Name: Taladegib (LY2940680)
Brand: Selleck Chemicals
SKU: S2157
Availability: InStock
Rating: 5 (7 reviews)

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Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	JAK TGF-beta/Smad Wnt/beta-catenin ERK GSK-3 ROCK PKA Secretase STAT Casein Kinase
Other Hedgehog/Smoothened Inhibitors	SAG (Smoothened Agonist) Hydrochloride Purmorphamine Cyclopamine (11-Deoxojervine) GANT 61 (NSC 136476) SAG (Smoothened Agonist) SANT-1 HPI-4 (Ciliobrevin A) BMS-833923 Ciliobrevin D Jervine

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.75mg/ml (7.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.54mg/ml (1.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	512.5	Formula	C₂₆H₂₄F₄N₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1258861-20-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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

Read more about storage stability stock solution CAS number SMILES

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	[1] https://pubmed.ncbi.nlm.nih.gov/22007748/ [2] http://cancerres.aacrjournals.org/cgi/content/meeting_abstract/71/8_MeetingAbstracts/2819?si

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-15)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07454291	RECRUITING	Idiopathic Pulmonary Fibrosis	Endeavor Biomedicines, Inc.	2026-04-28	PHASE1
NCT05199584	COMPLETED	Solid Tumors With PTCH1 Loss-of-function Mutations	Endeavor Biomedicines, Inc.	2022-05-24	PHASE2
NCT04968574	COMPLETED	Idiopathic Pulmonary Fibrosis	Endeavor Biomedicines, Inc.	2021-08-26	PHASE2
NCT05817240	COMPLETED	Idiopathic Pulmonary Fibrosis	Endeavor Biomedicines, Inc.	2023-05-03	PHASE1
NCT02530437	TERMINATED	Gastroesophageal Junction Adenocarcinoma; Stage IB Esophageal Adenocarcinoma AJCC v7; Stage II Esophageal Adenocarcinoma AJCC v7; Stage IIA Esophageal Adenocarcinoma AJCC v7; Stage IIB Esophageal Adenocarcinoma AJCC v7; Stage IIIA Esophageal Adenocarcinoma AJCC v7; Stage IIIB Esophageal Adenocarcinoma AJCC v7	M.D. Anderson Cancer Center	2017-03-07	PHASE1; PHASE2
NCT02784795	TERMINATED	Solid Tumor; Breast Cancer; Colon Cancer; Cholangiocarcinoma; Soft Tissue Sarcoma	Eli Lilly and Company	2016-11-04	PHASE1

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Taladegib (LY2940680) Hedgehog/Smoothened inhibitor

Chemical Structure

Molecular Weight: 512.5