PRT062607 (P505-15, BIIB057) HCl
PRT062607 (P505-15, BIIB057) HCl
CAS: 1370261-97-4
Molecular Formula: C19H24ClN9O
PRT062607 (P505-15, BIIB057) HCl - Names and Identifiers
PRT062607 (P505-15, BIIB057) HCl - Physico-chemical Properties
| Molecular Formula | C19H24ClN9O |
| Molar Mass | 429.90656 |
| Solubility | DMSO 86 mg/mL Water 86 mg/mL Ethanol <1 mg/mL |
| Storage Condition | -20℃ |
| MDL | MFCD25976708 |
| In vitro study | PRT062607(P505-15) has anti-SYK activity with at least 80-fold higher affinity than other kinases. PRT062607 effectively inhibits B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μm, respectively), and effectively inhibit the degranulation of basophils mediated by Fc epsilon receptor 1 (IC50 is 0.15 μM). PRT062607 acts on CLL cells, inhibits the secretion of BCR-dependent chemokines CCL3 and CCL4, and inhibits the migration of leukemia cells to tissue homing chemokines CXCL12,CXCL13, and below interstitial cells. After triggering BCR, PRT062607 further inhibits the phosphorylation of Syk and extracellular signal-regulated kinase. |
| In vivo study | The pharmacokinetic/pharmacodynamic relationship showed that Syk inhibition was maintained at 70% during the 24 h treatment of mice at a dose of 30 mg/kg. At a dose of 15 mg/kg for 24 hours, inhibition Syk ranged from 7.5 (C min) to 78.4 (C max) with a mean inhibition of 67%. Oral treatment of PRT062607 in two rodent models of rheumatoid arthritis produced anti-inflammatory activity in a dose-dependent manner. A statistically significant effect was observed at a concentration that specifically inhibited Syk activity by 67%. |
PRT062607 (P505-15, BIIB057) HCl - Introduction
PRT062607 (P505-15, BIIB057) HCl is a novel, highly selective Syk inhibitor with an IC50 of 1 nM, acting on Syk is more than 80 times more selective than acting on Fgr, Lyn, FAK, Pyk2 and Zap70.
Last Update：2022-10-16 17:41:26
PRT062607 (P505-15, BIIB057) HCl - Reference Information
| biological activity | PRT062607 (P505-15, BIIB057, PRT-2607) is a new type of highly selective Syk inhibitor. IC50 is 1 nM in cell-free test, and the selectivity for Syk is more than 80 times higher than that for Fgr,PAK5,Lyn,FAK,Pyk2, FLT3, MLK1 and Zap70. |
| Target | Value |
| Syk (Cell-free assay) | 1 nM |
| FGR (Cell-free assay) | 81 nM |
| MLK1 (Cell-free assay) | 88 nM |
| PYK2 (Cell-free assay) | 108 nM |
| YES (Cell-free assay) | 123 nM |
Last Update：2024-04-09 22:09:11
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Product Name: PRT062607 (P505-15, BIIB057) HCl Visit Supplier Webpage Request for quotationCAS: 1370261-97-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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