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CDK&Aurora kinase

TAK901 (934541-31-8)

TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.

Not Intended for Therapeutic Use. For research use only.

CAS: 934541-31-8 Category

TAK901 (934541-31-8) Description

TAK-901 is a small-molecule inhibitor of the serine-threonine kinase Aurora B with potential antineoplastic activity. Aurora B kinase inhibitor TAK-901 binds to and inhibits the activity of Aurora B, which may result in a decrease in the proliferation of tumor cells that overexpress Aurora B. Aurora B is a positive regulator of mitosis that functions in the attachment of the mitotic spindle to the centromere; the segregation of sister chromatids to each daughter cell; and the separation of daughter cells during cytokinesis. This serine/threonine kinase may be amplified and overexpressed by a variety of cancer cell types. Check for active clinical trials or closed clinical trials using this agent.

 

TAK901 (934541-31-8) Specifications

Product Name TAK901
Synonyms TAK901, TAK-901, TAK 901
Chemical Names 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide
Purity ≥98% (HPLC)
CAS Number 934541-31-8
Molecular Formula C28H32N4O3S
Molecular Weight 504.64
Monoisotopic Mass 504.21951 g/mol
MDL number MFCD18782651
InChIKey WKDACQVEJIVHMZ-UHFFFAOYSA-N
InChi Code InChI=1S/C28H32N4O3S/c1-5-36(34,35)21-8-6-7-19(14-21)23-15-22(28(33)30-20-9-11-32(4)12-10-20)18(3)26-25(23)24-13-17(2)16-29-27(24)31-26/h6-8,13-16,20H,5,9-12H2,1-4H3,(H,29,31)(H,30,33)
SMILES O=C(C1=C(C)C2=C(C(C3=CC=CC(S(=O)(CC)=O)=C3)=C1)C4=CC(C)=CN=C4N2)NC5CCN(C)CC5l
Form Powder
Color Crystalline solid
Solubility  Soluble in DMSO (>25 mg/ml)
Storage Temp.  −20°C
Shelf life >2 years if stored properly.
Handling Protect from air and light
Application A novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM

 


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RIDADR NONH for all modes of transport

References:

[1]. Cullinane C, Waldeck KL, Binns D, Bogatyreva E, Bradley DP, de Jong R, McArthur GA, Hicks RJ. Preclinical FLT-PET and FDG-PET imaging of tumor response to the multi-targeted Aurora B kinase inhibitor, TAK-901. Nucl Med Biol. 2014 Feb;41(2):148-54. doi: 10.1016/j.nucmedbio.2013.11.001. Epub 2013 Nov 15. PubMed PMID: 24332383.

[2]. Farrell P, Shi L, Matuszkiewicz J, Balakrishna D, Hoshino T, Zhang L, Elliott S, Fabrey R, Lee B, Halkowycz P, Sang B, Ishino S, Nomura T, Teratani M, Ohta Y, Grimshaw C, Paraselli B, Satou T, de Jong R. Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor. Mol Cancer Ther. 2013 Apr;12(4):460-70. doi: 10.1158/1535-7163.MCT-12-0657. Epub 2013 Jan 28. PubMed PMID: 23358665.

[3]. Farrell P, et al. Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor. Mol Cancer Ther. 2013 Apr;12(4):460-70.