TAK-960
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MedKoo CAT#: 205639

CAS#: 1137868-52-0 (free base)

Description: TAK-960 is a n orally available PLK1 inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor TAK-960 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressed tumor cells. PLK1, named after the polo gene of Drosophila melanogaster, is a serine/threonine kinase crucial in the regulation of mitosis.


Chemical Structure

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TAK-960
CAS# 1137868-52-0 (free base)

Theoretical Analysis

MedKoo Cat#: 205639
Name: TAK-960
CAS#: 1137868-52-0 (free base)
Chemical Formula: C27H34F3N7O3
Exact Mass: 561.26752
Molecular Weight: 561.59917
Elemental Analysis: C, 57.74; H, 6.10; F, 10.15; N, 17.46; O, 8.55

Price and Availability

Size Price Availability Quantity
50.0mg USD 550.0 2 Weeks
100.0mg USD 950.0 2 Weeks
200.0mg USD 1450.0 2 Weeks
500.0mg USD 2450.0 2 Weeks
1.0g USD 3650.0 2 Weeks
2.0g USD 5950.0 2 Weeks
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Related CAS #: 1137868-52-0 (free base)   1137868-96-2 (HCl)    

Synonym: TAK960, TAK 960, TAK960

IUPAC/Chemical Name: 4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide

InChi Key: GWRSATNRNFYMDI-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H34F3N7O3/c1-35-10-8-16(9-11-35)32-24(38)18-12-22(40-3)20(13-19(18)28)33-26-31-14-21-23(34-26)37(17-6-4-5-7-17)15-27(29,30)25(39)36(21)2/h12-14,16-17H,4-11,15H2,1-3H3,(H,32,38)(H,31,33,34)

SMILES Code: O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C=C2F

Appearance: White to beige 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, not in water

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

Preparing Stock Solutions

The following data is based on the product molecular weight 561.59917 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message

Sent On: Wed Nov 11 14:13:40 2020

Search: TAK-960

8 selected items

PubMed Results
Items 1-8 of 8 (Display the 8 citations in PubMed)

1: Hennenberg M, Kuppermann P, Yu Q, Herlemann A, Tamalunas A, Wang Y, Rutz B, Ciotkowska A, Strittmatter F, Stief CG, Gratzke C. Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734. doi: 10.3389/fphys.2018.00734. PMID: 29962965; PMCID: PMC6013909.

2: Klauck PJ, Bagby SM, Capasso A, Bradshaw-Pierce EL, Selby HM, Spreafico A, Tentler JJ, Tan AC, Kim J, Arcaroli JJ, Purkey A, Messersmith WA, Kuida K, Eckhardt SG, Pitts TM. Antitumor activity of the polo-like kinase inhibitor, TAK-960, against preclinical models of colorectal cancer. BMC Cancer. 2018 Feb 5;18(1):136. doi: 10.1186/s12885-018-4036-z. PMID: 29402316; PMCID: PMC5800287.

3: Talati C, Griffiths EA, Wetzler M, Wang ES. Polo-like kinase inhibitors in hematologic malignancies. Crit Rev Oncol Hematol. 2016 Feb;98:200-10. doi: 10.1016/j.critrevonc.2015.10.013. Epub 2015 Nov 4. PMID: 26597019.

4: Inoue M, Yoshimura M, Kobayashi M, Morinibu A, Itasaka S, Hiraoka M, Harada H. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666. doi: 10.1038/srep15666. PMID: 26503893; PMCID: PMC4621528.

5: Nair JS, Schwartz GK. Inhibition of polo like kinase 1 in sarcomas induces apoptosis that is dependent on Mcl-1 suppression. Cell Cycle. 2015;14(19):3101-11. doi: 10.1080/15384101.2015.1078033. PMID: 26236920; PMCID: PMC4825583.

6: Williams R. Discontinued in 2013: oncology drugs. Expert Opin Investig Drugs. 2015 Jan;24(1):95-110. doi: 10.1517/13543784.2015.971154. Epub 2014 Oct 14. PMID: 25315907.

7: Nie Z, Feher V, Natala S, McBride C, Kiryanov A, Jones B, Lam B, Liu Y, Kaldor S, Stafford J, Hikami K, Uchiyama N, Kawamoto T, Hikichi Y, Matsumoto S, Amano N, Zhang L, Hosfield D, Skene R, Zou H, Cao X, Ichikawa T. Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083. Epub 2013 Feb 27. PMID: 23664874.

8: Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E. TAK-960, a novel, orally available, selective inhibitor of polo- like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar;11(3):700-9. doi: 10.1158/1535-7163.MCT-11-0762. Epub 2011 Dec 21. PMID: 22188812.

TAK-960

50.0mg / USD 550.0