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.
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- Pureté : 99.83%
- CAS No.: 1619923-32-8
- Formule: C54H59ClF4N6O8S4
- Masse moléculaire:1159.79
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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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Masse moléculaire 1159.79
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
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)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
Protocole
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Pureté et documentation
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Fiche technique (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)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[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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