Epertinib hydrochloride S-22611 hydrochloride|cas:2071195-74-7|西域试剂

Epertinib hydrochloride S-22611 hydrochloride,98.25%

产品编号：Bellancom-107367A| CAS NO：2071195-74-7| 分子式：C₃₀H₂₈Cl₂FN₅O₃| 分子量：596.48

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货号	价格	库存与货期
Bellancom-107367A	￥2600.00	杭州北京（现货）
Bellancom-107367A	￥4200.00	杭州北京（现货）
Bellancom-107367A	￥7600.00	杭州北京（现货）
Bellancom-107367A	￥12000.00	杭州北京（现货）

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Epertinib hydrochloride 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 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.

体外研究

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.

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

Cell Proliferation Assay

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.
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.

西域 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)
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)
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)
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.

体内研究

西域 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)
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)
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)
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.

体内研究

西域 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)
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)
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)
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.

性状

Solid

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