Poziotinib (Synonyms: 波齐替尼; HM781-36B; NOV120101)

目录号: HY-15730 纯度: 99.96%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

HM781-36B 是一种口服活性，不可逆的泛 HER 抑制剂。HM781-36B 抑制 EGFR^wt、HER-2 和 HER-4 的 IC₅₀ 值分别为 3.2、5.3 和 23.5 nM，对突变的 EGFR，包括 EGFR^T790M 和 EGFR^L858R/T790M，IC₅₀ 值分别为 4.2 和 2.2 nM。具有良好的抗肿瘤活性。

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Poziotinib Chemical Structure

CAS No. : 1092364-38-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥860	In-stock
5 mg	￥800	In-stock
10 mg	￥1200	In-stock
50 mg	￥4200	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 8 篇科研文献

: Poziotinib purchased from MCE. Usage Cited in: Cancers (Basel). 2020 Nov 4;12(11):3249. [Abstract]; Poziotinib, at 0.1, 0.3 and 0.6 μM, produces a significant decrease in the expression level of the ABCG2 transporter protein in S1-M1-80 cells after 72 h of incubation, compared to cells incubated with vehicle (0 μM). ABCG2 protein expression is significantly decreased in S1-M1-80 cells following incubation with 0.6 µM of Poziotinib for 48 or 72 h.

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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

Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR^wt, HER-2 and HER-4 with IC₅₀s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR^T790M and EGFR^L858R/T790M, with IC₅₀s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity^[1]^[2].

IC₅₀ & Target

IC50: 3.2 nM (EGFR^wt), 5.3 nM (HER-2), 23.5 nM (HER-4) 4.2 nM (EGFR^T790M), 2.2 nM (EGFR^L858R/T790M)^[2]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	GI₅₀	0.654 μM Compound: Poziotinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	IC₅₀	0.9 nM Compound: 38; HM781e36B	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 72 hrs by MTS assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 72 hrs by MTS assay	[PMID: 28754471]
A-431	EC₅₀	1.445 μM Compound: Poziotinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	CC₅₀	31 nM Compound: Poziotinib	Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]
BaF3	GI₅₀	0.002 μM Compound: Poziotinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	EC₅₀	0.012 μM Compound: Poziotinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	IC₅₀	0.21 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring HER2-P780-Y781 ins GSP mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2-P780-Y781 ins GSP mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	0.43 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring HER2-A775-G776 ins YVMA mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2-A775-G776 ins YVMA mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	0.58 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR A763-Y764 ins FQEA mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR A763-Y764 ins FQEA mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	0.62 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR D770-N771 ins NPG mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR D770-N771 ins NPG mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
Calu-3	GI₅₀	10.12 nM Compound: cpd p	Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
HS27	GI₅₀	3830 nM Compound: 38; HM781e36B	Antiproliferative activity against human HS27 cells expressing wild type HER2 incubated for 72 hrs by MTS assay Antiproliferative activity against human HS27 cells expressing wild type HER2 incubated for 72 hrs by MTS assay	[PMID: 28754471]
NCI-H1975	IC₅₀	5.7 nM Compound: 38; HM781e36B	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay	[PMID: 28754471]
NCI-H358	GI₅₀	8.67 nM Compound: cpd p	Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
PC-9	GI₅₀	0.9 nM Compound: cpd p	Antiproliferative activity against human PC-9 cells expressing EGFR E746/A750 deletion mutant assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells expressing EGFR E746/A750 deletion mutant assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
SK-BR-3	IC₅₀	1 nM Compound: 38; HM781e36B	Antiproliferative activity against human SKBR3 cells expressing wild type HER2 incubated for 72 hrs by MTS assay Antiproliferative activity against human SKBR3 cells expressing wild type HER2 incubated for 72 hrs by MTS assay	[PMID: 28754471]

体外研究
(In Vitro)

The IC₅₀ levels of Poziotinib (HM781-36B) for N87 and SNU216 were 0.001 and 0.004 μM, respectively, which was 10-1000 fold lower than the IC₅₀ levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to ZD1839 or GW572016^[1].
Poziotinib (HM781-36B) also shows excellent selectivity with other kinases with greater than 100- to 1,000- fold IC₅₀ values compared with EGFR family members. Poziotinib (HM781-36B) possesses a functional α,β‐unsaturated carbonyl group as Michael acceptor moiety at the C6 position that allows covalent modifications of the EGFR kinase domain active site^[2].
The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC₅₀=0.003 and 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX^[3].

