FRAX597

SKU: orb1301151

Description

FRAX597 is a potent and selective ATP-competitive inhibitor of group I p21-activated kinases (PAKs), demonstrating high inhibitory activity against PAK1, PAK2, and PAK3. This small molecule is a valuable research tool for studying PAK signaling in cancer cell proliferation, invasion, and in vivo tumor models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1286739-19-2
• MW: 558.1
• Purity: 99.94% (May vary between batches)
• Formula: C₂₉H₂₈ClN₇OS
• SMILES: CCn1c2nc(Nc3ccc(cc3)N3CCN(C)CC3)ncc2cc(-c2ccc(cc2Cl)-c2cncs2)c1=O
• Target: PAK
• Solubility: DMSO:13.06 mg/mL (23.4 mM)

Bioactivity

• Target IC50:
  PAK3:19 nM|PAK1:8 nM|PAK2:13 nM
• In Vivo:
  FRAX597 exhibits potent inhibition against wild-type PAK1 (IC50=48 nM), whereas it shows significantly reduced efficacy against the V342F PAK1 mutation (IC50 > 3 μM) and the V342Y PAK1 mutation (IC50 > 2 μM). At a concentration of 100 nM, FRAX597 demonstrates substantial inhibitory effects on YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%).
• In Vitro:
  In NOD/SCID mice loaded with Nf2-/-SC4 Schwann cells, daily oral administration of FRAX597 (100 mg/kg) significantly inhibits tumor growth. Similarly, in SCID mice with intrinsic meningiomas, daily oral intake of FRAX597 (90 mg/kg) markedly suppresses tumor growth. Additionally, in KrasG12D mice, daily treatment with FRAX597 (90 mg/kg) leads to tumor regression and a decrease in Erk and Akt activity.
• Cell Research:
  30,000 cells/well are plated in 12-well dishes in triplicate. Cell growth media with or without FRAX597 is replaced daily. At indicated time points, cells from individual wells are trypsinized and counted using a Coulter counter.(Only for Reference)

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

FRAX 597, FRAX597, FRAX-597, Inhibitor, p21 activated kinases, inhibit, PAK3, PAK2, PAK, PAK1

Compound Identifiers

PubChem CID

70934541