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GPCR/G Protein Hedgehog/Smoothened Taladegib

Taladegib

Catalog No. T2666   CAS 1258861-20-9
Synonyms: LY2940680

Taladegib is an orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity.

Taladegib, CAS 1258861-20-9
Pack Size Availability Price/USD Quantity
2 mg In stock 74.00
5 mg In stock 104.00
10 mg In stock 162.00
50 mg In stock 446.00
100 mg In stock 770.00
1 mL * 10 mM (in DMSO) In stock 116.00
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Purity 100.00%
Purity 98.75%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Taladegib is an orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity.
Targets&IC50 Smoothened
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 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]
Synonyms LY2940680
Purity 100.00%
Molecular Weight 512.5
Formula C26H24F4N6O
CAS No. 1258861-20-9

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Redmond EM et al. Expert Opin Investig Drugs, 2011, 20(12),1649-1664. 2. Mark H. Bender, Cancer Research, 2011, Volume 71, Issue 8, Supplement1 3. 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. 4. 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.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library Clinical Compound Library Anti-cancer Clinical Compound Library Wnt&Hedgehog&Notch Compound Library

Related Products

Related compounds with same targets
Glasdegib ALLO-2 GANT 58 SAG hydrochloride (912545-86-9(free base)) JK184 Taladegib BMS833923 NVP-LDE225

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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.