BM-1074 |
Catalog No.GC13498
One-Click Copy Product Info
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1391108-10-3
Sample solution is provided at 25 µL, 10mM.
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BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM [1].
BM-1074 is a selective Bcl-2 and Bcl-xL inhibitor. It shows high binding affinity to both Bcl-2 and Bcl-xL. In H146 cell line, BM-1074 inhibits the cell growth with IC50 value of 1.3nM. It is found that 15 mg/kg dosed intravenously is the maximum tolerated dose (MTD) of BM-1074. BM-1074 at MTD induces cleavage of PARP and caspase-3 in H146 xenograft tumors in SCID mice, indicating a strong apoptosis induction in vivo. BM-1074 also shows rapid, complete and persistent antitumor efficacy in the H-146 xenograft model. Moreover, mice treated with BM-1074 shows no significant weight loss or other toxicity signs. In addition, BM-1074 inhibits cell growth in three other small-cell lung cancer cell lines, including H1963, H187 and H1417, with IC50 values of 1nM, 1.4nM and 2.3nM, respectively [1].
References:
[1] Aguilar A, Zhou H, Chen J, Liu L, Bai L, McEachern D, Yang CY, Meagher J, Stuckey J, Wang S. A potent and highly efficacious Bcl-2/Bcl-xL inhibitor. J Med Chem. 2013 Apr 11;56(7):3048-67.
| Cas No. | 1391108-10-3 | SDF | |
| Chemical Name | (R,Z)-5-(4-chlorophenyl)-4-(3-(4-(4-(4-((4-(dimethylamino)-1-(phenylthio)butan-2-yl)amino)-3-nitrophenylsulfonamido)phenyl)piperazin-1-yl)phenyl)-1-isopropyl-2-methyl-N-(methylsulfonyl)-1H-pyrrole-3-carbimidic acid | ||
| Canonical SMILES | CC(N1C(C)=C(/C(O)=N/S(C)(=O)=O)C(C2=CC(N3CCN(C4=CC=C(NS(C5=CC(N(=O)=O)=C(N[C@](CSC6=CC=CC=C6)([H])CCN(C)C)C=C5)(=O)=O)C=C4)CC3)=CC=C2)=C1C7=CC=C(Cl)C=C7)C | ||
| Formula | C50H57ClN8O7S3 | M.Wt | 1013.68 |
| Solubility | DMSO mg/mL Water mg/mL Ethanol mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 986.5 μL | 4.9325 mL | 9.865 mL |
| 5 mM | 197.3 μL | 986.5 μL | 1.973 mL |
| 10 mM | 98.7 μL | 493.3 μL | 986.5 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)