1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. PRT062607 Hydrochloride

PRT062607 Hydrochloride  (Synonyms: P505-15 Hydrochloride)

目录号: HY-15323 纯度: 98.68%
COA 产品使用指南

PRT062607 Hydrochloride (P505-15 Hydrochloride) 是一种有效的纯化的 Syk 抑制剂,IC50 为 1-2 nM。

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PRT062607 Hydrochloride Chemical Structure

PRT062607 Hydrochloride Chemical Structure

CAS No. : 1370261-97-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1377
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1 mg ¥569
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5 mg ¥1181
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10 mg ¥1841
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25 mg ¥3098
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50 mg ¥4647
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100 mg ¥6506
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRT062607 Hydrochloride (P505-15 Hydrochloride) is a highly specific and potent inhibitor of purified Syk (IC50 1-2 nM).

IC50 & Target

IC50: 1 nM (Syk), 81 nM (Fgr), 88 nM (MLK1), 123 nM (Yes)[1]

体外研究
(In Vitro)

PRT062607 (P505-15) is a novel, highly specific, and potent orally available small-molecule inhibitor of Syk. The potency of PRT062607 against its target kinase Syk is initially tested in two different purified kinase assays. Using a FRET assay, half-maximal Syk inhibition required 6±0.2 nM (mean±S.E.M.). Similar potency is observed when tested in a radioactive enzyme assay, with a resulting Syk IC50 of 2.1±0.4 nM (mean±S.E.M.). In human whole blood, PRT062607 potently inhibits 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)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In the mouse CAIA model, oral administration of PRT062607 (P505-15) results in an average inhibition of paw inflammation, as measured by daily scoring of inflammation compared with vehicle controls, of 12, 44, and 87% with average plasma concentration (C average over 24 h) assessed at the end of the study of 0.38, 0.95, and 1.47 μM, respectively. In mice treated with 30 mg/kg PRT062607, the damage to the joints is significantly reduced and seemed indistinguishable from normal mice. In the rat CIA model, the high dose of PRT062607 (15 mg/kg b.i.d.) completely suppresses inflammation in a majority of the animals (seven of eight), by the end of the study (mean inflammation score±S.E.M.=0.63±1.1; p<0.0001 versus vehicle)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

429.91

Formula

C19H24ClN9O

CAS 号
性状

固体

颜色

Light yellow to khaki

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O 中的溶解度 : ≥ 50 mg/mL (116.30 mM)

DMSO 中的溶解度 : ≥ 33 mg/mL (76.76 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3261 mL 11.6303 mL 23.2607 mL
5 mM 0.4652 mL 2.3261 mL 4.6521 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 50 mg/mL (116.30 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 98.68%

参考文献
Kinase Assay
[1]

Potency of Syk inhibition is determined by using a fluorescence resonance energy transfer (FRET) assay. The extent of substrate phosphorylation by Syk is measured in the presence of various PRT062607 (P505-15) concentrations. Syk activity is determined by a fluorescent antibody specific for phosphorylated tyrosine by using the increase of FRET. Twelve concentrations are tested for dose response. Specificity and potency of kinase inhibition is determined by evaluation of PRT062607 in the Kinase Profiler panel of 270 independent purified kinase assays. For profiling, PRT062607 is tested in duplicate at two concentrations at a fixed concentration of ATP. Subsequently, IC50 determinations using the radioactive assays are carried out at an ATP concentration optimized for each individual kinase. All radioactive ATP incorporation enzyme assays are performed[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

SUDHL4 cells (106 cells) are stimulated for 30 min with F(ab)′2 anti-human IgM antibody. Signaling is terminated by resuspending cells in ice-cold lysis buffer (50 mM Tris, pH 7.4, 150 mM NaCl, 0.5 mM EDTA, 1% nonidet P-40, and 0.5% sodium deoxycholate) containing freshly added protease and phosphatase inhibitor tablets. Protein lysates are resolved by SDS-polyacrylamide gel electrophoresis under reducing conditions and probed with the indicated antibodies. Secondary antibody conjugated to horseradish peroxidase and enhanced chemiluminescence detection reagent are used for the detection of specific protein. Where indicated, cells are pretreated for 1 h at 37°C with PRT062607 or vehicle control before stimulation. Densitometry of exposed films is performed by using the AlphaImager 2200. Ba/F3 cells are seeded at 5000 cells per well in a 384-well tissue culture plate containing media with various concentrations of PRT062607 or staurosporin. After 3 days, viability of cells is quantitated by CellTiter Glo following the manufacturer-supplied protocols[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Female BALB/c mice receive a single oral dose of 15 or 30 mg/kg PRT062607 and are anesthetized with a subcutaneous ketamine cocktail, and blood is 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 is 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 is processed for intracellular phospho-flow cytometry to evaluate BCR signaling as described earlier; mouse B cells are detected by using CD45R-B220 PerCP-conjugated antibody. Plasma samples are analyzed for PRT062607 concentration by using a liquid chromatography tandem mass spectrometer. The analytical range is 2 to 5000 ng/mL.
Rats[1]
Collagen-induced arthritis (CIA) is induced in female, 7-week old Lewis rats by subcutaneous injection of bovine collagen II emulsified with incomplete Freund's adjuvant at the base of the tail. On day 10, the rats are boosted with a second subcutaneous injection. PRT062607 administration is initiated when at least one hind paw is inflamed (inflammation score 1), and enrollment into a treatment group is designated as day 1 of the study for each individual animal (n=8/dose group). Progression of disease is evidenced by increased edema and erythema of one or both ankle joints, followed by the involvement of the metatarsal and interphalangeal joints. Fully developed arthritis is observed approximately 4 to 7 days after the onset of inflammation. Hind paws (sum of two paws) are scored daily for progression of inflammation. Inflammation scores for each paw are determined based on the following scale: 0, normal; 1, mild, but definite redness and swelling of the ankle possibly limited to individual digits; 2, moderate redness and swelling of ankle; 3, severe redness and swelling of the entire paw including digits; and 4, maximally inflamed limb with involvement of multiple joints. Ankle thickness measurements are obtained by a caliper device. At study termination, rats are anesthetized, and blood is harvested by cardiac puncture for complete blood counts and drug plasma concentration.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

PRT062607 Hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 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 1.1630 mL 2.3261 mL 5.8152 mL
15 mM 0.1551 mL 0.7754 mL 1.5507 mL 3.8768 mL
20 mM 0.1163 mL 0.5815 mL 1.1630 mL 2.9076 mL
25 mM 0.0930 mL 0.4652 mL 0.9304 mL 2.3261 mL
30 mM 0.0775 mL 0.3877 mL 0.7754 mL 1.9384 mL
40 mM 0.0582 mL 0.2908 mL 0.5815 mL 1.4538 mL
50 mM 0.0465 mL 0.2326 mL 0.4652 mL 1.1630 mL
60 mM 0.0388 mL 0.1938 mL 0.3877 mL 0.9692 mL
H2O 80 mM 0.0291 mL 0.1454 mL 0.2908 mL 0.7269 mL
100 mM 0.0233 mL 0.1163 mL 0.2326 mL 0.5815 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PRT062607 Hydrochloride
目录号:
HY-15323
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