Bfl-1-IN-6 TFA
Based on 1 Customer Validation
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.
- Purity: 99.42%
- CAS No.: 3106364-91-1
- Formula: C24H25ClF4N2O4
- Molecular Weight:516.92
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Caspase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Bfl-1 19 nM (IC50) |
Caspase 3 |
In Vitro
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.
Parmacokinetics
In Vivo
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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Appearance Solid
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Molecular Weight 516.92
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Formula C24H25ClF4N2O4
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Color White to off-white
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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
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (193.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.84 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.84 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9345 mL | 9.6727 mL | 19.3454 mL | 48.3634 mL |
| 5 mM | 0.3869 mL | 1.9345 mL | 3.8691 mL | 9.6727 mL | |
| 10 mM | 0.1935 mL | 0.9673 mL | 1.9345 mL | 4.8363 mL | |
| 15 mM | 0.1290 mL | 0.6448 mL | 1.2897 mL | 3.2242 mL | |
| 20 mM | 0.0967 mL | 0.4836 mL | 0.9673 mL | 2.4182 mL | |
| 25 mM | 0.0774 mL | 0.3869 mL | 0.7738 mL | 1.9345 mL | |
| 30 mM | 0.0645 mL | 0.3224 mL | 0.6448 mL | 1.6121 mL | |
| 40 mM | 0.0484 mL | 0.2418 mL | 0.4836 mL | 1.2091 mL | |
| 50 mM | 0.0387 mL | 0.1935 mL | 0.3869 mL | 0.9673 mL | |
| 60 mM | 0.0322 mL | 0.1612 mL | 0.3224 mL | 0.8061 mL | |
| 80 mM | 0.0242 mL | 0.1209 mL | 0.2418 mL | 0.6045 mL | |
| 100 mM | 0.0193 mL | 0.0967 mL | 0.1935 mL | 0.4836 mL |
Bfl-1-IN-6 TFA Related Classifications
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