MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953).
CAS 1215208-65-3 MFCD315208653
化学结构图
SMILES: COc1cc(C(=O)c2ccc3c(N)c(OC)ccc3n2)cc(OC)c1OC
化学属性
| Mol. Weight | 368.38 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953). |
|---|---|
| Formula | C20H20N2O5 |
| Synonym | MPT0B214; MPT 0B214; MPT-0B214 |
| IUPAC Name | (5-amino-6-methoxyquinolin-2-yl)(3,4,5-trimethoxyphenyl)methanone |
| InChIKey | HBQYPNDXFXSVNP-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H20N2O5/c1-24-15-8-7-13-12(18(15)21)5-6-14(22-13)19(23)11-9-16(25-2)20(27-4)17(10-11)26-3/h5-10H,21H2,1-4H3 |
| Canonical SMILES | O=C(C1=NC2=CC=C(OC)C(N)=C2C=C1)C3=CC(OC)=C(OC)C(OC)=C3 |
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- MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953).
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