Bfl-1-IN-5
Based on 1 Customer Validation
Bfl-1-IN-5 is a covalent and selective Bfl-1 inhibitor with an IC50 of 22 nM. Bfl-1-IN-5 shows selectivity for Bfl-1 over Bcl-xl, Bcl-2 and Mcl-1. Bfl-1-IN-5 induces caspase-3/7 activation, reduces the viability of Bfl-1-expressing lymphoma cells in combination with an Mcl-1 inhibitor, and binds covalently to intracellular Bfl-1. Bfl-1-IN-5 can be used for lymphoma research.
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- Pureté : 99.24%
- CAS No.: 3097167-82-0
- Formule: C24H24F3N3O2
- Masse moléculaire:443.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Bfl-1 22 nM (IC50) |
Caspase-3 |
Caspase-7 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| KARPAS-422 | EC50 |
>10 μM
Compound: R,R,S-26
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Cytotoxicity against human KARPAS-422 cells assessed as cell viability incubated for 24 hrs by Cell Titer Glo assay
Cytotoxicity against human KARPAS-422 cells assessed as cell viability incubated for 24 hrs by Cell Titer Glo assay
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[PMID: 39291659] |
In Vitro
Bfl-1-IN-5 ((R,R,S)-26) (100 μM; 120 min) inhibits Bfl-1-Bim interaction in a biochemical TR-FRET assay with an IC50 of 0.022 μM[1].
Bfl-1-IN-5 is selective for Bfl-1 over Bcl-xl, Bcl-2, and Mcl-1 with IC50 values greater than 30, 30, and 100 μM, respectively[1].
Bfl-1-IN-5 (10 μM; 5 h) engages endogenous Bfl-1 covalently in SU-DHL-1 cells, demonstrating cellular target engagement[1].
Bfl-1-IN-5 shows low intrinsic clearance in human liver microsomes and human hepatocytes, with substantially higher clearance in mouse hepatocytes[1].
Bfl-1-IN-5 (0.3 nM-10 μM; 6 h) activates caspase-3/7 in SU-DHL-1 cells with an EC50 of 0.37 μM when combined with Mcl-1 inhibitor AZD-5991 (HY-101533)[1].
Bfl-1-IN-5 (0.3 nM-10 μM; 24 h) reduces viability of SU-DHL-1 cells with an EC50 of 1.3 μM when combined with AZD-5991[1].
Bfl-1-IN-5 (0.3 nM-10 μM; 24 h) does not reduce viability of Bfl-1-null Karpas-422 cells at concentrations up to 10 μM, consistent with Bfl-1-dependent activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:SU-DHL-1 lymphoma cells
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Concentration:0.3 nM to 10 μM
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Incubation Time:24 h
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Result:Reduced SU-DHL-1 cell viability with an EC50 of 1.3 μM in combination with Mcl-1 inhibitor
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Cell Line:Karpas-422 cells
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Concentration:0.3 nM to 10 μM
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Incubation Time:24 h
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Result:Showed no loss of cell viability in Bfl-1-null Karpas-422 cells at concentrations up to 10 μM (EC50 > 10 μM).
Chemical Information
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CAS No. 3097167-82-0
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Appearance Solid
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Masse moléculaire 443.46
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Formule C24H24F3N3O2
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Color White to off-white
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SMILES
C=CC(N(C1=CC=C(O[C@H]2C[C@H](N)CC2)C=C1)[C@H](C3=CC=C(C(F)(F)F)C(C#N)=C3)C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (225.50 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. 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. 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 (5.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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 (5.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
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Fiche technique (294 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
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. 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 | 2.2550 mL | 11.2750 mL | 22.5499 mL | 56.3749 mL |
| 5 mM | 0.4510 mL | 2.2550 mL | 4.5100 mL | 11.2750 mL | |
| 10 mM | 0.2255 mL | 1.1275 mL | 2.2550 mL | 5.6375 mL | |
| 15 mM | 0.1503 mL | 0.7517 mL | 1.5033 mL | 3.7583 mL | |
| 20 mM | 0.1127 mL | 0.5637 mL | 1.1275 mL | 2.8187 mL | |
| 25 mM | 0.0902 mL | 0.4510 mL | 0.9020 mL | 2.2550 mL | |
| 30 mM | 0.0752 mL | 0.3758 mL | 0.7517 mL | 1.8792 mL | |
| 40 mM | 0.0564 mL | 0.2819 mL | 0.5637 mL | 1.4094 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4510 mL | 1.1275 mL | |
| 60 mM | 0.0376 mL | 0.1879 mL | 0.3758 mL | 0.9396 mL | |
| 80 mM | 0.0282 mL | 0.1409 mL | 0.2819 mL | 0.7047 mL | |
| 100 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5637 mL |
Bfl-1-IN-5 Related Classifications
HY-169172 Related Classifications
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