Cyclopamine/11-deoxojervine

Solubility:DMSO

Storage:-20C 2 years

Biologieal

GDC-0449 is a more potent and specific synthetic oral SMO(signaling transducer Smoothened)inhibitor,with 0.003µM of Gli-luc(Gli-luciferase assay)IC50,GDC-0449,which inhibits the growth of primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation in vitro and has recently entered the clinic.

Reference

1. Tremblay MR, Nesler M, Weatherhead R, Castro AC.Recent patents for Hedgehog pathway inhibitors for the treatment of malignancy. Expert Opin Ther Pat. 2009 Jun 8

2. Scales SJ, de Sauvage FJ. Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol Sci. 2009 Jun;30(6):303-12. Epub 2009 May 13.

3. Zhang Y, Laterra J, Pomper MG. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp.Neoplasia. 2009 Jan;11(1):96-101.

4. Molckovsky A, Siu LL.First-in-class, first-in-human phase I results of targeted agents: Highlights of the 2008 American Society of Clinical Oncology meeting.J Hematol Oncol. 2008 Oct 29;1:20.

5. LoRusso, P.M. et al. (2008) A first-in-human, first-in-class, phase 1 study of systemic Hedgehog pathway antagonist, GDC-0449, in patients with advanced solid tumors. J. Clin. Oncol. 26 (Suppl.), 3516

6. Rudin, C.M. et al. (2008) Updated safety and efficacy data from a firstin-human, first-in-class phase I study of Hedgehog pathway antagonist GDC-0449. European Journal of Cancer Supplements 6, 112�C113