1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. PRT062607

PRT062607 (Synonyms: P505-15; PRT-2607; BIIB-057)

Cat. No.: HY-15322
Handling Instructions

PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.

For research use only. We do not sell to patients.

PRT062607 Chemical Structure

PRT062607 Chemical Structure

CAS No. : 1370261-96-3

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Description

PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70. IC50 value: 1-2 nM [1] Target:Syk kinase inhibitor 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) [1]. P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL [2]. 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 [3]. 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 [1]. 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 [2].

Clinical Trial
Molecular Weight

393.45

Formula

C₁₉H₂₃N₉O

CAS No.

1370261-96-3

SMILES

NC(C1=CN=C(N[[email protected]]2[[email protected]@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PRT062607P505-15PRT-2607BIIB-057PRT 062607PRT-062607PRT2607PRT 2607BIIB057BIIB 057SykSpleen tyrosine kinaseInhibitorinhibitorinhibit

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PRT062607
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