P505-15 Acetate

SKU: orb1702983

Description

P505-15 Acetate is a selective spleen tyrosine kinase (Syk) inhibitor that suppresses leukocyte function and inflammation. It is used in research to study autoimmune and inflammatory diseases, demonstrating efficacy in reducing arthritis scores and histological damage in in vivo models.

Research Area

Cardiovascular Research, Cell Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 1370261-98-5
• MW: 453.5
• Purity: 99.01% (May vary between batches)
• Formula: C₂₁H₂₇N₉O₃
• SMILES: CC(O)=O.N[C@H]1CCCC[C@H]1Nc1ncc(C(N)=O)c(Nc2cccc(c2)-n2nccn2)n1
• Target: Src,Syk,FAK,PYK2,Apoptosis,PAK,Tyrosinase,MLK
• Solubility: DMSO:10 mg/mL (22.05 mM)

Bioactivity

• Target IC50:
  Syk:1-2 nM|Lck:249 nM|PAK5:166 nM
• In Vivo:
  Similar levels of ex vivo inhibition were measured after dosing in mice (Syk signaling IC50 0.32 μM). Oral administration of P505-15 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis . Oral dosing in mice prevented BCR-mediated splenomegaly and significantly inhibited NHL tumor growth in a xenograft model. In addition, combination treatment of primary CLL cells with P505-15 plus fludarabine produced synergistic enhancement of activity at nanomolar concentrations .
• In Vitro:
  In human whole blood, P505-15 potently inhibited B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM) . P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL . PRT318 and P505-15 effectively antagonize CLL cell survival after BCR triggering and in nurse-like cell-co-cultures. Moreover, they inhibit BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT318 and P505-15 furthermore inhibit Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering .

Storage & Handling

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

Alternative Names

PRT 062607 Acetate, PRT062607 Acetate, PRT-062607 Acetate, P505 15 Acetate, P50515 Acetate, P-50515 Acetate, P505-15 Acetate, P 50515 Acetate, tyrosine kinase

Compound Identifiers

PubChem CID

56948400