BCL-XL-IN-5
BCL-XL-IN-5 is an orally active, highly selective BH3-mimetic BCL-XL inhibitor with a cKi of 7.96 pM. BCL-XL-IN-5 triggers caspase-3 activation and robust PARP cleavage to initiate apoptosis in BCL-XL-dependent MOLT-4 T-cell acute lymphoblastic leukemia cells. BCL-XL-IN-5 serves as a potent selective probe for investigating BCL-XL-dependent malignancies, such as acute lymphoblastic leukemia.
For research use only. We do not sell to patients.
- CAS No.: 2599098-78-7
- Formula: C36H38N8O2S
- Molecular Weight:646.80
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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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Bcl-xL 7.96 pM (Ki) |
BCL-XL-IN-5 (Compound 29) (48 h) inhibits MOLT-4 growth with an IC50 of 4.85 nM, and displays high selectivity for BCL-XL versus BCL-W, BCL-2 and MCL-1[1].
BCL-XL-IN-5 (48 h) inhibits MOLT-4 growth with an IC50 of 4.85 nM and shows no activity against RS4;11 cells (>1000 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT4 cells
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Concentration:0.3 nM; 1 nM; 3 nM; 10 nM
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Incubation Time:4 h
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Result:Activated Caspase-3 in a concentration-dependent manner.
Exhibited caspase-activating effects that were completely abolished by the broad-spectrum caspase inhibitor Q-VD-OPh (Q-VD) (HY-12305).
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Cell Line:MOLT4 cells
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Concentration:0.3 nM; 1 nM; 3 nM; 10 nM
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Incubation Time:4 h
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Result:Reduced PARP protein levels in a concentration-dependent manner.
Elicited PARP protein reduction that was fully rescued upon treatment with the broad-spectrum caspase inhibitor Q-VD.
BCL-XL-IN-5 (7.5 mg/kg; p.o.; single dose) provokes prominent upregulation of apoptotic biomarkers in MOLT-4 xenograft tumor-bearing mice[1].
BCL-XL-IN-5 (2.5-7.5 mg/kg; i.v.; twice weekly; for 3 weeks) effectively inhibits tumor growth and exhibits a good safety profile in MOLT-4 xenograft tumor-bearing mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD SCID mice bearing MOLT-4 tumor xenografts[1]
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Dosage:7.5 mg/kg
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Administration:i.v., single dose
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Result:Elevated cleaved PARP levels by 38.6-fold relative to untreated controls.
Raised cleaved caspase 3 levels by 18.9-fold relative to untreated controls.
Caused a significant decrease in platelet count.
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Animal Model:Female NOD SCID mice bearing MOLT-4 tumor xenografts[1]
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Dosage:7.5 mg/kg
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Administration:p.o., single dose
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Result:Elevated cleaved PARP levels by 24.1-fold relative to untreated controls.
Raised cleaved caspase 3 levels by 7.2-fold relative to untreated controls.
Induced a marked reduction in platelet counts.
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Animal Model:Female NOD SCID mice bearing MOLT-4 tumor xenografts[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 7.5 mg/kg
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Administration:i.v., twice weekly, for 3 weeks
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Result:Significantly reduced tumor volume in mice.
Yielded day 17 TGI values of 122%, 124% and 133% at 2.5, 5, 7.5 mg/kg, and outperformed A-1331852 (HY-19741) at 7.5 mg/kg (133% vs 115% TGI).
Did not affect the body weight of the mice.
Chemical Information
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CAS No. 2599098-78-7
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Molecular Weight 646.80
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Formula C36H38N8O2S
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SMILES
O=C(O)C1=NC(N2CCCC3=C(C)C(NC4=NC5=CC=CC=C5S4)=NN=C32)=CC=C1C6=C(C)N(CC78CC9CC(C8)CC(C9)C7)N=C6
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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)
BCL-XL-IN-5 Related Classifications
HY-184471 Related Classifications
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