Neratinib (Synonyms: 来那替尼; HKI-272)

目录号: HY-32721 纯度: 99.94%: Data Sheet SDS COA 产品使用指南
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Neratinib (HKI-272) 是一种具有口服活性的、不可逆的、高选择性的 HER2 和 EGFR 抑制剂，IC₅₀ 值分别为 59 nM 和 92 nM。

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Neratinib Chemical Structure

CAS No. : 698387-09-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥500	In-stock
5 mg	￥350	In-stock
10 mg	￥600	In-stock
25 mg	￥950	In-stock
50 mg	￥1300	In-stock
100 mg	￥2300	In-stock
200 mg	￥4200	In-stock
500 mg		询价
1 g		询价

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Customer Review

Other Forms of Neratinib:

MCE 顾客使用本产品发表的 21 篇科研文献

: Neratinib purchased from MCE. Usage Cited in: Sci Transl Med. 2018 Jun 20;10(446):eaao2565. [Abstract]; Immunoblots of 3 individual KM tumors from mice treated for 3 days with Neratinib or vehicle control.

: Neratinib purchased from MCE. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]; Influence of BIBW 2992 or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.

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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

Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively^[1].

IC₅₀ & Target^[1]

HER2

59 nM (IC₅₀)

EGFR

92 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	1.9 μM Compound: 2; HKI272	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
BT-474	IC₅₀	2.06 nM Compound: Neratinib	Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
COLO-678	IC₅₀	694.11 nM Compound: Neratinib	Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
ES-2	IC₅₀	787.91 nM Compound: Neratinib	Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
MDA-MB-468	IC₅₀	405.51 nM Compound: Neratinib	Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
MFE-280	IC₅₀	1291.95 nM Compound: Neratinib	Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NCI-H441	IC₅₀	1280.72 nM Compound: Neratinib	Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NCI-N87	IC₅₀	0.64 nM Compound: Neratinib	Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NUGC-4	IC₅₀	38.15 nM Compound: Neratinib	Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
Sf9	IC₅₀	2.5 nM Compound: 3, HKI-272	Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting	[PMID: 24900643]
Sf9	IC₅₀	66 nM Compound: 3, HKI-272	Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting	[PMID: 24900643]
SK-BR-3	IC₅₀	10.34 nM Compound: Neratinib	Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
SK-BR-3	IC₅₀	7.2 nM Compound: 45	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by sulforhodamine B colorimetric assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by sulforhodamine B colorimetric assay	[PMID: 36332549]

体外研究
(In Vitro)

Neratinib 对其他丝氨酸-苏氨酸激酶没有活性，例如 Akt、细胞周期蛋白 D1/cdk4、细胞周期蛋白 E/cdk2、细胞周期蛋白 B1/cdk1、IKK-2、MK-2、PDK1、c-Raf 和 Tpl-2，以及作为酪氨酸激酶 c-Met^[1]。
Neratinib (0.5 ng/mL–5 μg/mL，2 天) 抑制显示高水平 HER-2 (3T3/neu、SK-Br-3 和 BT474) 并且在既不表达 HER-2 也不表达 EGFR (3T3、MDA-MB-435 和 SW620) 的细胞系中活性低得多^[1]。
Neratinib (0-2 nM，12-16 小时) 将 BT474 细胞周期停滞在 G1-S 期^[1]。
Neratinib 抑制 MAPK 和 Akt 磷酸化、细胞周期蛋白 D1 水平的下调和 p27^[1]的诱导。

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

Cell Proliferation Assay^[1]

Cell Line:	3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620
Concentration:	0.5 ng/mL–5 μg/mL
Incubation Time:	2 days (6 days for BT474)
Result:	Inhibited cell proliferation with IC₅₀ values of 700 ± 78, 3 ± 0.14, 2 ± 0.18, 2 ± 0.06, 81± 9, 960 ± 165 and 690 ± 84 nM against 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 cells, respectively.

Western Blot Analysis^[1]

Cell Line:	BT474 or A431 cells
Concentration:	0, 2, 10, 50, 100 and 200 nM
Incubation Time:	3 h
Result:	Decreased ligand-independent receptor phosphorylation by 50% (IC₅₀) at 5 nM in BT474 cells, repressed EGF-dependent phosphorylation of EGFR in A431 cells at a comparable dose (IC₅₀ = 3 nM). Effectively repressed phosphorylation of MAPK and Akt in BT474 cells.

Cell Cycle Analysis^[1]

Cell Line:	BT474
Concentration:	0–2 nM
Incubation Time:	12–16 h
Result:	Blocked cell cycle progression, causing a G1-S arrest, a 50% decrease in the number of cells in the S (DNA synthesis) phase of the cell cycle was observed at a concentration of 2 nM.

体内研究
(In Vivo)

Neratinib (HKI-272) (0 -80 mg/kg/天；ig；42 天) 对表达高水平 HER-2 或 EGFR 的癌细胞显示出抗癌活性^[1]。

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

Animal Model:	Female athymic (nude) mice, tumor xenograft^[1]
Dosage:	10, 20, 40, 60 or 80 mg/kg/day
Administration:	Gavage, 42 days
Result:	Reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3 and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts.

Clinical Trial

分子量

557.04

Formula

C₃₀H₂₉ClN₆O₃

CAS 号

698387-09-6

性状

固体

颜色

White to yellow

中文名称

来那替尼

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 8.33 mg/mL (14.95 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	1.7952 mL	8.9760 mL	17.9520 mL
5 mM	0.3590 mL	1.7952 mL	3.5904 mL
10 mM	0.1795 mL	0.8976 mL	1.7952 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: ≥ 0.83 mg/mL (1.49 mM); 澄清溶液

此方案可获得 ≥ 0.83 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 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。

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: 99.94%

选择批次：

Data Sheet (634 KB) SDS (394 KB)

COA (285 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Rabindran SK, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res, 2004, 64(11), 3958-3965. [Content Brief]

Neratinib 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	1.7952 mL	8.9760 mL	17.9520 mL	44.8801 mL
	5 mM	0.3590 mL	1.7952 mL	3.5904 mL	8.9760 mL
	10 mM	0.1795 mL	0.8976 mL	1.7952 mL	4.4880 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:

Neratinib698387-09-6HKI-272来那替尼HKI272HKI 272EGFREpidermal growth factor receptorErbB-1HER1breast cancersolid tumorsnon–small-cell lung cancerBT474A431gastric cancerInhibitorinhibitorinhibit

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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）

Neratinib (Synonyms: 来那替尼; HKI-272)

Customer Review

Other Forms of Neratinib:

MCE 顾客使用本产品发表的 21 篇科研文献