BM-1074Bcl-2/Bcl-xL inhibitor,potent and selective CAS# 1391108-10-3 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1391108-10-3 | SDF | Download SDF |
| PubChem ID | 56933431 | Appearance | Powder |
| Formula | C50H57ClN8O7S3 | M.Wt | 1013.68 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO mg/mL Water mg/mL Ethanol mg/mL | ||
| Chemical Name | 5-(4-chlorophenyl)-4-[3-[4-[4-[[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylamino]phenyl]piperazin-1-yl]phenyl]-2-methyl-N-methylsulfonyl-1-propan-2-ylpyrrole-3-carboxamide | ||
| SMILES | CC1=C(C(=C(N1C(C)C)C2=CC=C(C=C2)Cl)C3=CC(=CC=C3)N4CCN(CC4)C5=CC=C(C=C5)NS(=O)(=O)C6=CC(=C(C=C6)NC(CCN(C)C)CSC7=CC=CC=C7)[N+](=O)[O-])C(=O)NS(=O)(=O)C | ||
| Standard InChIKey | GISBATIMZJHKJK-RRHRGVEJSA-N | ||
| Standard InChI | InChI=1S/C50H57ClN8O7S3/c1-34(2)58-35(3)47(50(60)54-68(6,63)64)48(49(58)36-15-17-38(51)18-16-36)37-11-10-12-42(31-37)57-29-27-56(28-30-57)41-21-19-39(20-22-41)53-69(65,66)44-23-24-45(46(32-44)59(61)62)52-40(25-26-55(4)5)33-67-43-13-8-7-9-14-43/h7-24,31-32,34,40,52-53H,25-30,33H2,1-6H3,(H,54,60)/t40-/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
BM-1074 Dilution Calculator
BM-1074 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 0.9865 mL | 4.9325 mL | 9.865 mL | 19.7301 mL | 24.6626 mL |
| 5 mM | 0.1973 mL | 0.9865 mL | 1.973 mL | 3.946 mL | 4.9325 mL |
| 10 mM | 0.0987 mL | 0.4933 mL | 0.9865 mL | 1.973 mL | 2.4663 mL |
| 50 mM | 0.0197 mL | 0.0987 mL | 0.1973 mL | 0.3946 mL | 0.4933 mL |
| 100 mM | 0.0099 mL | 0.0493 mL | 0.0987 mL | 0.1973 mL | 0.2466 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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A potent and highly efficacious Bcl-2/Bcl-xL inhibitor.[Pubmed:23448298]
J Med Chem. 2013 Apr 11;56(7):3048-3067.
Our previously reported Bcl-2/Bcl-xL inhibitor, 4, effectively inhibited tumor growth but failed to achieve complete regression in vivo. We have now performed extensive modifications on its pyrrole core structure, which has culminated in the discovery of 32 (BM-1074). Compound 32 binds to Bcl-2 and Bcl-xL proteins with K(i) values of <1 nM and inhibits cancer cell growth with IC50 values of 1-2 nM in four small-cell lung cancer cell lines sensitive to potent and specific Bcl-2/Bcl-xL inhibitors. Compound 32 is capable of achieving rapid, complete, and durable tumor regression in vivo at a well-tolerated dose schedule. Compound 32 is the most potent and efficacious Bcl-2/Bcl-xL inhibitor reported to date.
