product name Taladegib (LY2940680)
Description: Taladegib (also known as LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Taladegib binds mostly to extracelluar loops and has a different functioning site with the reported Smo receptor inhibitor SANT-1 which binds to 7TM. LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib.
References: Expert Opin Investig Drugs. 2011 Dec;20(12):1649-64.
512.5
Formula
C26H24F4N6O
CAS No.
1258861-20-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (9.8 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (3.9 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19426140
| In Vitro |
In vitro activity: LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. Kinase Assay: Cell Assay: When tested with cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib, LY2940680 inhibited cell proliferation. |
|---|---|
| In Vivo | LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. |
| Animal model | |
| Formulation & Dosage | |
| References | Expert Opin Investig Drugs. 2011 Dec;20(12):1649-64. |
