Taladegib

SKU: orb1305194

Description

Taladegib (LY2940680) is a potent, orally active smoothened (Smo) antagonist that inhibits the Hedgehog signaling pathway. It is used in cancer research, demonstrating antitumor activity in both in vitro assays and in vivo models of Hedgehog pathway-dependent malignancies.

Research Area

Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1258861-20-9
• MW: 512.5
• Purity: 99.92%
• Formula: C₂₆H₂₄F₄N₆O
• SMILES: CN(C1CCN(CC1)c1nnc(-c2ccnn2C)c2ccccc12)C(=O)c1ccc(F)cc1C(F)(F)F
• Target: Hedgehog/Smoothened,Smo
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.95 mM);DMSO:5.64 mg/mL (11 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Hedgehog, inhibit, LY2940680, LY-2940680, LY 2940680, Smo, Smoothened, Taladegib

Compound Identifiers

PubChem CID

49848070