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MPT0B392

Catalog No.GC36652

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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MPT0B392 Chemical Structure

Cas No.: 1346169-92-3

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Sample solution is provided at 25 µL, 10mM.

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Background

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[1]. JNK Caspase

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]. Cell Viability Assay[1] Cell Line: HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) cells

The effects of MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) shows relative potent anti-leukemia activity in a vivo xenograft model[1]. Animal Model: Severe combined immunodeficient (SCID) mice [1]

[1]. Chao MW, et al. An oral quinoline derivative, MPT0B392, causes leukemic cells mitotic arrest and overcomes drug resistant cancer cells. Oncotarget. 2017 Apr,8(17):27772-27785.

Chemical Properties

Cas No. 1346169-92-3 SDF
Canonical SMILES NC1=C2C(N=C(S(=O)(C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=CC=C1OC
Formula C19H20N2O6S M.Wt 404.44
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

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1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3628 mL 24.7255 mL
5 mM 0.4945 mL 2.4726 mL 4.9451 mL
10 mM 0.2473 mL 1.2363 mL 2.4726 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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