4SC-207


CAS No. : 871015-11-1

4SC-207,871015-11-1
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000084
Molecular Formula:C19H18N4O3S
Molecular Weight:382.43622
Target:microtubule inhibitor
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Appearance:white solid powder
Purity: > 98%
Cat No:I000084
Cas No:871015-11-1
Product-Name:4SC-207
InChI:InChI=1S/C19H18N4O3S/c1-2-26-19(25)23-9-7-14-15(10-20)18(27-16(14)12-23)22-17(24)6-5-13-4-3-8-21-11-13/h3-6,8,11H,2,7,9,12H2,1H3,(H,22,24)/b6-5+
InChIKey:KNQCFGQPDILWLT-AATRIKPKSA-N
SMILES:O=C(OCC)N1CCC2=C(SC(NC(/C=C/C3=CC=CN=C3)=O)=C2C#N)C1
4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. 4SC-207 may be a potential anti-cancer agent.
1:PLoS One. 2013 Nov 6;8(11):e79594. doi: 10.1371/journal.pone.0079594. eCollection 2013. A novel microtubule inhibitor 4SC-207 with anti-proliferative activity in taxane-resistant cells.Bausch E,Kohlhof H,Hamm S,Krauss R,Baumgartner R,Sironi L, PMID: 24324550 PMCID: PMC3855670 DOI: 10.1371/journal.pone.0079594
Abstract: Microtubule inhibitors are invaluable tools in cancer chemotherapy: taxanes and vinca alkaloids have been successfully used in the clinic over the past thirty years against a broad range of tumors. However, two factors have limited the effectiveness of microtubule inhibitors: toxicity and resistance. In particular, the latter is highly unpredictable, variable from patient to patient and is believed to be the cause of treatment failure in most cases of metastatic cancers. For these reasons, there is an increasing demand for new microtubule inhibitors that can overcome resistance mechanisms and that, at the same time, have reduced side effects. Here we present a novel microtubule inhibitor, 4SC-207, which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. In summary, our results suggest that 4SC-207 may be a potential anti-cancer agent.
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