PF-3758309

SKU: orb1221674

Description

PF-03758309 (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.

Key Properties

• CAS Number: 898044-15-0
• MW: 490.62
• Purity: >98% (HPLC)
• Formula: C₂₅H₃₀N₈OS
• SMILES: CN(C)C[C@@H](NC(=O)N1Cc2c([nH]nc2Nc2nc(C)nc3c2scc3)C1(C)C)c1ccccc1
• Target: NMDAR
• Solubility: DMSO : ≥ 100 mg/mL; 203.82 mM

Bioactivity

• In Vivo:
  PF-3758309 (7.5-30 mg/kg; p.o. ; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models. Animal model: Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors). Dosage: 7.5-30 mg/kg. Administration: Oral administration; twice daily for 9-18 days. Result: Significant tumor growth inhibition (TGI) in HCT116 and A549 models.
• In Vitro:
  PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50 = 190 nM; PAK3, IC50 = 99 nM). In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM). PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50 = 20 nM) and anchorage-independent growth (IC50 = 27 nM) of A549 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

NMDAR