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Epertinib hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Epertinib hydrochloride图片
CAS NO:2071195-74-7
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
S-22611 hydrochloride
产品介绍
Epertinib (S-22611) hydrochloride 是一种口服有效的，可逆的，选择性的EGFR，HER4和HER2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。
生物活性

Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor ofEGFR,HER4andHER2, withIC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity[1][2].

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 IC50values of 4.5 and 1.6 nM, respectively[2].
Epertinib hydrochloride shows inhibitory activity against MDA-MB-361 cell, with an IC50of 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].

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 IC50values 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].

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 ED50values 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

性状

Solid

Formula

C30H28Cl2FN5O3

CAS 号

2071195-74-7

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
In Vitro: 

DMSO : 125 mg/mL(209.56 mM;Need ultrasonic)

H2O : 33.33 mg/mL(55.88 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6765 mL8.3825 mL16.7650 mL
5 mM0.3353 mL1.6765 mL3.3530 mL
10 mM0.1677 mL0.8383 mL1.6765 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.49 mM，饱和度未知) 的澄清溶液。

    以 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；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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (3.49 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.49 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在本网站选购。