PD168393

目录号: HY-13896 纯度: 98.58%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

PD168393 是有效、选择性和细胞渗透性的 EGFR 酪氨酸激酶 (EGFR tyrosine kinase) 和 ErbB2 的抑制剂。PD168393 不可逆转地失活 EGF 受体 (IC₅₀=0.7 nM)，但对胰岛素受体、PDGFR、FGFR 和 PKC 无作用。

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PD168393 Chemical Structure

CAS No. : 194423-15-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥625	In-stock
2 mg	￥550	In-stock
5 mg	￥770	In-stock
10 mg	￥1300	In-stock
25 mg	￥2600	In-stock
50 mg	￥4600	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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MCE 顾客使用本产品发表的 2 篇科研文献

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

生物活性
纯度 & 产品资料
参考文献

生物活性

PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC₅₀=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC^[1].

IC₅₀ & Target^[1]

EGFR

0.7 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.012 μM Compound: 2, PD-168393	Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by Western blot Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by Western blot	[PMID: 20151670]
A-431	IC₅₀	0.036 μM Compound: PD168393	Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA	[PMID: 27135370]
A-431	IC₅₀	0.152 μM Compound: 2, PD-168393	Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot	[PMID: 20151670]
A-431	IC₅₀	1.96 μM Compound: PD168393	Antiproliferative activity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 27135370]
A-431	IC₅₀	1.96 μM Compound: 3, PD-168393	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay Antiproliferative activity against human A431 cells after 72 hrs by MTT assay	[PMID: 17154492]
A-431	IC₅₀	2.7 nM Compound: 3	Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting	[PMID: 10753475]
A549	IC₅₀	17.9 nM Compound: 2, PD168393	Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western blot analysis Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western blot analysis	[PMID: 23988354]
A549	IC₅₀	3.94 nM Compound: 2, PD168393	Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot analysis Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot analysis	[PMID: 23988354]
BaF3	GI₅₀	< 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	< 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	< 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	< 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	< 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	< 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	< 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	> 0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
NCI-H1975	IC₅₀	0.028 μM Compound: I	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as inhibition of EGF-mediated autophosphorylation incubated for 30 mins prior to EGF challenge by cytoblot assay Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as inhibition of EGF-mediated autophosphorylation incubated for 30 mins prior to EGF challenge by cytoblot assay	10.1039/C3MD00118K
NCI-H1975	IC₅₀	0.44 μM Compound: I	Cytotoxicity against gefitinib-resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay Cytotoxicity against gefitinib-resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay	10.1039/C3MD00118K
NCI-H1975	IC₅₀	0.61 μM Compound: 2, PD-168393	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 20151670]
Sf9	IC₅₀	< 0.001 μM Compound: 2, PD-168393	Inhibition of human recombinant EGFR expressed in baculovirus-infected Sf9 cells by radioactive phosphotransfer assay Inhibition of human recombinant EGFR expressed in baculovirus-infected Sf9 cells by radioactive phosphotransfer assay	[PMID: 17334377]
SK-BR-3	IC₅₀	0.015 μM Compound: 2	Inhibition of cell growth of SKBr3 cell lines using cell-based assay Inhibition of cell growth of SKBr3 cell lines using cell-based assay	[PMID: 11495584]
SK-BR-3	IC₅₀	0.2 μM Compound: I	Cytotoxicity against human SKBR3 cells expressing wild type EGFR assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay Cytotoxicity against human SKBR3 cells expressing wild type EGFR assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay	10.1039/C3MD00118K
SW-620	IC₅₀	4.133 μM Compound: 2	Inhibition of cell growth of SW620 cell lines using cell-based assay Inhibition of cell growth of SW620 cell lines using cell-based assay	[PMID: 11495584]
SW-620	IC₅₀	8.23 μM Compound: 2, PD-168393	Cytotoxicity against human SW620 cells after 72 hrs by MTT assay Cytotoxicity against human SW620 cells after 72 hrs by MTT assay	[PMID: 20151670]

体外研究
(In Vitro)

PD168393 inhibits ligand-dependent receptor phosphorylation and inhibits EGF-induced tyrosine phosphorylation in A431 cells and Heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC₅₀ values of 4.3 nM and 5.7 nM, respectively^[1].

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

体内研究
(In Vivo)

PD168393 (intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28) is effective in vivo, and produces tumor growth inhibition of 115% after 15 days’ treatment in human epidermoid carcinoma xenografts in mice^[1].

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

Animal Model:	A431 human epidermoid carcinoma grown as a xenograft in nude mice^[1]
Dosage:	58 mg/kg
Administration:	Intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28
Result:	Suppressed the growth of human epidermoid carcinoma xenografts.

分子量

369.22

Formula

C₁₇H₁₃BrN₄O

CAS 号

194423-15-9

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 30 mg/mL (81.25 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	2.7084 mL	13.5421 mL	27.0841 mL
5 mM	0.5417 mL	2.7084 mL	5.4168 mL
10 mM	0.2708 mL	1.3542 mL	2.7084 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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 (6.77 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。
以 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。

以下溶解方案，请直接配制工作液。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： 50% PEG300 50% Saline
Solubility: 3.33 mg/mL (9.02 mM); 悬浊液; 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

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.58%

选择批次：

Data Sheet (628 KB) SDS (392 KB)

COA (288 KB) LCMS (102 KB)

产品使用指南 (1538 KB)

参考文献

[1]. D W Fry, et al. Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7. [Content Brief]

PD168393 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7084 mL	13.5421 mL	27.0841 mL	67.7103 mL
	5 mM	0.5417 mL	2.7084 mL	5.4168 mL	13.5421 mL
	10 mM	0.2708 mL	1.3542 mL	2.7084 mL	6.7710 mL
	15 mM	0.1806 mL	0.9028 mL	1.8056 mL	4.5140 mL
	20 mM	0.1354 mL	0.6771 mL	1.3542 mL	3.3855 mL
	25 mM	0.1083 mL	0.5417 mL	1.0834 mL	2.7084 mL
	30 mM	0.0903 mL	0.4514 mL	0.9028 mL	2.2570 mL
	40 mM	0.0677 mL	0.3386 mL	0.6771 mL	1.6928 mL
	50 mM	0.0542 mL	0.2708 mL	0.5417 mL	1.3542 mL
	60 mM	0.0451 mL	0.2257 mL	0.4514 mL	1.1285 mL
	80 mM	0.0339 mL	0.1693 mL	0.3386 mL	0.8464 mL

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.

Keywords:

PD168393194423-15-9PD 168393PD-168393EGFRAutophagyApoptosisEpidermal growth factor receptorErbB-1HER1MDA-MB-453tumor epidermoid carcinomaPDGFRFGFRInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

PD168393

Customer Review

MCE 顾客使用本产品发表的 2 篇科研文献