| 常用名 | R406(游离的) | CAS号 | 841290-80-0 |
|---|---|---|---|
| 价格 | 纯度 | 99.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情(用途,包装等)
用途: R406 is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. IC50 value: 41 nM [1]Target: Syk in vitro: R406 is a potent inhibitor of immunoglobulin E (IgE)- and IgG-mediated activation of Fc receptor signaling. R406 inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. R406 inhibits phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 binds to the ATP binding pocket of Syk and inhibits its kinase activity as an ATP-competitive inhibitor with Ki of 30 nM. R406 blocks Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and Bcr-mediated activation of B lymphocytes [1]. R406 significantly induces chronic lymphocytic leukemia (CLL) cell apoptosis in nurselike cells cocultures and blocks CCL3 and CCL4 secretion by CLL cells in response to B-cell antigen receptor (Bcr) triggering [2]. R406 is a potent inhibitor of platelet signaling and functions initiated by FcγRIIA cross-linking by specific antibodies or by sera from HIT patients [3].in vivo: R406 reduces cutaneous reverse passive Arthus reaction by approximately 86% at 5 mg/kg in prophylactic treated mice. R406 also shows efficacy in inhibiting paw inflammation in antibody-induced arthritis mouse models [1]. R406 does not adversely affect macrophage or neutrophil function in innate immune responses and has minimal functional immunotoxicity notwithstanding its lymphocytopenic effect [4]. 物理化学性质: CAS号:841290-80-0 常用中文名:R406(游离的) 常用英文名:R406 (free base) 分子式:C22H23FN6O5 分子量:470.454 密度:1.4±0.1 g/cm3 沸点:N/A 熔点:N/A 闪点:N/A 储存条件:-20°C |