PP58|cas:212391-58-7|西域试剂

PP58,99.48%

产品编号：Bellancom-18622| CAS NO：212391-58-7| 分子式：C₂₂H₁₉Cl₂N₅O₂| 分子量：456.32

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18622	￥1150.00	杭州北京（现货）
Bellancom-18622	￥1800.00	杭州北京（现货）
Bellancom-18622	￥4900.00	杭州北京（现货）

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PP58

产品介绍

PP58是吡啶[2,3-d]嘧啶化合物，抑制PDGFR，FGFR和Src家族活性的IC₅₀值在纳摩尔级。

生物活性

PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC₅₀ values.

体外研究

PP58 inhibits Src with a subnanomolar IC₅₀ value in the assays. PP58 behaves as a titration reagent at higher Src protein concentrations. As analyzed by immunoblotting with specific antiserum, the PP58 matrix specifically depletes Src from total lysate, whereas binding to the PP58 beads is prevented when free inhibitor is included. The ectopically expressed FGFR1 receptor tyrosine kinase is specifically retained on PP58 beads. PP58 matrix could be a novel affinity reagent for the purification of cellular pyrido[2,3-d]pyrimidine inhibitor targets. PP58 affinity chromatography leads to the identification of protein kinases belonging to various different groups and families, indicating that the pyrido[2,3-d]pyrimidine inhibitor is not selective for a set of phylogenetically related members of the human kinome. The K_i values of PP58 for p38α and JNK2 are 3.8±1.9 nM and 0.32±0.04 μM, respectively. PP58 affinity matrix also serves as an efficient purification reagent for a variety of protein kinases, which lack this structural feature and have much lower affinities for the pyrido[2,3-d]pyrimidine inhibitor PP58. PP58 inhibits anisomycin activated p38 in a dose-dependent manner with an IC₅₀ below 10 nM. LPS-stimulated TNF-α production is potently inhibited by PP58 with a cellular IC₅₀ value of around 3 nM. The T341M mutation abrogates the sensitivity to PP58 inhibition by increasing the cellular IC₅₀ value of about 10 nM by more than 1000-fold. The cellular wild-type FGFR1 activity is potently inhibited by low nanomolar concentrations of PP58, whereas dramatic resistance formation is detected for the FGFR1-V561M mutant. PP58 inhibits CSK activity with an IC₅₀ value of around 100 nM.

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

体内研究

PP58 can exhibit some degree of selectivity at low nanomolar concentrations in vivo.

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

体内研究

PP58 can exhibit some degree of selectivity at low nanomolar concentrations in vivo.

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (136.97 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1914 mL	10.9572 mL	21.9144 mL
5 mM	0.4383 mL	2.1914 mL	4.3829 mL
10 mM	0.2191 mL	1.0957 mL	2.1914 mL

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。-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。

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

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (4.56 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.56 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明