NTRC-0066-0
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MedKoo CAT#: 407828

CAS#: 1817791-73-3

Description: NTRC-0066-0 is a a highly potent and selective small molecule inhibitor of TTK. In cell lines and in mice, 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.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 315 2 Weeks
25mg USD 640 2 Weeks
100mg USD 1460 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-08-03. Prices are subject to change without notice.

NTRC-0066-0, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407828
Name: NTRC-0066-0
CAS#: 1817791-73-3
Chemical Formula: C33H39N7O2
Exact Mass: 565.3165
Molecular Weight: 565.722
Elemental Analysis: C, 70.06; H, 6.95; N, 17.33; O, 5.66


Synonym: NTRC-0066-0; NTRC 0066-0; NTRC0066-0; NTRC-00660; NTRC 00660; NTRC00660

IUPAC/Chemical Name: 8-[2-Methoxy-4-(4-methyl-piperazin-1-yl)-phenylamino]-4,5-dihydro-7,9,9b-triaza-cyclopenta[a]naphthalene-3-carboxylic acid (2,6-diethyl-phenyl)-amide

InChi Key: HGEIUFJVGHMGRR-UHFFFAOYSA-N

InChi Code: InChI=1S/C33H39N7O2/c1-5-22-8-7-9-23(6-2)30(22)36-32(41)26-14-15-40-28(26)13-10-24-21-34-33(37-31(24)40)35-27-12-11-25(20-29(27)42-4)39-18-16-38(3)17-19-39/h7-9,11-12,14-15,20-21H,5-6,10,13,16-19H2,1-4H3,(H,36,41)(H,34,35,37)

SMILES Code: O=C(C(C=C1)=C2N1C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4OC)=NC=C3CC2)NC6=C(CC)C=CC=C6CC


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model.


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 (β-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, Storchová 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.