PRT062607 (P505-15) HCl - 10mM in DMSO , CAS No.1370261-97-4

CAS: 1370261-97-4 Cat. No.: P408611 Peso molecular: 429.91 PubChem CID: 56948527

GRADE & PURITY 10mM in DMSO

Synonyms

BIIB057, PRT-2607 | 5-Pyrimidinecarboxamide, 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-, hydrochloride (1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.

In vitro

PRT062607(P505-15) anti-SYK activity is at least 80-fold greater than its affinity for other kinases. at least 80-fold greater than its affinity for other kinases. PRT062607 potently inhibits 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). PRT062607 inhibits 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. PRT062607 furthermore inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.

In vivo

The pharmacokinetic/pharmacodynamic relationship predicted that 70% Syk suppression is maintained in mice over a 24h period after 30 mg/kg dosing. At 15 mg/kg, Syk inhibition ranges from 7.5% (Cmin) to 78.4% (Cmax) with an average inhibition of 67% over 24 h. Oral administration of PRT062607 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. Statistically significant efficacy is observed at concentrations that specifically suppressed Syk activity by 67%.

Cell Data

cell lines：Calu-3 and A-549 cell lines

Concentrations：~6 μM

Incubation Time：3 days

Powder Purity:≥98%

Specifications

Sinónimos

BIIB057, PRT-2607 | 5-Pyrimidinecarboxamide, 2-[[(1R, 2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1, 2, 3-triazol-2-yl)phenyl]amino]-, hydrochloride (1:1)

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Nombres e identificadores

• Isómeros SMILES: C1CC[C@H]([C@H](C1)N)NC2=NC=C(C(=N2)NC3=CC(=CC=C3)N4N=CC=N4)C(=O)N.Cl
• CAS alternativo: 1370261-96-3
• PubChem CID: 56948527
• Peso molecular: 429.91