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PRT062607 hydrochloride

产品编号 T2696 CAS 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。

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PRT062607 hydrochloride Chemical Structure

PRT062607 hydrochloride, CAS 1370261-97-4

规格	价格/CNY	货期
1 mg	￥ 454	现货
2 mg	￥ 639	现货
5 mg	￥ 945	现货
10 mg	￥ 1,542	现货
25 mg	￥ 2,995	现货
50 mg	￥ 3,950	现货
200 mg	￥ 7,890	现货
1 mL * 10 mM (in DMSO)	￥ 1,139	现货

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纯度: 99.93%

纯度: 97.7%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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	FGR:81 nM (cell free), MLK1:88 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
化合物与蛋白结合的复合物	JAK2 JH2 in complex with PRT062607
分子量	429.91
分子式	C19H23N9O·HCl
CAS No.	1370261-97-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 79 mg/mL (183.8 mM)

DMSO: 80 mg/mL (186.1 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O / DMSO	1 mM	2.3261 mL	11.6303 mL	23.2607 mL	58.1517 mL
	5 mM	0.4652 mL	2.3261 mL	4.6521 mL	11.6303 mL
	10 mM	0.2326 mL	1.163 mL	2.3261 mL	5.8152 mL
	20 mM	0.1163 mL	0.5815 mL	1.163 mL	2.9076 mL
	50 mM	0.0465 mL	0.2326 mL	0.4652 mL	1.163 mL
	100 mM	0.0233 mL	0.1163 mL	0.2326 mL	0.5815 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Coffey G, et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9. 2. Hoellenriegel J, et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

PRT062607 hydrochloride 1370261-97-4 Angiogenesis MAPK Tyrosine Kinase/Adaptors MLK Src Syk inhibit PRT 062607 PRT062607 PRT062607 (P505-15, BIIB057) HCl PRT-062607 Inhibitor Spleen tyrosine kinase PRT-062607 hydrochloride PRT-062607 Hydrochloride PRT062607 Hydrochloride P505-15 PRT 062607 Hydrochloride P505-15 Hydrochloride inhibitor

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PRT062607 hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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