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PRT062607

CAS No. : 1370261-96-3

Biological Activity：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].

Research Area：Inflammation/Immunology

Targets：Syk

Related Small Molecules:Lanraplenib monosuccinate;OXSI-2;SYK/JAK-IN-1;PRT062607 Hydrochloride;MNS;TAK-659 hydrochloride;Syk Inhibitor II dihydrochloride dihydrate;Fostamatinib-d9;R406 free base;Fostamatinib Disodium;GSK2646264;Cevidoplenib;TAS05567;Midostaurin-d5;BAY 61-3606 dihydrochloride;Syk Kinase Peptide Substrate;Entospletinib;Gusacitinib;SRX3207;R112;Cerdulatinib;Syk-IN-3;GSK143 dihydrochloride

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