Molecular Weight(MW): 512.5
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.|
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. 
|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. |
|In vitro||DMSO||5 mg/mL (9.75 mM) warming|
|Ethanol||2 mg/mL (3.9 mM)|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02530437||Not yet recruiting||Esophageal Cancer||M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Eli Lilly and Company||November 2016||Phase 1|Phase 2|
|NCT01919398||Recruiting||Neoplasm Metastasis||Eli Lilly and Company||August 2013||Phase 1|
|NCT01697514||Withdrawn||Medulloblastoma, Childhood|Rhabdomyosarcoma||Eli Lilly and Company||July 2013||Phase 1|
|NCT01722292||Terminated||Small Cell Lung Carcinoma||Eli Lilly and Company||January 2013||Phase 1|Phase 2|
|NCT01746745||Completed||Healthy Volunteers||Eli Lilly and Company||January 2013||Phase 1|
|NCT01681186||Completed||Healthy Volunteers||Eli Lilly and Company||September 2012||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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