BM-1197
Based on 1 Customer Validation
BM-1197 (UBX1967) is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo.
For research use only. We do not sell to patients.
- Purity : 99.85%
- CAS No.: 1391107-89-3
- Formula: C53H59ClF4N6O7S4
- Molecular Weight:1131.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Bcl-2 3.5 nM (IC50) |
Bcl-xL 5.2 nM (IC50) |
In Vitro
BM-1197 (2-2000 nM; 3 d) has marginal cytotoxicity against wild-type mouse embryonic fibroblast (MEF) cells but exerts potent growth-inhibitory activity in the MCL1 / cells[1].
BM-1197 shows potent growth-inhibitory activities in 7 small cell lung cancer (SCLC) cell lines with IC50s <100 nM, moderate activity in 3 SCLC cell lines with IC50s of ~600 nM and weak activity in 2 SCLC cell lines with IC50s >2000 nM[1].
BM-1197 (100 nM; 16 h) potently induces apoptosis in H146 cells[1].
BM-1197 (100 nM; 2 h) disrupts the association between Bcl-xl and Puma or Bim in H146 cells[1].
BM-1197 (100 nM; 0.5-2 h) induces Bax translocation, and it (3-30 nM; 2 h) induces cytochrome c release in H146 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MEF/MCL1−/− cells
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Concentration:2, 20, 200, 2000 nM
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Incubation Time:3 days
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Result:Inhibited MCL1−/− cells proliferation.
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Cell Line:H146 cells
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Concentration:100 nM
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Incubation Time:16 hours
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Result:Induced apoptosis in a strictly Bax/Bak-dependent manner.
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Cell Line:H146 cells
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Concentration:100 nM
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Incubation Time:2 hours
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Result:Attenuated the associations between Bcl-xL and BimEL or Puma.
In Vivo
BM-1197 (15 mg/kg; i.v.) causes thrombocytopenia in mice but the effect is reversible even at highly efficacious doses[1].
BM-1197 (10 mg/kg; i.v. qd) exerts a strong anti-tumor effect and is well tolerated in OCI-Ly8 xenograft models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice bearing H146 cells[1]
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Dosage:10 mg/kg
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Administration:I.v. daily 5 days per week for 2 weeks
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Result:Remained tumor free for at least 32 days after the end of the treatment.
Chemical Information
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CAS No. 1391107-89-3
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Appearance Solid
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Molecular Weight 1131.78
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Formula C53H59ClF4N6O7S4
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Color White to light yellow
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SMILES
C[S](=O)(C(C(C1=CC(N2CCN(C(C=C3)=CC=C3N[S](=O)(C(C=C4)=CC([S](C(F)(F)F)(=O)=O)=C4N[C@@H](CSC5=CC=CC=C5)CCN(CC6)CCC6O)=O)CC2)=CC(F)=C1)=C(C(C=C7)=CC=C7Cl)N8C(C)C)=C8C)=O
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Synonyms
UBX1967
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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.
Solvent & Solubility
In Vitro:
DMSO : 250 mg/mL (220.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 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
[1]. Bai L, et, al. BM-1197: a novel and specific Bcl-2/Bcl-xL inhibitor inducing complete and long-lasting tumor regression in vivo. PLoS One. 2014 Jun 5; 9(6): e99404. [Content Brief]
[2]. Sun YL, et, al. A novel Bcl-2 inhibitor, BM-1197, induces apoptosis in malignant lymphoma cells through the endogenous apoptotic pathway. BMC Cancer. 2019 Dec 31; 20(1):1. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.8836 mL | 4.4178 mL | 8.8356 mL | 22.0891 mL |
| 5 mM | 0.1767 mL | 0.8836 mL | 1.7671 mL | 4.4178 mL | |
| 10 mM | 0.0884 mL | 0.4418 mL | 0.8836 mL | 2.2089 mL | |
| 15 mM | 0.0589 mL | 0.2945 mL | 0.5890 mL | 1.4726 mL | |
| 20 mM | 0.0442 mL | 0.2209 mL | 0.4418 mL | 1.1045 mL | |
| 25 mM | 0.0353 mL | 0.1767 mL | 0.3534 mL | 0.8836 mL | |
| 30 mM | 0.0295 mL | 0.1473 mL | 0.2945 mL | 0.7363 mL | |
| 40 mM | 0.0221 mL | 0.1104 mL | 0.2209 mL | 0.5522 mL | |
| 50 mM | 0.0177 mL | 0.0884 mL | 0.1767 mL | 0.4418 mL | |
| 60 mM | 0.0147 mL | 0.0736 mL | 0.1473 mL | 0.3682 mL | |
| 80 mM | 0.0110 mL | 0.0552 mL | 0.1104 mL | 0.2761 mL | |
| 100 mM | 0.0088 mL | 0.0442 mL | 0.0884 mL | 0.2209 mL |