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.
For research use only. We do not sell to patients.
- CAS No.: 406228-58-8
- Formula: C36H47N5O5S2
- Molecular Weight:693.92
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Bcl-xL <0.5 μM (Ki) |
Bcl-2 40 μM (Ki) |
Bcl-W 180 μM (Ki) |
Bcl-B 1300 μM (Ki) |
In Vitro
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. Further protocols information, click here.
In Vivo
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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Molecular Weight 693.92
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Formula 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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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.
Protocols
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-371191 Related Classifications
HY-122275 Related Classifications
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