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Epertinib hydrochloride

(Synonyms: S-22611 hydrochloride)

目录号: PL01601 纯度: ≥98%

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。

CAS No. :2071195-74-7

商品编号	规格	价格	会员价
PL01601-5mg	5mg	¥1815.00	请登录
PL01601-10mg	10mg	¥2875.00	请登录
PL01601-25mg	25mg	¥4415.00	请登录
PL01601-50mg	50mg	¥6225.00	请登录
PL01601-100mg	100mg	¥8375.00	请登录
PL01601-200mg	200mg	¥11295.00	请登录
PL01601-1 mL x 10 mM (in DMSO)	1 mL x 10 mM (in DMSO)	¥2385.00	请登录

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中文名称	Epertinib hydrochloride
英文名称	Epertinib hydrochloride
英文别名	Epertinib (hydrochloride);(R,Z)-1-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)but-2-yn-1-one O-morpholin-3-ylmethyl oxime hydrochloride;S-22611 hydrochloride;Epertinib hydrochloride
Cas No.	2071195-74-7
分子式	C₃₀H₂₈Cl₂FN₅O₃
分子量	596.48
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	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。

产品详情	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 of EGFR, HER4 and HER2, with IC 50 s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity.
性状	Solid
IC50 & Target[1][2]	EGFR 1.48 ± 0.0 nM (IC50) HER4 2.49 ± 0.1
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. Epertinib hydrochloride shows inhibitory activity against MDA-MB-361 cell, with an IC50 of 26.5 nM. Epertinib hydrochloride (0-10 μM, 72 h) can selectively inhibit the proliferation of a range of cancer cell lines expressing EGFR and/or HER2. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Epertinib hydrochloride (0-100 mg/kg, Orally, once daily for 28 days) shows antitumor activity. Epertinib hydrochloride (50 mg/kg, Orally, once daily for 30 days) significantly reduces the brain tumor volume. Epertinib hydrochloride (0-50 mg/kg, Orally, once daily for 10-28 days) significantly inhibits the tumor growth in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. 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. [2]. 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.

溶解度数据	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

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[1]. 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.
[2]. 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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Epertinib hydrochloride

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