PP58 - CAS:212391-58-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	PP58
英文名称:	PP58
别名:	2-((4-(2-氨基乙氧基)苯基)氨基)-6-(2,6-二氯苯基)-8-甲基吡啶并[2,3-d]嘧啶-7(8H)-酮 2-aminopyrido[2,3-d]pyrimidin-7(8H)-one 58
CAS No:	212391-58-7	分子式:	C₂₂H₁₉Cl₂N₅O₂	分子量:	456.327
CAS No:	212391-58-7
分子式:	C₂₂H₁₉Cl₂N₅O₂
分子量:	456.327

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P11589 PP58 ≥98% (psaitong)

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包装规格：

5mg 25mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO（5mg/mL超声）

产品描述：

基本信息

产品编号：P11589
产品名称：PP58
CAS:	212391-58-7	储存条件	粉末	-20℃	四年

分子式：	C22H19Cl2N5O2		溶于液体	-80℃	六个月
分子量	456.33			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO
		Ethanol
		Water
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.1914mL	10.9572mL	21.9144mL
5mM	0.4383mL	0.4383mL	4.3829mL
10mM	0.2191mL	1.0957mL	2.1914mL

生物活性

产品描述	一种吡啶[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。
靶点/IC₅₀	PDGFR
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 Ki values of PP58 for p38α and JNK2 are 3.8±1.9nM and 0.32±0.04μM, 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 10nM. LPSstimulated TNF-αproduction is potently inhibited by PP58 with a cellular IC50 value of around 3nM. The T341M mutation abrogates the sensitivity to PP58 inhibition by increasing the cellular IC50 value of about 10nM 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 100nM.
体内研究	与没有经过Pazopanib或者仅用10mg/kg的Pazopanib治疗的小鼠相比，经过30mg/kg或者100mg/kg Pazopanib治疗的小鼠其肿瘤症状明显减轻。Pazopanib治疗耐受性良好，各组小鼠之间体重没有发生明显差异。
特征	PP58 can exhibit some degree of selectivity at low nanomolar concentrations in vivo.

推荐实验方法(仅供参考)

激酶实验：

MEK1 and Aurora A activities are tested at 37 ℃in a total volume of 30μL. The kinases are assayed using 50μM ATP and 1μ Ci [γ-32P]ATP in the presence of different PP58 concentrations. Kinase substrate proteins included are 0.25mg/mL inactive GST-ERK2 for MEK1 and 0.025mg/mL kemptide for Aurora A,respectively. Reactions are stopped by addition of SDS sample buffer. Determination of IC50 [0–100%] values is performed using GraFit software.

保存条件：

-20℃

UN码：

HazardClass：

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安全说明：

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