MPT0B014
Based on 1 Customer Validation
MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.67%
- CAS No.: 1215208-59-5
- Formule: C19H17NO4
- Masse moléculaire:323.34
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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
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Tubulin polymerization[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
24.6 nM
Compound: 9
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Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay
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[PMID: 20148562] |
| KB | IC50 |
24 nM
Compound: 9
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Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay
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[PMID: 20148562] |
| MKN-45 | IC50 |
16.3 nM
Compound: 9
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Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay
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[PMID: 20148562] |
| NCI-H460 | IC50 |
36 nM
Compound: 9
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Antiproliferative activity against human H460 cells after 72 hrs by methylene blue dye assay
Antiproliferative activity against human H460 cells after 72 hrs by methylene blue dye assay
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[PMID: 20148562] |
MPT0B014 (0-1 μM; 48 h) inhibits A549, H1299 and H226 cells growth in a dose-dependent manner[1].
MPT0B014 (0.05-0.3 μM; 24 and 48 h) arrests cell cycle at G2/M and sub-G1 phases and induces apoptosis in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, H1299, H226 and HUVEC cells
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Concentration:0, 0.025, 0.05, 0.075 and 1 μM
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Incubation Time:48 h
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Result:Inhibited cell viability with IC50s of 0.109±0.01, 0.055±0.004, 0.077±0.005 and 0.536±0.166 μM against A549, H1299, H226 and HUVEC cells, respectively.
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Cell Line:A549, H1299 and H226
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Concentration:0.05, 0.1 and 0.3 μM
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Incubation Time:24 and 48 h
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Result:Treatment for 24 h led to notable accumulation of cells in the G2/M phase. At 48 h, sub-G1 apoptotic cell populations were increased in a concentration-dependent manner. Cells in the G2/M phase began to rise at 12 h post-treatment and peaked at 24 h. Following this, there was an emergence of cells in the sub-G1 population phase until 48 h.
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Cell Line:A549, H1299 and H226
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Concentration:0.05, 0.1 and 0.3 μM
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Incubation Time:24 h
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Result:Resulted in a marked increase in expression of the mitosis marker MPM2 and the proteins cyclin B1, Cdc2, Thr161, Aurora A and Aurora B in a concentration-dependent manner. Decreased the expression of Cdc (Tyr15) and Cdc25C, whereas total protein levels of Cdc2 did not change.
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Cell Line:A549
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Concentration:0.05, 0.075, 0.1 and 0.3 μM
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Incubation Time:48 h
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Result:Induced apoptosis in a concentration-dependent manner.
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Cell Line:A549
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Concentration:0.05, 0.1 and 0.3 μM
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Incubation Time:24, 36 and 48 h
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Result:Induced activation of caspases-3, -7, -8 and -9, and cleavage of PARP in a time- and concentration-dependent manner. Significantly induced Bcl-2 phosphorylation. Down-regulated Mcl-1 expression in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude athymic mice, A549 xenografts[1]
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Dosage:100 mg/kg alone or in combination with 25 mg/kg Erlotinib (HY-50896)
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Administration:i.v./i.p., daily for 25 days
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Result:The combined treatment resulted in more significant tumor growth delay (28%) compared with treatment alone (7%). The combination produced significantly higher anti-tumor activity. The growth of A549 cancer cell xenografts was suppressed by 11, 21 and 49% (tumor growth inhibition) after treatment with MPT0B014, Erlotinib and MPT0B014 plus Erlotinib, respectively.
Chemical Information
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CAS No. 1215208-59-5
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Appearance Solid
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Masse moléculaire 323.34
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Formule C19H17NO4
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Color Off-white to light yellow
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SMILES
O=C(C1=CC=C2N=CC=CC2=C1)C3=CC(OC)=C(OC)C(OC)=C3
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Synonyms
6-(3′,4′,5′-Trimethoxybenzoyl)quinoline
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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
DMSO : 50 mg/mL (154.64 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)
Pureté et documentation
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Fiche technique (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 3.0927 mL | 15.4636 mL | 30.9272 mL | 77.3180 mL |
| 5 mM | 0.6185 mL | 3.0927 mL | 6.1854 mL | 15.4636 mL | |
| 10 mM | 0.3093 mL | 1.5464 mL | 3.0927 mL | 7.7318 mL | |
| 15 mM | 0.2062 mL | 1.0309 mL | 2.0618 mL | 5.1545 mL | |
| 20 mM | 0.1546 mL | 0.7732 mL | 1.5464 mL | 3.8659 mL | |
| 25 mM | 0.1237 mL | 0.6185 mL | 1.2371 mL | 3.0927 mL | |
| 30 mM | 0.1031 mL | 0.5155 mL | 1.0309 mL | 2.5773 mL | |
| 40 mM | 0.0773 mL | 0.3866 mL | 0.7732 mL | 1.9329 mL | |
| 50 mM | 0.0619 mL | 0.3093 mL | 0.6185 mL | 1.5464 mL | |
| 60 mM | 0.0515 mL | 0.2577 mL | 0.5155 mL | 1.2886 mL | |
| 80 mM | 0.0387 mL | 0.1933 mL | 0.3866 mL | 0.9665 mL | |
| 100 mM | 0.0309 mL | 0.1546 mL | 0.3093 mL | 0.7732 mL |
MPT0B014 Related Classifications
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