1. Stem Cell/Wnt
  2. Smo

LY2940680 (Synonyms: Taladegib)

Cat. No.: HY-13242 Purity: 99.76%
Data Sheet SDS Handling Instructions

LY2940680 is an antagonist of the smoothened receptor.

For research use only. We do not sell to patients.
LY2940680 Chemical Structure

LY2940680 Chemical Structure

CAS No. : 1258861-20-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $124 In-stock
5 mg $110 In-stock
10 mg $160 In-stock
50 mg $450 In-stock
100 mg $850 In-stock
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500 mg   Get quote  

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Description

LY2940680 is an antagonist of the smoothened receptor.

IC50 & Target

Smo[1]

In Vitro

LY2940680, a small-molecule antagonist of the smoothened receptor, shows a slight inhibitory effect on cell proliferation without differences between mucin- (IC50: LY2940680=49.8±4.5 μM) and mixed- Cholangiocarcinoma (CCA) (IC50: LY2940680=61.2±21.1 μM)[1]. The IC50 for LY2940680 inhibition of [3H]MRT-92 binding is right shifted (3- to 100-fold) for the S387AECL2, L325F3.36f, and D473H6.54f mutants but did not differ from that of WT receptor for the other mutants. The ability of SANT-1 to inhibit [3H]MRT-92 binding to V329F3.40f and T466F6.47f mutants is abolished, and it is severely impaired for L325F3.40f, I408F5.51f, and M525G7.45f mutants (4- to 140-fold drop of the IC50), but is not modified for the S387AECL2 mutant. Taken together, these data confirm our docking hypothesis that MRT-92-binding mode differs from that of either LY2940680 or SANT-1 by simultaneously occupying binding sites 1 and 2[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01919398 Eli Lilly and Company Neoplasm Metastasis August 2013 Phase 1
NCT01697514 Eli Lilly and Company Medulloblastoma, Childhood|Rhabdomyosarcoma July 2013 Phase 1
NCT01746745 Eli Lilly and Company Healthy Volunteers January 2013 Phase 1
NCT01722292 Eli Lilly and Company Small Cell Lung Carcinoma January 2013 Phase 1|Phase 2
NCT01681186 Eli Lilly and Company Healthy Volunteers September 2012 Phase 1
NCT02530437 M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Ignyta, Inc. Esophageal Cancer March 7, 2017 Phase 1|Phase 2
NCT02784795 Eli Lilly and Company Solid Tumor|Breast Cancer|Colon Cancer|Cholangiocarcinoma|Soft Tissue Sarcoma November 2016 Phase 1
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References
Molecular Weight

512.5

Formula

C₂₆H₂₄F₄N₆O

CAS No.

1258861-20-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 5.2 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
LY2940680
Cat. No.:
HY-13242
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