MPT0B392
Based on 1 Customer Validation
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.63%
- CAS 番号: 1346169-92-3
- 分子式: C19H20N2O6S
- 分子量:404.44
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保管条件:Powder -20°C, 3 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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Caspase アイソフォーム固有の製品をすべて表示
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生物活性
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JNK |
Caspase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
16 nM
Compound: 15
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Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay
Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay
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[PMID: 22060033] |
| KB | IC50 |
18 nM
Compound: 15
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Growth inhibition of human KB cells after 72 hrs by methylene blue assay
Growth inhibition of human KB cells after 72 hrs by methylene blue assay
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[PMID: 22060033] |
| MKN-45 | IC50 |
4 nM
Compound: 15
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Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay
Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay
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[PMID: 22060033] |
MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) inhibits the cell viability of HL60, MOLT-4, and CCRF-CEM cells with IC50s of 0.02 μM, 0.03 μM and 0.02 μM, respectively[1].
MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells[1].
MPT0B392 (0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours) triggers cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner[1].
MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreases in Mcl-1L[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) cells
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Concentration:0.001, 0.003, 0.01, 0.03, 0.1 μM
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Incubation Time:24 and 48 hours
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Result:Inhibited the cell viability.
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Cell Line:HL60 cells
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Concentration:0.1 μM
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Incubation Time:48 hours
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Result:Induced apoptosis in cancer cells.
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Cell Line:HL60 cells
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Concentration:0.1 μM or 0.01, 0.03, 0.1 μM
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Incubation Time:0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours
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Result:Triggered cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner.
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Cell Line:HL60 cells
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Concentration:0.1 μM
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Incubation Time:48 hours
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Result:Increased the phosphorylation of Bcl-2, Mcl-1S and decreased in Mcl-1L.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Severe combined immunodeficient (SCID) mice [1]
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Dosage:50 mg/kg or 100 mg/kg
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Administration:Oral gavage; 12 or 14 days
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Result:Resulted in significant tumor growth delay (83.3%) and tumor volume inhibition without loss of body weight.
化学情報
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CAS 番号 1346169-92-3
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性状 Solid
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分子量 404.44
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分子式 C19H20N2O6S
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Color Light yellow to yellow
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SMILES
NC1=C2C(N=C(S(=O)(C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=CC=C1OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (247.26 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 2.4726 mL | 12.3628 mL | 24.7255 mL | 61.8139 mL |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | 12.3628 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 mL | 6.1814 mL | |
| 15 mM | 0.1648 mL | 0.8242 mL | 1.6484 mL | 4.1209 mL | |
| 20 mM | 0.1236 mL | 0.6181 mL | 1.2363 mL | 3.0907 mL | |
| 25 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4726 mL | |
| 30 mM | 0.0824 mL | 0.4121 mL | 0.8242 mL | 2.0605 mL | |
| 40 mM | 0.0618 mL | 0.3091 mL | 0.6181 mL | 1.5453 mL | |
| 50 mM | 0.0495 mL | 0.2473 mL | 0.4945 mL | 1.2363 mL | |
| 60 mM | 0.0412 mL | 0.2060 mL | 0.4121 mL | 1.0302 mL | |
| 80 mM | 0.0309 mL | 0.1545 mL | 0.3091 mL | 0.7727 mL | |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2473 mL | 0.6181 mL |
MPT0B392 関連分類
HY-101287 関連分類
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