DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated with DAT-230. Apoptosis induced by DAT-230 was related with the activation of caspase-9, caspase-3 and PARP cleavage, which were at the downstream of mitochondria.
CAS 1504583-00-9 MFCD604583009
化学结构图
SMILES: COc1ccc(-c2ccsc2-c2cc(C)c(C)c(OC)c2)cc1N
化学属性
| Mol. Weight | 339.45 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated with DAT-230. Apoptosis induced by DAT-230 was related with the activation of caspase-9, caspase-3 and PARP cleavage, which were at the downstream of mitochondria. |
|---|---|
| Formula | C20H21NO2S |
| Synonym | DAT230; DAT 230; DAT-230. |
| IUPAC Name | 2-methoxy-5-(2-(3-methoxy-4,5-dimethylphenyl)thiophen-3-yl)aniline |
| InChIKey | NPXKFXXMFDKVTM-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H21NO2S/c1-12-9-15(11-19(23-4)13(12)2)20-16(7-8-24-20)14-5-6-18(22-3)17(21)10-14/h5-11H,21H2,1-4H3 |
| Canonical SMILES | NC1=CC(C2=C(C3=CC(C)=C(C)C(OC)=C3)SC=C2)=CC=C1OC |
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- DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated with DAT-230. Apoptosis induced by DAT-230 was related with the activation of caspase-9, caspase-3 and PARP cleavage, which were at the downstream of mitochondria.
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