ARN25499 | Cdc42 GTPase interaction inhibitor

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5 mg$75.00
25 mg$275.00
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ARN25499 is a novel Cdc42 GTPase interaction inhibitor.  It inhibits the interaction between Cdc42 and its downstream effectors (i.e PAK) instead of the Cdc42-GEF interaction.  ARN25499 displayed activity against four melanoma cancer cell lines (IC50s: SKM28 13.5 µM, SKMeI3 8.1 µM, WM3248 12.8 µM, A375 9.7 µM) and one colon cancer line (IC50 = 11.2 µM SW480).  It also displayed good pharmacokinetics in mice. ARN25499 also showed in vivo efficacy in melanoma PDX tumors in NSG mice @ 10mg/kg.

References/Citations:

  1. Brindani et al. (2024), Discovery of CDC42 Inhibitors with a Favorable Pharmacokinetic Profile and Anticancer In Vivo Efficacy; J. Med. Chem. 67 10401
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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

ARN25499 is a novel Cdc42 GTPase interaction inhibitor.  It inhibits the interaction between Cdc42 and its downstream effectors (i.e PAK) instead of the Cdc42-GEF interaction.  ARN25499 displayed activity against four melanoma cancer cell lines (IC50s: SKM28 13.5 µM, SKMeI3 8.1 µM, WM3248 12.8 µM, A375 9.7 µM) and one colon cancer line (IC50 = 11.2 µM SW480).  It also displayed good pharmacokinetics in mice. ARN25499 also showed in vivo efficacy in melanoma PDX tumors in NSG mice @ 10mg/kg.

References/Citations:

  1. Brindani et al. (2024), Discovery of CDC42 Inhibitors with a Favorable Pharmacokinetic Profile and Anticancer In Vivo Efficacy; J. Med. Chem. 67 10401