Taladegib (LY2940680)

Catalog No.S2157

For research use only.

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

Taladegib (LY2940680) Chemical Structure

CAS No. 1258861-20-9

Selleck's Taladegib (LY2940680) has been cited by 5 Publications

Purity & Quality Control

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Biological Activity

Description Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
Targets
Smoothened [1]
In vitro

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. [1]

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. [2]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 512.5
Formula

C26H24F4N6O

CAS No. 1258861-20-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C(=CC=N1)C2=NN=C(C3=CC=CC=C32)N4CCC(CC4)N(C)C(=O)C5=C(C=C(C=C5)F)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01919398 Completed Drug: LY2940680 Neoplasm Metastasis Eli Lilly and Company August 2013 Phase 1
NCT01697514 Withdrawn Drug: LY2940680 Medulloblastoma Childhood|Rhabdomyosarcoma Eli Lilly and Company July 2013 Phase 1
NCT01746745 Completed Drug: [^14C]-LY2940680 Healthy Volunteers Eli Lilly and Company January 2013 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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