Description
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.
Product information
CAS Number: 1346169-92-3
Molecular Weight: 404.44
Formula: C19H20N2O6S
Chemical Name: 6-methoxy-2-(3,4,5-trimethoxybenzenesulfonyl)quinolin-5-amine
Smiles: COC1C(=CC(=CC=1OC)S(=O)(=O)C1C=CC2=C(N)C(=CC=C2N=1)OC)OC
InChiKey: RBBRZMLZQCYQJM-UHFFFAOYSA-N
InChi: InChI=1S/C19H20N2O6S/c1-24-14-7-6-13-12(18(14)20)5-8-17(21-13)28(22,23)11-9-15(25-2)19(27-4)16(10-11)26-3/h5-10H,20H2,1-4H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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. MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells. 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. MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreases in Mcl-1L.
In Vivo:
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.
Products are for research use only. Not for human use.
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