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

EGFR-IN-8 是 EGFR 和 c-Met 雙重抑制劑，化合物 48。EGFR-IN-8 有望成為進(jìn)一步開(kāi)發(fā)靶向 EGFR TKI 抗性 NSCLC 活性分子的靶點(diǎn)。

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EGFR-IN-8 Chemical Structure

EGFR-IN-8 Chemical Structure

CAS No. : 2407957-87-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥6765
In-stock
50 mg ￥6150
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
細(xì)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]
體外研究
(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.
體內(nèi)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 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 8.33 mg/mL (12.58 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
EGFR-IN-8
目錄號(hào)：
HY-126320
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