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.
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- CAS No.: 3106364-91-1
- Formule: C24H25ClF4N2O4
- Masse moléculaire:516.92
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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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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Masse moléculaire 516.92
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Formule 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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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)
Bfl-1-IN-6 TFA Related Classifications
HY-170434A Related Classifications
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