标签归档：epertinib

Epertinib hydrochloride(Synonyms: S-22611 hydrochloride)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Epertinib hydrochloride (Synonyms: S-22611 hydrochloride) 纯度: 99.76%

Epertinib hydrochloride (S-22611 hydrochloride) 是一种有效，可口服，可逆的，选择性的 EGFR，HER2 和 HER4 抑制剂，IC50 值分别为 1.48 nM，7.15 nM 和 2.49 nM。Epertinib hydrochloride 具有高效的抗肿瘤活性。

Epertinib hydrochloride(Synonyms: S-22611 hydrochloride)

Epertinib hydrochloride Chemical Structure

CAS No. : 2071195-74-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3412 In-stock
5 mg ￥2600 In-stock
10 mg ￥4200 In-stock
25 mg ￥7600 In-stock
50 mg ￥12000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Epertinib hydrochloride 相关产品

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生物活性

Epertinib hydrochloride (S-22611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride shows potent antitumor activity[1].

IC50 & Target[1]

EGFR

1.48 nM (IC50)

HER4

2.49 nM (IC50)

HER2

7.15 nM (IC50)

分子量

596.48

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 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
10 mM 0.1677 mL 0.8383 mL 1.6765 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°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。

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-CD in 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 μL 20% 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. [1]. Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105(8):1040-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Epertinib(Synonyms: S-22611)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Epertinib (Synonyms: S-22611)

Epertinib (S-22261) 是一种有效，可口服，可逆的，选择性的 EGFR，HER2 和 HER4 抑制剂，IC50 值分别为 1.48 nM，7.15 nM 和 2.49 nM。Epertinib 具有高效的抗肿瘤活性。

Epertinib(Synonyms: S-22611)

Epertinib Chemical Structure

CAS No. : 908305-13-5

规格 价格 是否有货
1 mg ￥2200 询问价格 & 货期

* Please select Quantity before adding items.

Epertinib 的其他形式现货产品:

Epertinib hydrochloride

生物活性

Epertinib (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity[1].

IC50 & Target[1]

EGFR

1.48 nM (IC50)

HER2

2.49 nM (IC50)

HER4

7.15 nM (IC50)

体外研究
(In Vitro)

Epertinib (S-22261) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively, and shows no effect on KDR, IGF1R, SRC, KIT, and PDGFRβ (IC50, >10000 nM). Epertinib inhibits relative phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50s of 4.5 and 1.6 nM, respectively.
Furthermore, Epertinib exhibits inhibitory activity against the growth of cancer cell lines expressing EGFR and/or HER2, with IC50s of 8.3 nM (NCI-N87 (stomach)), 9.9 nM (BT-474 (breast)), and 14 nM (SK-BR-3 (breast))[1].
Epertinib also inhibits MDA-MB-361 cell growth, with an IC50 of 26.5 nM[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Epertinib shows antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days, with an ED50 of 10.2 mg/kg. Epertinib (50 mg/kg, p.o.) is four times more potent activity than GW572016 and completely inhibits the growth of cancer cells in mice[1].
Epertinib (50 mg/kg, p.o.) markedly reduces the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model (IVM)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

560.02

Formula

C30H27ClFN5O3
CAS 号

908305-13-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献

  • [1]. Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105(8):1040-8.

    [2]. Tanaka Y, et al. Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity. Sci Rep. 2018 Jan 10;8(1):343.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务