1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR c-Met/HGFR
  3. EGFR-IN-8

EGFR-IN-8 是 EGFRc-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 活性分子的靶点。

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EGFR-IN-8 Chemical Structure

EGFR-IN-8 Chemical Structure

CAS No. : 2407957-87-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥6765
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50 mg ¥6150
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.2 μM
Compound: 48
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
A549 IC50
0.3 μM
Compound: 48
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31446247]
CL97 IC50
0.5 μM
Compound: 48
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
CL97 IC50
0.6 μM
Compound: 48
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31446247]
MDA-MB-231 IC50
0.2 μM
Compound: 48
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
NCI-H1975 IC50
0.3 μM
Compound: 48
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31446247]
NCI-H1975 IC50
0.3 μM
Compound: 48
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
PC-9 IC50
0.5 μM
Compound: 48
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31446247]
PC-9 IC50
0.6 μM
Compound: 48
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31446247]
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].

MCE 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].

MCE 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
性状

固体

颜色

Light yellow to yellow

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
细胞实验: 

DMSO 中的溶解度 : 8.33 mg/mL (12.58 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5105 mL 7.5526 mL 15.1053 mL 37.7632 mL
5 mM 0.3021 mL 1.5105 mL 3.0211 mL 7.5526 mL
10 mM 0.1511 mL 0.7553 mL 1.5105 mL 3.7763 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
EGFR-IN-8
目录号:
HY-126320
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