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网站主页 化工产品目录 生物化工 抑制剂 血管生成(Angiogenesis) Syk 抑制剂 PRT062607 (HYDROCHLORIDE) 化合物 PRT062607 hydrochloride
  • 化合物 PRT062607 hydrochloride|T2696|TargetMol

化合物 PRT062607 hydrochloride|T2696|TargetMol

PRT062607 hydrochloride
1370261-97-4
272 1mg 起订
567 5mg 起订
912 10mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 PRT062607 hydrochloride
英文名称:
PRT062607 hydrochloride
CAS号:
1370261-97-4
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.93%
产品类别:
抑制剂
货号:
T2696

Product Introduction

Bioactivity

名称PRT062607 hydrochloride
描述PRT062607 hydrochloride (P505-15 Hydrochloride) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases.
细胞实验NLC co-cultures were established by suspending PBMC from patients with CLL in complete RPMI medium with 10% fetal bovine serum and penicillin-streptomycin-glutamine to a concentration of 107 cells/mL (total 2 mL). Cells were incubated for 14 days in 24-well plates as previously described. To evaluate whether the Syk inhibitors PRT318 and P505-15 could overcome the protective effect of NLC, CLL cells were cultured under standardized conditions on NLC or in suspension, in the presence or absence of PRT318 and P505-15. At the indicated time points, CLL cells were collected and assayed for cell viability as previously described [2].
激酶实验Potency of Syk inhibition was determined by using a fluorescence resonance energy transfer (FRET) assay. The extent of substrate phosphorylation by Syk was measured in the presence of various P505-15 concentrations. Syk activity was determined by a fluorescent antibody specific for phosphorylated tyrosine by using the increase of FRET. Twelve concentrations were tested for dose response. Specificity and potency of kinase inhibition was determined by evaluation of P505-15 in the Millipore KinaseProfiler panel of 270 independent purified kinase assays. For profiling, P505-15 was tested in duplicate at two concentrations at a fixed concentration of ATP. Subsequently, IC50 determinations using the radioactive assays were carried out at an ATP concentration optimized for each individual kinase. All radioactive ATP incorporation enzyme assays were performed at Millipore UK [1].
动物实验All animal studies were performed in strict accordance with the Institutional Animal Care and Use Committee ethical guidelines. Female BALB/c mice received a single oral dose of 15 or 30 mg/kg P505-15 and were anesthetized with a subcutaneous ketamine cocktail, and blood was harvested via cardiac puncture at 0.5, 1, 2, 3, 4, 5, 6, 8, and 24 h postdose, (n = 3/time point; n = 8 vehicle controls). Blood was dispensed into three heparin-containing tubes, one for determination of drug concentration and the remaining two for ex vivo stimulation with isotype control or anti-mouse IgD antibody for 10 min. Blood was processed for intracellular phospho-flow cytometry to evaluate BCR signaling as described earlier; mouse B cells were detected by using CD45R-B220 PerCP-conjugated antibody. Plasma samples were analyzed for P505-15 concentration by using a liquid chromatography tandem mass spectrometer. The analytical range was 2 to 5000 ng/ml [1].
体外活性PRT062607 (P505-15) is a highly specific and potent inhibitor of purified Syk (IC50 1-2 nM). 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). Similar levels of ex vivo inhibition were measured after dosing in mice (Syk signaling IC50 0.32 μM) [1]. P505-15 abrogated the pro-survival effect of anti-IgM and induced CLL cell apoptosis. Treatment with P505-15 (2 mM/mL) decreased CLL cell viability to 62.9 ± 5.1% after 48 hours. Treatment with lower concentrations of PRT318 and P505-15 also reduced the viability of CLL cells [2].
体内活性Demonstrating a rapid onset of action, 0.5 h after oral administration of 30 mg/kg P505-15, Syk activity was reduced by 80% and nearly completely suppressed for the next 5 h relative to vehicle control-treated mice. Syk activity remained more than 60% suppressed for the first 8 h postdosing, returning to levels of vehicle control treatment by 24 h. At the lower dose of 15 mg/kg, more than 50% suppression of Syk activity was observed between 2 and 6 h after oral administration of the compound [1].
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 79 mg/mL (183.8 mM)
DMSO : 45 mg/mL (104.67 mM)
关键字inhibit | PRT 062607 | PRT062607 | PRT-062607 | Inhibitor | Spleen tyrosine kinase | PRT-062607 hydrochloride | PRT062607 hydrochloride | PRT-062607 Hydrochloride | PRT062607 Hydrochloride | P505-15 | PRT 062607 Hydrochloride | Syk
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PRT062607 (P505-15, BIIB057) HCl|||P505-15 Hydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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