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Taladegib (LY2940680) is an orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
5 mg | $56 | In Stock | |
10 mg | $87 | In Stock | |
25 mg | $151 | In Stock | |
50 mg | $241 | In Stock | |
100 mg | $358 | In Stock | |
200 mg | $497 | In Stock |
Description | Taladegib (LY2940680) is an orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity. |
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 | Taladegib has excellent pharmacokinetic properties in rodent and non-rodent species. Taladegib administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. Taladegib reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and Taladegib induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. Taladegib inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. [2] |
Alias | LY2940680 |
Molecular Weight | 512.5 |
Formula | C26H24F4N6O |
Cas No. | 1258861-20-9 |
Smiles | CN(C1CCN(CC1)c1nnc(-c2ccnn2C)c2ccccc12)C(=O)c1ccc(F)cc1C(F)(F)F |
Relative Density. | 1.39 g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 5.64 mg/mL (11 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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