EGFR-IN-7|cas:2267329-76-8|西域试剂

EGFR-IN-7,99.76%

产品编号：Bellancom-128862| CAS NO：2267329-76-8| 分子式：C₃₂H₄₁BrN₉O₂P| 分子量：694.60

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-128862	￥2950.00	杭州北京（现货）
Bellancom-128862	￥4950.00	杭州北京（现货）
Bellancom-128862	￥13000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

EGFR-IN-7

产品介绍

EGFR-IN-7 是一种有效的选择性 EGFR 激酶抑制剂，具有口服活性。EGFR-IN-7 对 EGFR (WT) 和 EGFR (突变体 C797S/T790M/L858R) 具有抑制作用，IC₅₀ 值分别为 7.92 nM 和 0.218 nM。EGFR-IN-7 可用于各种癌症的研究。

生物活性

EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC₅₀ values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers.

体外研究

EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC₅₀ values of 7.92 nM, 0.218 nM and 0.16 nM, respectively.
EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC₅₀ value of 154 nM.
EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC₅₀ value of 22 nM.
EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC₅₀ value of 19 nM.

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

Cell Proliferation Assay

Cell Line:	A431 cells; Ba/F 3 (EGFRΔ19del/T790M/C797S) suspension cells
Concentration:	1 mM; 10 μM-0.508 nM
Incubation Time:	3 days
Result:	Inhibited proliferation in cells.

体内研究
(In Vivo)

EGFR-IN-7 (compound 34; 5-45 mg/kg; p.o.; daily; for 13 days) shows potent anti-tumor activity in a subcutaneously implanted Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mouse resistance model.
EGFR-IN-7 (25 and 50 mg/kg; p.o.; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model.

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

Animal Model:	Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)
Dosage:	5, 15, 45 mg/kg
Administration:	Oral administration, daily, for 13 days
Result:	Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice.

Animal Model:	Subcutaneous xenograft PC-9 (Δ19del) model
Dosage:	0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg
Administration:	Oral administration, once a day, 3 weeks
Result:	Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy.

体内研究

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

Animal Model:	Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)
Dosage:	5, 15, 45 mg/kg
Administration:	Oral administration, daily, for 13 days
Result:	Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice.

Animal Model:	Subcutaneous xenograft PC-9 (Δ19del) model
Dosage:	0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg
Administration:	Oral administration, once a day, 3 weeks
Result:	Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy.

体内研究

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

Animal Model:	Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)
Dosage:	5, 15, 45 mg/kg
Administration:	Oral administration, daily, for 13 days
Result:	Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice.

Animal Model:	Subcutaneous xenograft PC-9 (Δ19del) model
Dosage:	0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg
Administration:	Oral administration, once a day, 3 weeks
Result:	Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (7.20 mM; ultrasonic and warming and adjust pH to 5 with 0.1 M HCL and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4397 mL	7.1984 mL	14.3968 mL
5 mM	0.2879 mL	1.4397 mL	2.8794 mL
10 mM	---	---	---

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。-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: ≥ 1.25 mg/mL (1.80 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (1.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (1.80 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (1.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (1.80 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (1.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。