PP121 - CAS:1092788-83-4 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	PP121
英文名称:	PP121
别名:	1-环戊基-3-(1H-吡咯并[2,3-b]吡啶-5-基)-1H-吡唑并[3,4-d]嘧啶-4-胺;PP121 抑制剂;Wright 亚甲蓝试剂;桑色素.桑黄素 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS No:	1092788-83-4	分子式:	C₁₇H₁₇N₇	分子量:	319.36
CAS No:	1092788-83-4
分子式:	C₁₇H₁₇N₇
分子量:	319.36

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

P10814 PP121 ≥98% (psaitong)

相关产品

包装规格：

5mg 10mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO（20 mg/mL 超声）

产品描述：

基本信息

产品编号：	P10814
产品名称：	PP121
CAS:	1092788-83-4	储存条件	粉末	-20℃	四年

分子式：	C17H17N7		溶于液体	-80℃	6个月
分子量：	319.36			-20℃	1个月
化学名：	PP121;1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Solubility (25°C)：
体外:	DMSO	64mg/mL (200.4mM)
	Ethanol	Insoluble
	Water	Insoluble
体内(现配现用):	1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2mg/mL(6.26mM);Clear solution
	此方案可获得 ≥ 2 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
	2.请依序添加每种溶剂：10% DMSO→90%(20% SBE-β-CD in saline) Solubility:≥2mg/mL(6.26mM);Clear solution
	此方案可获得 ≥ 2 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.0 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。
	3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2mg/mL(6.26mM);Clear solution
	此方案可获得 ≥ 2 mg/mL (6.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
＜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	3.1313mL	15.6563mL	31.3126mL
5mM	0.6263mL	3.1313mL	6.2625mL
10mM	0.3131mL	1.5656mL	3.1313mL

生物活性

产品描述	是多靶点激酶抑制剂，抑制mTOR，DNK-PK，VEGFR2，Src，PDGFR的IC50值分别为10，60，12，14，2nM。
靶点	mTOR;PDGFR;VEGFR;Src;Apoptosis
体外研究	PP121 blocks the PI3K pathway by direct inhibition of PI3K/mTOR in two glioblastoma cell lines,U87 and LN229.PP121 potently inhibits the proliferation of a diverse panel of tumor cell lines containing mutations in the PI3-K pathway components PIK3CA,PTEN,or RAS.PP121 induces a G0G1 arrest in most tumor cells.PP121 directly inhibits Src in cells and reverses its biochemical and morphological effects.PP121 potently inhibits the Ret kinase domain in vitro (IC50<1nM).PP121 potently blocks VEGF stimulated activation of the PI3-K and MAPK pathways.PP121 inhibits VEGFR2 autophosphorylation at low nanomolar concentrations,confirming that this molecule directly targets VEGFR2 in cells.PP121 inhibits Bcr-Abl induced tyrosine phosphorylation in K562 cells as well as BaF3 cells that express Bcr-Abl.
体内研究	Oral administration of PP121 remarkably inhibits Eca-109 xenograft growth.Mice body weights are not significantly affected by PP121 or the vehicle treatment.PP121 oral administration dramatically inhibits activations of Akt-mTOR and NFkB in xenograft tumors.p-Akt Ser 473 and p-IKKa/b are both inhibited by PP121 administration.

推荐实验方法(仅供参考)

激酶实验：

Purified kinase domains are incubated with inhibitors (PP121) at 2-or 4-fold dilutions over a concentration range of 50-0.001µM or with vehicle (0.1% DMSO) in the presence of 10µM ATP,2.5µCi of γ- 32P-ATP and substrate.Reactions are terminated by spotting onto nitrocellulose or phosphocellulose membranes,depending on the substrate;this membrane is then washed 5-6 times to remove unbound radioactivity and dried.Transferred radioactivity is quantitated by phosphorimaging and IC50 values are calculated by fitting the data to a sigmoidal doseresponse using Prism software.

细胞实验:

Cells grown in 96-well plates are treated with PP121 at 4-fold dilutions (10µM-0.040μM) or vehicle (0.1% DMSO).After 72h cells are exposed to Resazurin sodium salt (22µM) and fluorescence is quantified.IC50 values are calculated.For proliferation assays involving single cell counting,non-adherent cells are plated at low density (3–5% confluence) and treated with drug (2.5µM) or vehicle (0.1% DMSO).Cells are diluted into trypan blue daily and viable cells counted using a hemocytometer.

动物实验:
Mice:Eca-109 cells are injected into the axillary regions of nude mice (5×106 cells/mouse).When the tumor volumes reach around 200 mm3,the mice are randomly separated to three groups:Untreated control,PP121 (30mg/kg) and vehicle (10% 1-methyl-2-pyrrolidinone and 90% PEG 300) group.Tumor volumes and the mice body weights are measured every 10 d.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果