Taladegib (LY2940680)

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

Taladegib (LY2940680) Chemical Structure

Taladegib (LY2940680) Chemical Structure

CAS No. 1258861-20-9

Purity & Quality Control

Taladegib (LY2940680) Related Products

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01919398 Completed
Neoplasm Metastasis
Eli Lilly and Company
August 2013 Phase 1
NCT01697514 Withdrawn
Medulloblastoma Childhood|Rhabdomyosarcoma
Eli Lilly and Company
July 2013 Phase 1
NCT01746745 Completed
Healthy Volunteers
Eli Lilly and Company
January 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 512.5 Formula

C26H24F4N6O

CAS No. 1258861-20-9 SDF Download Taladegib (LY2940680) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (146.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 27 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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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