PP58

CAS: 212391-58-7 货号: P656000 分子式: C22H19Cl2N5O2 分子量: 456.32
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
P656000-1ml
期货 Stock Image
¥339.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR , FGFR and Src family activities with nanomolar IC 50 values.

In Vitro

PP58 inhibits Src with a subnanomolar IC 50 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 IC 50 below 10 nM. LPS-stimulated TNF-α production is potently inhibited by PP58 with a cellular IC 50 value of around 3 nM. The T341M mutation abrogates the sensitivity to PP58 inhibition by increasing the cellular IC 50 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 IC 50 value of around 100 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PP58 can exhibit some degree of selectivity at low nanomolar concentrations in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:PDGFR

规格

规格或纯度
10mM in DMSO
英文名称
PP58
生化机理
PP58 是一种吡啶并[2,3-d]嘧啶类化合物,可抑制表皮生长因子受体、表皮生长因子受体和 Src 家族的活性,其 IC 50 值为纳摩尔级。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=CC=C3Cl)Cl)NC4=CC=C(C=C4)OCCN
分子量
456.32

技术文档

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🔬 规格说明书

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高级数据

质检证书(CoA,COO,BSE/TSE 和分析图谱)
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常见问题

本产品应如何储存?
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输?
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包,并按上述储存条件保存;处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 212391-58-7,分子式为 C22H19Cl2N5O2,分子量为 456.32 g/mol。
如何获取批次专用COA?
每个订单都会随附分析证书(COA),您也可以从账户订单历史中下载。如需订购前的COA,请联系您的客户代表,或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。