1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Epertinib hydrochloride

Epertinib hydrochloride  (Synonyms: S-22611 hydrochloride)

目录号: HY-107367A 纯度: 98.25%
COA 产品使用指南

Epertinib (S-22611) hydrochloride 是一种口服有效的,可逆的,选择性的 EGFRHER4HER2 抑制剂,IC50 值分别为 1.48 nM,2.49 nM 和 7.15 nM。Epertinib hydrochloride 具有高效的抗肿瘤活性。

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Epertinib hydrochloride Chemical Structure

Epertinib hydrochloride Chemical Structure

CAS No. : 2071195-74-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3412
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1 mg ¥1040
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5 mg ¥2600
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10 mg ¥4200
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25 mg ¥7600
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Customer Review

Other Forms of Epertinib hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity[1][2]. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

EGFR

1.48 ± 0.0 nM (IC50)

HER4

2.49 ± 0.1 nM (IC50)

HER2

7.15 nM (IC50)

体外研究
(In Vitro)

Epertinib hydrochloride inhibits the phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50 values of 4.5 and 1.6 nM, respectively[2].
Epertinib hydrochloride shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM[1].
Epertinib hydrochloride (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2[2].

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

Cell Proliferation Assay[2]

Cell Line: NCI-N87 (stomach), BT-474 (breast), SK-BR-3 (breast), MDA-MB-453 (breast), MDA-MB-175VII (breast), HT115 (colon), Calu-3 (lung), fR2 (breast), and MRC-5 (lung)
Concentration: 0-10 μM
Incubation Time: 72 h
Result: Inhibited the growth of NCI-N87, BT-474, SK-BR-3, MDA-MB-453, MDA-MB-175VII, HT115, Calu-3, fR2, and MRC-5, with IC50 values of 8.3 ± 2.6, 9.9 ± 0.8, 14.0 ± 3.6, 48.6 ± 3.1, 21.6 ± 4.3, 53.3 ± 8.6, 241.5 ± 29.2, 5366.7 ± 65.2, and 4964.6 ± 340.3.
体内研究
(In Vivo)

Epertinib hydrochloride (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity[1].
Epertinib hydrochloride (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume[1].
Epertinib hydrochloride (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner[2].

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

Animal Model: Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1]
Dosage: 12.5, 25, 50, 100  mg/kg
Administration: Orally, once daily for 28 days
Result: Showed antitumor activity in the mammary fat pad implantation model using both cell lines and the ED50 values were comparable (24.1 mg/kg and 26.5 mg/kg for MDA-MB-361 and BR2 (MDA-MB-361-luc-BR2), respectively).
Animal Model: Nude mice (BALB/cAJcl-nu/nu, implanted intracranially with MDA-MB-361 or BR2 cells)[1]
Dosage: 50 mg/kg
Administration: Orally, once daily for 30 days
Result: Significantly reduced the brain tumor volume, indicating that epertinib could have potent antitumor activity in brain metastasis even in the presence of an intact BTB (blood-tumor barrier).
Animal Model: Nude mice (BALB/cAJcl-nu/nu, prepared by subcutaneous implantation of human gastric cancer cells, NCI-N87 into the back of nude mice)[2]
Dosage: 0, 6.25, 12.5, 25, and 50 mg/kg
Administration: Oral gavage, daily for 10-28 days
Result: Significantly inhibited the tumor growth in a dose-dependent manner.
分子量

596.48

Formula

C30H28Cl2FN5O3

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (209.56 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)

H2O 中的溶解度 : 33.33 mg/mL (55.88 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6765 mL 8.3825 mL 16.7650 mL
5 mM 0.3353 mL 1.6765 mL 3.3530 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 (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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: ≥ 2.08 mg/mL (3.49 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.49 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):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

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

Epertinib hydrochloride 相关分类

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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.6765 mL 8.3825 mL 16.7650 mL 41.9126 mL
5 mM 0.3353 mL 1.6765 mL 3.3530 mL 8.3825 mL
10 mM 0.1677 mL 0.8383 mL 1.6765 mL 4.1913 mL
15 mM 0.1118 mL 0.5588 mL 1.1177 mL 2.7942 mL
20 mM 0.0838 mL 0.4191 mL 0.8383 mL 2.0956 mL
25 mM 0.0671 mL 0.3353 mL 0.6706 mL 1.6765 mL
30 mM 0.0559 mL 0.2794 mL 0.5588 mL 1.3971 mL
40 mM 0.0419 mL 0.2096 mL 0.4191 mL 1.0478 mL
50 mM 0.0335 mL 0.1677 mL 0.3353 mL 0.8383 mL
DMSO 60 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6985 mL
80 mM 0.0210 mL 0.1048 mL 0.2096 mL 0.5239 mL
100 mM 0.0168 mL 0.0838 mL 0.1677 mL 0.4191 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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.

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Epertinib hydrochloride
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HY-107367A
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