GDC-0449 (Vismodegib) is a potent, orally bioavailable, specific hedgehog pathway small-molecule inhibitor with IC50 of 3 nM. It blocks the activities of the Hedgehog-ligand cell surface receptor SMO and suppresses Hedgehog signaling [1].The hedgehog (HH) pathway, a key signaling pathway in embryological development, is normally inactive in differentiated cells, with the exception of roles in tissue maintenance and repair. Constitutive reactivation of the HH pathway via mutations and aberrant autocrine/paracrine HH ligand stimulation has been linked to a number of cancers5. GDC-0449 has been shown to target SMO with an EC50 of 2.8nmol/L on a human palatal mesenchymal cell line (HEPM) stably expressing a GLI-responsive luciferase reporter gene, and to induce rapid regression of the tumor and suppression of the hedgehog pathway in the Ptc1+/? murine medulloblastoma model. Furthermore, GDC-0449 inhibits the growth of primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation in vitro [1-3]. GDC-0449 is also an inhibitor of two multiple ATP-binding cassette (ABC) transporters, ABCG2/BCRP and ABCB1/Pgp, and is a mild inhibitor of ABCC1/MRP1. The overexpression of ABC transporters is associated with multidrug resistance. The IC50 values for inhibition of ABCG2 and Pgp were approximately 1.4 and 3.0 µM, respectively [4].

Technical information:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.

Cellagen利用广泛的研究以及我们在干细胞生物学，药物化学和产品开发方面的专业知识，Cellagen长期以来一直为专业OEM产品提供世界领先的公司，为一线干细胞研究奠定了基础。

现在，Cellagen扩展了其最佳产品系列，并直接向研究界提供。Cellagen与世界领先的科学家有着密切的联系，并且始终认识到高标准科学研究的未满足需求。