Home Stem Cells & Wnt Hedgehog/Smoothened inhibitor Taladegib (LY2940680)

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Taladegib (LY2940680) Hedgehog/Smoothened inhibitor

Cat.No.S2157

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

Chemical Structure

Molecular Weight: 512.5

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Quality Control

Batch: Purity: 99.82%
99.82

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (146.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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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Chemical Information, Storage & Stability

Molecular Weight 512.5 Formula

C26H24F4N6O

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

Synonyms N/A 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

Mechanism of Action

Targets/IC50/Ki
Smoothened
In vitro
Taladegib (LY2940680) inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patients with cancer who developed resistance to vismodegib.
In vivo
Taladegib (LY2940680) has excellent pharmacokinetic properties in rodent and non-rodent species. When administered orally to Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, it produces remarkable efficacy and significantly improves their survival. This compound reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. It inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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