MPT0B392 |
Catalog No.GC36652 |
MPT0B392, un dérivé de quinoléine actif par voie orale, induit l'activation de la kinase N-terminale c-Jun (JNK), conduisant À l'apoptose. MPT0B392 inhibe la polymérisation de la tubuline et déclenche l'induction de l'arrêt mitotique, suivi de la perte de potentiel de la membrane mitochondriale et du clivage des caspases par activation de JNK et conduit finalement À l'apoptose. MPT0B392 s'est avéré être un nouvel agent de dépolymérisation des microtubules et améliore la cytotoxicité du sirolimus dans les cellules leucémiques aiguës résistantes au sirolimus et la lignée cellulaire multirésistante.
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Cas No.: 1346169-92-3
Sample solution is provided at 25 µL, 10mM.
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.
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