EGFR-IN-8

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EGFR-IN-8  纯度: 98.31%

EGFR-IN-8 是 EGFR 和 c-Met 双重抑制剂，化合物 48。EGFR-IN-8 有望成为进一步开发靶向 EGFR TKI 抗性 NSCLC 药物的靶点。

EGFR-IN-8

EGFR-IN-8 Chemical Structure

CAS No. : 2407957-87-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5100 In-stock
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
50 mg ￥16500 In-stock
100 mg ￥25500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC[1].

IC50 & Target

EGFR; c-Met[1]
体外研究
(In Vitro)

EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively[1].
EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status[1].

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.

Cell Viability Assay[1]

Cell Line: A549, PC9, H1975, CL68, and CL97 cells
Concentration: 0-20 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Showed inhibitory effects on different cells.

Western Blot Analysis[1]

Cell Line: A549, PC9, H1975, CL68, and CL97 cells
Concentration: 0-0.6 μM
Incubation Time: 48 hours
Result: Decreased EGFR and c-Met expression.

体内研究
(In Vivo)

EGFR-IN-8 (oral gavage; 50 and 150 mg/kg; once daily; 20 days) exhibits a dose-dependent suppression (29% and 60%, respectively) of H1975 xenograft tumor growth at 50 and 150 mg/kg[1].

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.

Animal Model: Nude mice H1975 xenograft tumor model[1]
Dosage: 50 and 150 mg/kg
Administration: Oral gavage; 50 and 150 mg/kg; once daily; 20 days
Result: Inhibited H1975 xenograft tumor growth.

分子量

662.02

Formula

C32H23ClF3N7O4
CAS 号

2407957-87-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (12.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5105 mL 7.5526 mL 15.1053 mL
5 mM 0.3021 mL 1.5105 mL 3.0211 mL
10 mM 0.1511 mL 0.7553 mL 1.5105 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。-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。
参考文献

  • [1]. Dokla EME, et al. 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. Eur J Med Chem. 2019 Aug 9;182:111607.

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