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Cat. No. Name Size Price Add Cart
KI1459TAK-441QuoteQuote

Chemical Characteristic

Product NameTAK-441
CAS No.1186231-83-3
Molecular Weight 576.56
FormulaC28H31F3N4O6
Chemical Name6-Ethyl-N-[1-(hydroxyacetyl)piperidin-4-yl]-1-methyl-4-oxo-5-(2-oxo-2-phenylethyl)-3-(2,2,2-trifluoroethoxy)-4,5-dihydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide
Smilesc1(=O)c2c(cc(n1CC(=O)c1ccccc1)CC)n(c(c2OCC(F)(F)F)C(=O)NC1CCN(CC1)C(=O)CO)C
Chemical Structure

Biological activities

TAK-441 is a potent, selective hedgehog signaling pathway inhibitor. The IC90 value of TAK-441 for tumor growth inhibition is 0.68 µg/mL. TAK-441 binds to Smo and is being developed for the treatment of cancer.[1] TAK-441 suppresses transcription factor Gli1 mRNA expression in tumor-associated stromal tissue. TAK-441 also inhibits tumor growth (treatment/control ratio, 3%) in a mouse medulloblastoma allograft model.[2] TAK-441 treatment significantly delays castration-resistant progression of LNCaP xenografts.[3] In mice bearing xenografts of human pancreatic tumors, the IC50 values of TAK-441 for Gli1 mRNA inhibition in the tumor and skin are estimated to be 45.7 and 113 ng/mL, respectively.[1]

Protocols

In vivo: TAK-441 is dissolved in dimethylsulfoxide-polyethylene glycol (1:1, v/v).[1]

References

[1] Kogame A, et al. Pharmacokinetic and pharmacodynamic modeling of hedgehog inhibitor TAK-441 for the inhibition of Gli1 messenger RNA expression and antitumor efficacy in xenografted tumor model mice. Drug Metab Dispos. 2013, 41(4): 727-734.
[2] Ohashi T, et al. Discovery of the investigational drug TAK-441, a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor: modification of the core skeleton for improved solubility. Bioorg Med Chem. 2012, 20(18): 5507-5517.
[3] N Ibuki, et al. TAK-441, a novel investigational smoothened antagonist, delays castration-resistant progression in prostate cancer by disrupting paracrine hedgehog signaling. International Journal of Cancer. 2013.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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