Bfl-1-IN-6 TFA
Bfl-1-IN-6 TFA is an orally active BFL1 inhibitor with an IC50 of 19 nM. Bfl-1-IN-6 TFA selectively binds covalently to BFL1, stabilizes the protein and displaces BIM from BFL1, thereby inducing apoptosis activity. Bfl-1-IN-6 TFA stabilizes BFL1 protein, activates cleaved caspase 3, and exhibits antitumor activity in mouse models. Bfl-1-IN-6 TFA can be used for the research of hematological malignancies.
For research use only. We do not sell to patients.
- CAS No.: 3106364-91-1
- Formula: C24H25ClF4N2O4
- Molecular Weight:516.92
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Bfl-1 19 nM (IC50) |
Caspase 3 |
Bfl-1-IN-6 (Compound 20) TFA induces caspase activation in SUDHL1 cells treated with 0.5 μM AZD5991 (HY-101533) with an EC50 of 350 nM, thereby resulting in decreased cell viability[1].
Bfl-1-IN-6 TFA combined with 0.5 μM AZD5991 reduces the viability of SUDHL1 cells, with an EC50 of 250 nM, and causes no significant off-target toxicity in BFL1-deficient Karpas-422 cells[1].
Bfl-1-IN-6 (0.3-9 μM; 6 h) TFA induces dose-dependent BFL1 stabilization and activation of cleaved caspase-3 in OCILY10 cells, and exhibits targeted apoptotic activity after 6 hours of treatment[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:CD-1 (male)[1]
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Dosage:100 mg/kg; 300 mg/kg
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Administration:p.o.; single dose
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Result:Increased BFL1 levels to ~180% of vehicle control levels.
Increased cleaved caspase 3 levels to ~150% of vehicle control levels.
Increased BFL1 levels to ~200% of vehicle control levels.
Increased cleaved caspase 3 levels to ~200% of vehicle control levels.
Chemical Information
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CAS No. 3106364-91-1
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Molecular Weight 516.92
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Formula C24H25ClF4N2O4
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SMILES
C(C(O)=O)(F)(F)F.N([C@@H](C)C1=CC=C(Cl)C=C1)(C(C=C)=O)C2=CC(F)=C(O[C@@H]3CC[C@@H](N)C3)C=C2
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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)
Bfl-1-IN-6 TFA Related Classifications
HY-170434A Related Classifications
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