PF-3758309

SKU: orb1300605

Description

PF-3758309

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 898044-15-0
• MW: 490.62
• Purity: 99.37%
• Formula: C₂₅H₃₀N₈OS
• SMILES: CN(C)C[C@@H](NC(=O)N1Cc2c(Nc3nc(C)nc4ccsc34)n[nH]c2C1(C)C)c1ccccc1
• Target: Apoptosis,PAK
• Solubility: DMSO:91 mg/mL (185.48 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.73 mM);Ethanol:91 mg/mL (185.48 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PAK2:190 nM|PAK1:13.7 nM (Ki)|PAK4:1.3 nM|PAK4:18.7 nM(Ki)|PAK3:99 nM|PAK6:17.1 nM(Ki)|PAK5:18.1 nM(Ki)
• In Vivo:
  In the HCT116 tumor model, PF-3758309 act as an antiproliferative inducing apoptosis. In the sensitive model, PF-3758309 (EC50=0.4 nM) blocks the growth of multiple human tumor xenografts.
• In Vitro:
  PF-3758309 (Kd = 2.7 nM), an effective inhibitor of PAK4 （Ki=18.7 nM）, has ATP competition. PF-3758309 (IC50 = 1.3 nM) inhibits phosphorylation of the PAK4 substrate GEF-H1 in cells. In the tumor cell, PF-3758309(IC50 = 4.7 nM) grows in a linesanchorage-independent manner. In HCT116 cells, PF-3758309 inhibits endogenous pGEF-H1 accumulation. In A549 cells, PF-3758309 effectively inhibits cellular proliferation in IC50 of 20 nM and anchorage-independent growth in IC50 of 27 nM.
• Cell Research:
  HEK293T, HCT116, and SKOV3 cells are plated on 384-well plates for 24 hours culture. PF-3758309( ~1 μM) is added to the cell culture incubating 72 hours. After drug treatment,cell proliferation and other indicators of metabolism are measured.
• Animal Research:
  Nude mice with Xenograft tumors were orally fed with PF-3758309（7.5-30 mg/kg BID）dissolved in 0.5% methylcellulose.

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

Apoptosis, ATP-competitive, oncogenic, PAK, PAK1, PAK3, PAK4, PAK6, PAK5, inhibit, Inhibitor, growth, proliferation, survival, p21 activated kinases, PF03758309, PF-03758309, PF309, PF-309, PF3758309, PF-3758309, PF 3758309, PF 309, PF 03758309, signaling, tumor

Compound Identifiers

PubChem CID

25227462