[CAS NO. 1258861-20-9] Taladegib
PRODUCTS SPECIFICATIONS [1258861-20-9]
DESCRIPTION [1258861-20-9]
Overview
| MDL | MFCD21609264 |
|---|---|
| Molecular Weight | 512.50 |
| Molecular Formula | C26H24F4N6O |
| SMILES | CN1N=CC=C1C2=C3C(C=CC=C3)=C(N=N2)N4CCC(CC4)N(C)C(C5=C(C=C(C=C5)F)C(F)(F)F)=O |
1 Publications Citing Use of MCE
Summary
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
IC50 & Target
Smo [1]
In Vitro
Taladegib, a small-molecule antagonist of the smoothened receptor, shows a slight inhibitory effect on cell proliferation without differences between mucin- (IC 50 : Taladegib=49.8±4.5 μM) and mixed- Cholangiocarcinoma (CCA) (IC 50 : Taladegib=61.2±21.1 μM) [1] . The IC 50 for Taladegib inhibition of [ 3 H]MRT-92 binding is right shifted (3- to 100-fold) for the S387A ECL2 , L325F 3.36f , and D473H 6.54f mutants but did not differ from that of WT receptor for the other mutants. The ability of SANT-1 to inhibit [ 3 H]MRT-92 binding to V329F 3.40f and T466F 6.47f mutants is abolished, and it is severely impaired for L325F 3.40f , I408F 5.51f , and M525G 7.45f mutants (4- to 140-fold drop of the IC 50 ), but is not modified for the S387A ECL2 mutant. Taken together, these data confirm our docking hypothesis that MRT-92-binding mode differs from that of either Taladegib or SANT-1 by simultaneously occupying binding sites 1 and 2 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01226485 | Eli Lilly and Company |
Advanced Cancer
|
September 2010 | Phase 1 |
| NCT05199584 | Endeavor Biomedicines, Inc. |
Solid Tumors With PTCH1 Loss-of-function Mutations
|
May 24, 2022 | Phase 2 |
| NCT01722292 | Eli Lilly and Company |
Small Cell Lung Carcinoma
|
January 2013 | Phase 1|Phase 2 |
| NCT01697514 | Eli Lilly and Company |
Medulloblastoma, Childhood|Rhabdomyosarcoma
|
July 2013 | Phase 1 |
| NCT01681186 | Eli Lilly and Company |
Healthy Participants
|
September 2012 | Phase 1 |
| NCT01919398 | Eli Lilly and Company |
Neoplasm Metastasis
|
August 2013 | Phase 1 |
| NCT02784795 | Eli Lilly and Company |
Solid Tumor|Breast Cancer|Colon Cancer|Cholangiocarcinoma|Soft Tissue Sarcoma
|
November 4, 2016 | Phase 1 |
| NCT02530437 | M.D. Anderson Cancer Center|National Cancer Institute (NCI) |
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
|
March 7, 2017 | Phase 1|Phase 2 |
| NCT04968574 | Endeavor Biomedicines, Inc. |
Idiopathic Pulmonary Fibrosis
|
August 26, 2021 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 97.56 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9512 mL | 9.7561 mL | 19.5122 mL |
| 5 mM | 0.3902 mL | 1.9512 mL | 3.9024 mL |
| 10 mM | 0.1951 mL | 0.9756 mL | 1.9512 mL |
References
- [1] Fraveto A, et al, Sensitivity of Human Intrahepatic Cholangiocarcinoma Subtypes to Chemotherapeutics and Molecular Targeted Agents: A Study on Primary Cell Cultures. PLoS One. 2015 Nov 16;10(11):e0142124.
- [2] Hoch L, et al. MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. FASEB J. 2015 May;29(5):1817-29.
- [3] Ma W, et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246.