Mcl-1-IN-16
Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- Formula: C42H43Cl2N5O7
- Molecular Weight:800.73
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Mcl-1 < 0.08 nM (Ki) |
Caspase-3 8.8 nM (EC50) |
Caspase-7 11 nM (EC50) |
Mcl-1-IN-16 (Compound 13) inhibits cell proliferation with an GI50 value of 14 and 25 nM against H929 and A427 cells, and does not show inhibitory effect on K562 cells[1].
Mcl-1-IN-16 (4 h) activates Caspase 3/7 in H929 and A427 cells of EC50s of 8.8 and 11 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A427 cell line-derived NSCLC xenograft model established in Balb/c nude, female mice[1]
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Dosage:30 and 60 mg/kg
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Administration:Intravenous injection (i.v.), once every 14 days for 28 days
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Result:Achieved complete tumor regression at 60 mg/kg, with the therapeutic effect lasting for 50 days after administration. No weight loss or clinical signs of toxicity.
Chemical Information
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Molecular Weight 800.73
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Formula C42H43Cl2N5O7
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SMILES
CC1=C(Cl)C(C)=CC(OCCCC2=C(C(N(C3=CC(OC)=C(OC)C4=C3N(CCCOC5)C(C(O)=O)=C4)C[C@H]6C)=O)N6C7=C2C=CC(Cl)=C7C(C5=N8)=CN8C)=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)
Mcl-1-IN-16 Related Classifications
HY-178008 Related Classifications
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