YAP/TAZ inhibitor-2

SKU: orb1689775

Description

YAP/TAZ inhibitor-2 is a potent, orally bioavailable small molecule that disrupts the TEAD-YAP/TAZ interaction with an EC50 of 3 nM. It demonstrates robust anti-proliferative effects in cellular assays and has shown promising antitumor activity in vivo, making it a valuable chemical probe for Hippo pathway and cancer research.

Research Area

Cancer Biology; Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2762617-31-0
• MW: 390.33
• Purity: 98.84% (May vary between batches)
• Formula: C₁₉H₁₄F₄N₄O
• SMILES: FC(=C)C(=O)N1CC(C1)n1nc(-c2ccc(cc2)C(F)(F)F)c2cccnc12
• Target: YAP
• Solubility: DMSO:90 mg/mL (230.57 mM)

Bioactivity

• In Vivo:
  YAP/TAZ inhibitor-2 (0.5, 2, 5, 50 mg/kg; p.o.; daily for 28 days) exhibits anti-tumor activity without significant body weight loss during the treatment in BALB/c nude mice (NCI-H226 xenograft model) .
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• In Vitro:
  YAP/TAZ inhibitor-2 (compound 5) exhibits antiproliferative activity in NCI-H226 cells, with an IC50 value of 5.33 nM over 24 hours at concentrations ranging from 0 to 20000 nM .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YAP/TAZ inhibitor-2, YAP/TAZinhibitor2 , YAP–TEAD

Compound Identifiers

PubChem CID

164885340