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.
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- Reinheit: 99.48%
- CAS. Nr.: 1391107-89-3
- Formel: C53H59ClF4N6O7S4
- Molecular Weight:1131.78
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Bcl-2 3.5 nM (IC50) |
Bcl-xL 5.2 nM (IC50) |
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.
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. Nr. 1391107-89-3
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Appearance Solid
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Molecular Weight 1131.78
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
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)
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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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)
Verweise
[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
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 |
|---|---|---|---|---|---|
| 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 |
BM-1197 Related Classifications
HY-120882 Related Classifications
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