A-371191
A-371191 is a selective Bcl-XL antagonist with a Ki <0.5 μM, and also acts as a mitochondria-targeting agent and chemosensitizer. A-371191 restores the sensitivity of cancer cells overexpressing Bcl-XL to Cisplatin (HY-17394) and Doxorubicin (HY-15142A). A-371191 reduces tumor volume in mice with intraperitoneal tumors. A-371191 can be used in the research of acute myeloid leukemia.
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- CAS No.: 406228-58-8
- Formule: C36H47N5O5S2
- Masse moléculaire:693.92
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Stockage:
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
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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Bcl-xL <0.5 μM (Ki) |
Bcl-2 40 μM (Ki) |
Bcl-W 180 μM (Ki) |
Bcl-B 1300 μM (Ki) |
A-371191 binds selectively to Bcl-XL with a Ki value of <0.5 μM, and exhibits significantly lower affinity for other anti-apoptotic Bcl-2 family proteins[1].
A-371191 accumulates and localizes to mitochondria in NIH-H460 cells[1].
Combined treatment with A-371191 (1.8-3.2 μM) restores the sensitivity of HL-60/Bcl-XL cells to Cisplatin (HY-17394) and Doxorubicin (HY-15142A), which is consistent with the response of HL-60/neo control cells[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:SCID mice[1]
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Dosage:75 mg/kg; 150 mg/kg
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Administration:i.p.; twice daily; 7 days
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Result:Reduced average tumor volume to 2667 mm3 at 75 mg/kg.
Reduced average tumor volume to 1742 mm3 at 150 mg/kg (control average was 2435 mm3).
Caused approximately 1% body weight gain over treatment period.
Chemical Information
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CAS No. 406228-58-8
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Masse moléculaire 693.92
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Formule C36H47N5O5S2
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SMILES
O=C(NS(=O)(C1=CC=C(N[C@H](CCCCN(C)C)CSC2=CC=CC=C2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N(CC4)CCC54CCCC5)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-371191 Related Classifications
HY-122275 Related Classifications
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