GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM. It targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. The Hedgehog signaling pathway plays an important role in tissue growth and repair; aberrant constitutive activation of Hedgehog pathway signaling and uncontrolled cellular proliferation may be associated with mutations in the Hedgehog-ligand cell surface receptors PTCH and SMO. It inhibits the growth of primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation in vitro and has recently entered the clinic. It also inhibits ABCG2, Pgp, and MRP1-important ABC transporters associated with MDR. The IC50 values of GDC-0449 (Vismodegib) for inhibition of ABCG2 and Pgp were about1.4 and 3.0 ¦ÌM, respectively. It has been used to treat medulloblastoma in animal models.

June 21, 2017

prudect name : GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM. It targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. The Hedgehog signaling pathway plays an important role in tissue growth and repair; aberrant constitutive activation of Hedgehog pathway signaling and uncontrolled cellular proliferation may be associated with mutations in the Hedgehog-ligand cell surface receptors PTCH and SMO. It inhibits the growth of primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation in vitro and has recently entered the clinic. It also inhibits ABCG2, Pgp, and MRP1-important ABC transporters associated with MDR. The IC50 values of GDC-0449 (Vismodegib) for inhibition of ABCG2 and Pgp were about1.4 and 3.0 ¦ÌM, respectively. It has been used to treat medulloblastoma in animal models.
GDC-0449 Vismodegib

Synonyms: GDC-0449 VismodegibCAS NO: 879085-55-9Molecular Formula: C₁₉H₁₄Cl₂N₂O₃SMolecular Weight: 421.30Purity: 98% minSolubility: In DMSOStorage: -20°C

NVP-LDE 225 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515829