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

体内研究
(In Vivo)

The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only^[1].

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

分子量

491.34

Formula

C₂₃H₂₁Cl₂FN₄O₃

CAS 号

1092364-38-9

性状

固体

颜色

White to off-white

中文名称

波齐替尼；波奇替尼；泊齐替尼

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (101.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0353 mL	10.1763 mL	20.3525 mL
5 mM	0.4071 mL	2.0353 mL	4.0705 mL
10 mM	0.2035 mL	1.0176 mL	2.0353 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, 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。

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： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.87 mg/mL (5.84 mM); 澄清溶液
方案二

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.87 mg/mL (5.84 mM); 澄清溶液
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.09 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，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (4.58 mM); 澄清溶液

此方案可获得 ≥ 2.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 22.5 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。
方案五

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (4.58 mM); 澄清溶液

此方案可获得 ≥ 2.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 22.5 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。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

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: 99.96%

选择批次：

Data Sheet (632 KB) SDS (393 KB)

COA (252 KB) LCMS (121 KB) 元素分析报告 (213 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Nam HJ, et al. Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. Cancer Lett. 2011 Mar 28;302(2):155-65. [Content Brief]

[2]. Cha MY, et al. Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in CP-358774-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54. [Content Brief]

[3]. Kang MH, et al. Antitumor Activity of HM781-36B, alone or in Combination with Chemotherapeutic Agents, in Colorectal Cancer Cells. Cancer Res Treat. 2015 Mar 5. [Content Brief]

Poziotinib 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	2.0353 mL	10.1763 mL	20.3525 mL	50.8813 mL
	5 mM	0.4071 mL	2.0353 mL	4.0705 mL	10.1763 mL
	10 mM	0.2035 mL	1.0176 mL	2.0353 mL	5.0881 mL
	15 mM	0.1357 mL	0.6784 mL	1.3568 mL	3.3921 mL
	20 mM	0.1018 mL	0.5088 mL	1.0176 mL	2.5441 mL
	25 mM	0.0814 mL	0.4071 mL	0.8141 mL	2.0353 mL
	30 mM	0.0678 mL	0.3392 mL	0.6784 mL	1.6960 mL
	40 mM	0.0509 mL	0.2544 mL	0.5088 mL	1.2720 mL
	50 mM	0.0407 mL	0.2035 mL	0.4071 mL	1.0176 mL
	60 mM	0.0339 mL	0.1696 mL	0.3392 mL	0.8480 mL
	80 mM	0.0254 mL	0.1272 mL	0.2544 mL	0.6360 mL
	100 mM	0.0204 mL	0.1018 mL	0.2035 mL	0.5088 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:

Poziotinib1092364-38-9HM781-36B NOV120101波齐替尼波奇替尼泊齐替尼NOV120101NOV 120101NOV-120101EGFRApoptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Poziotinib (Synonyms: 波齐替尼; HM781-36B; NOV120101)

Customer Review

MCE 顾客使用本产品发表的 8 篇科研文献

Poziotinib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 EGFR 亚型特异性产品:

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纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Poziotinib 相关分类

完整储备液配制表

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Poziotinib (Synonyms: 波齐替尼; HM781-36B; NOV120101)

Customer Review

Poziotinib 相关抗体

MCE 顾客使用本产品发表的 8 篇科研文献

Poziotinib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 EGFR 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Poziotinib 相关抗体:

摩尔计算器

稀释计算器

Poziotinib 相关分类

完整储备液配制表

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