TargetMol

NTRC 0066-0

Product Code:
 
TAR-T28216
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T28216-50mg50mg£648.00
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TAR-T28216-100mg100mg£870.00
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Further Information

Bioactivity:
NTRC-0066-0 is a a highly potent and selective inhibitor of TTK. NTRC 0066-0 inhibits the phosphorylation of a TTK substrate and induces chromosome missegregation. NTRC 0066-0 inhibits tumor growth in MDA-MB-231 xenografts as a single agent after oral application. The combination of NTRC 0066-0 with a therapeutic dose of docetaxel resulted in doubling of mouse survival and extended tumor remission, without toxicity.
CAS:
1817791-73-3
Formula:
C33H39N7O2
Molecular Weight:
565.722
Purity:
0.98
SMILES:
CCc1cccc(CC)c1NC(=O)c1ccn-2c1CCc1cnc(Nc3ccc(cc3OC)N3CCN(C)CC3)nc-21

References

1. Zaman GJR, de Roos JADM, Libouban MAA, Prinsen MBW, de Man J, Buijsman RC, Uitdehaag JCM. TTK inhibitors as a targeted therapy for CTNNB1 (?-catenin) mutant cancers. Mol Cancer Ther. 2017 Jul 27. pii: molcanther.0342.2017. doi: 10.1158/1535-7163.MCT-17-0342. [Epub ahead of print] PubMed PMID: 28751540. 2. Uitdehaag JCM, de Man J, Willemsen-Seegers N, Prinsen MBW, Libouban MAA, Sterrenburg JG, de Wit JJP, de Vetter JRF, de Roos JADM, Buijsman RC, Zaman GJR. Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity. J Mol Biol. 2017 Jul 7;429(14):2211-2230. doi: 10.1016/j.jmb.2017.05.014. Epub 2017 May 21. PubMed PMID: 28539250. 3. Libouban MAA, de Roos JADM, Uitdehaag JCM, Willemsen-Seegers N, Mainardi S, Dylus J, de Man J, Tops B, Meijerink JPP, Storchov? Z, Buijsman RC, Medema RH, Zaman GJR. Stable aneuploid tumors cells are more sensitive to TTK inhibition than chromosomally unstable cell lines. Oncotarget. 2017 Jun 13;8(24):38309-38325. doi: 10.18632/oncotarget.16213. PubMed PMID: 28415765; PubMed Central PMCID: PMC5503534. 4. Maia AR, de Man J, Boon U, Janssen A, Song JY, Omerzu M, Sterrenburg JG, Prinsen MB, Willemsen-Seegers N, de Roos JA, van Doornmalen AM, Uitdehaag JC, Kops GJ, Jonkers J, Buijsman RC, Zaman GJ, Medema RH. Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model. Ann Oncol. 2015 Oct;26(10):2180-92. doi: 10.1093/annonc/mdv293. Epub 2015 Jul 7. PubMed PMID: 26153498.