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PRT062607 hydrochloride

产品编号 T2696Cas号 1370261-97-4
别名 PRT062607 (P505-15, BIIB057) HCl, P505-15 Hydrochloride

PRT062607 hydrochloride (P505-15 Hydrochloride) 是纯化的 Syk 抑制剂,IC50=1-2 nM。

PRT062607 hydrochloride

PRT062607 hydrochloride

纯度: 99.93%
产品编号 T2696 别名 PRT062607 (P505-15, BIIB057) HCl, P505-15 HydrochlorideCas号 1370261-97-4

PRT062607 hydrochloride (P505-15 Hydrochloride) 是纯化的 Syk 抑制剂,IC50=1-2 nM。

规格价格库存数量
1 mg¥ 453现货
5 mg¥ 945现货
10 mg¥ 1,520现货
25 mg¥ 2,560现货
50 mg¥ 3,850现货
100 mg¥ 5,390现货
200 mg¥ 7,360现货
500 mg¥ 10,900现货
1 mL x 10 mM (in DMSO)¥ 1,130现货
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纯度:99.93%
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产品介绍

生物活性
产品描述
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.
靶点活性
MLK1:88 nM (cell free), FGR:81 nM (cell free), Syk:1 nM (cell free)
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].
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].
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].
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].
别名PRT062607 (P505-15, BIIB057) HCl, P505-15 Hydrochloride
化学信息
分子量429.91
分子式C19H23N9O·HCl
CAS No.1370261-97-4
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 79 mg/mL (183.8 mM)
DMSO: 45 mg/mL (104.67 mM)
溶液配制表
DMSO/H2O
1mg5mg10mg50mg
1 mM2.3261 mL11.6303 mL23.2607 mL116.3034 mL
5 mM0.4652 mL2.3261 mL4.6521 mL23.2607 mL
10 mM0.2326 mL1.1630 mL2.3261 mL11.6303 mL
20 mM0.1163 mL0.5815 mL1.1630 mL5.8152 mL
50 mM0.0465 mL0.2326 mL0.4652 mL2.3261 mL
100 mM0.0233 mL0.1163 mL0.2326 mL1.1630 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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