1-IN-11 (0.2 μM, 12-24 h) induces apoptosis in HCT-116 cells[1].
AKT1-IN-11 (0.1-0.2 μM; 24 h) inhibits cell migration and reverses the epithelial mesenchymal transition process in HCT-116 cells[1].
AKT1-IN-11 (0.1-0.2 μM; 2-8 h) induces G2/M phase arrest in HCT-116 cells, and downregulates the expression of Cyclin B1 and CDK4[1].
AKT1-IN-11 (0.1 μM; 12 h) promotes microtubule depolymerization in HCT-116 cells[1].
AKT1-IN-11 (0.1-0.2 μM, 24 h) concentration-dependently downregulates p-AKT expression in HCT-116 cells and inhibits AKT pathway activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:0.1, 0.2 μM
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Incubation Time:2, 4, 8 and 24 h
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Result:Downregulated the expression of phosphorylated AKT1 (p-AKT) in a concentration-dependent manner.
Downregulated the expression of Cyclin B1 and CDK4.
Reduced the levels of E-cadherin and increased the levels of N-cadherin.
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Cell Line:HCT-116 cells
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Concentration:0.1 μM
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Incubation Time:12 h
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Result:Disrupted microtubule structure.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (Male, BALB/c-nu/nu, 6-8 weeks) with subcutaneous injection of HCT-116 cells[1]
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Dosage:1, 2 mg/kg
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Administration:Intraperitoneally injection; once every two days; 6 doses
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Result:Reduced tumor volumes without causing a significant decrease in body weight.
Reduced the tumor weight-to-body weight ratio.
Reduced the Ki67-positive rate and increased the TUNEL-positive rate.
Chemical Information
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CAS No. 3087064-94-3
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Molecular Weight 692.69
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Formula C33H32N4O11S
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SMILES
COC1=C(OC)C(OC)=CC([C@H]2[C@]3([H])[C@@](COC3=O)([H])[C@@H](OCC4=CN(S(C5=CC=C(NC(C)=O)C=C5)(=O)=O)N=N4)C6=CC7=C(OCO7)C=C26)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AKT1-IN-11 Related Classifications
HY-179516 Related Classifications
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