BM-1244
Based on 1 Customer Validation
BM-1244 (APG-1252-M1) is a Bcl-xL/Bcl-2 inhibitor with Kis of 134 nM and 450 nM. BM-1244 has anti-tumor effects by inducing apoptosis and suppressing tumor growth. BM-1244 can induce cytochrome C and Smac release from mitochondria with caspase-3 and PARP cleavage. BM-1244 exhibits synergy with chemotherapy in vivo. BM-1244 can be studied in research for colorectal cancer, acute myeloid leukemia and gastric cancer.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1619923-32-8
- Formula: C54H59ClF4N6O8S4
- Molecular Weight:1159.79
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
BM-1244 (Compound APG-1252-M1) (10 nM-100 μM, 3 d) inhibits the proliferation in cells that expresses Bcl-2, Bcl-xl and Bax (AGS (IC50 = 1.146 μM), N87 (IC50 = 0.9007 μM)[2].
BM-1244 (0.03-3 μM) activates the protein of capase and leads to the release of cytochrome c by inhibiting Bcl-2/Bcl-xl, and results in apoptosis in AGS and N87 cell lines[2].
BM-1244 (0.03-1 μM, 48 h) changes the ratio of apoptotic AGS and N87 cancer cells with increased concentration, but has no effect on the cell cycle[2].
BM-1244 (0.03-0.3 μM, 24 h) downregulates the ratio of JC-laggregate-positive and JC-1 monomer-positive cells with increased concentration in AGS and N87 cells[2].
BM-1244 (0.3 μM) increases the percentage of apoptotic cells when combined with 5-FU (HY-90006) (3 μM) in AGS and N87 cells[2].
BM-1244 (Compound APG-1252-M1) (1 μM, 24 h) decreases the survival of some sensitive CRC cell lines (HCC2998, HCT116, SW480) and induces apoptosis[3].
BM-1244 (1 μM, 2 h) results in the release of Cyt C and Smac from mitochondria in HCT116 cells[3].
BM-1244 (1 μM, 4-24 h) decreases Mcl-1 levels in HCC2998 cells starting at 8 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC2998 and HCT116 cells
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Concentration:1 μM
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Incubation Time:4, 8, 12, 16, 24 h
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Result:Did not alter the levels of Bcl-2, Bcl-XL, Bim, Bax, DR4, DR5 and LC3 II in HCT116 cells.
Increased the level of Mcl-1 and Bid from 2 to 24 h.
Did not alter LC3 II levels in HCC2998 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c athymic nude mice (male, 4-6 weeks), cells of N87 mixed with Matrigel (1:5, s.c. into right infra-axillary)[2]
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Dosage:25, 50, 100 mg/kg qd for 10 days; 25 mg/kg once a week for 2 weeks when combined with 5-FU; 50 mg/kg qd for 10 days
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Administration:Intravenous injection (i.v.)
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Result:Prohibited the growth of tumor when used alone.
Did not affect the body weight of mice.
Resulted in lightest tumor weight with 100 mg/kg.
Resulted in higher expression of cleaved caspase 3 in combined group.
Chemical Information
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CAS No. 1619923-32-8
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Appearance Solid
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Molecular Weight 1159.79
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Formula C54H59ClF4N6O8S4
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Color White to off-white
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SMILES
O=C(C1CCN(CC[C@@H](NC2=CC=C(S(=O)(NC3=CC=C(N4CCN(C5=CC(F)=CC(C6=C(C7=CC=C(Cl)C=C7)N(C(C)C)C(C)=C6S(=O)(C)=O)=C5)CC4)C=C3)=O)C=C2S(=O)(C(F)(F)F)=O)CSC8=CC=CC=C8)CC1)O
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Synonyms
APG-1252-M1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 120 mg/mL (103.47 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)
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 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (4.31 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Purity & Documentation
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Data Sheet (282 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)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Kim R. Unknotting the roles of Bcl-2 and Bcl-xL in cell death. Biochem Biophys Res Commun. 2005;333(2):336-343. [Content Brief]
[2]. Yi, H., et al., (2020). Bcl-2/Bcl-xl inhibitor APG-1252-M1 is a promising therapeutic strategy for gastric carcinoma. Cancer medicine, 9(12), 4197-4206. [Content Brief]
[3]. Yao, W., et al., (2022). Mcl-1 levels critically impact the sensitivities of human colorectal cancer cells to APG-1252-M1, a novel Bcl-2/Bcl-XL dual inhibitor that induces Bax-dependent apoptosis. Neoplasia (New York, N.Y.), 29, 100798. [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 | 0.8622 mL | 4.3111 mL | 8.6223 mL | 21.5556 mL |
| 5 mM | 0.1724 mL | 0.8622 mL | 1.7245 mL | 4.3111 mL | |
| 10 mM | 0.0862 mL | 0.4311 mL | 0.8622 mL | 2.1556 mL | |
| 15 mM | 0.0575 mL | 0.2874 mL | 0.5748 mL | 1.4370 mL | |
| 20 mM | 0.0431 mL | 0.2156 mL | 0.4311 mL | 1.0778 mL | |
| 25 mM | 0.0345 mL | 0.1724 mL | 0.3449 mL | 0.8622 mL | |
| 30 mM | 0.0287 mL | 0.1437 mL | 0.2874 mL | 0.7185 mL | |
| 40 mM | 0.0216 mL | 0.1078 mL | 0.2156 mL | 0.5389 mL | |
| 50 mM | 0.0172 mL | 0.0862 mL | 0.1724 mL | 0.4311 mL | |
| 60 mM | 0.0144 mL | 0.0719 mL | 0.1437 mL | 0.3593 mL | |
| 80 mM | 0.0108 mL | 0.0539 mL | 0.1078 mL | 0.2694 mL | |
| 100 mM | 0.0086 mL | 0.0431 mL | 0.0862 mL | 0.2156 mL |
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