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EGFR-IN-11
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EGFR-IN-11图片
CAS NO:2463200-44-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
EGFR-IN-11 是第四代EGFR-酪氨酸激酶抑制剂 (EGFR-TKI),对三重突变的EGFRL858R/T790M/C797SIC50为 18 nM。EGFR-IN-11 显著抑制 EGFR 磷酸化,诱导细胞凋亡,将细胞周期阻滞在 G0/G1处。
生物活性

EGFR-IN-11 is a fourth-generationEGFR-tyrosine kinase inhibitor (EGFR-TKI) with anIC50of 18 nM for triple mutantEGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses theEGFRphosphorylation, induce theapoptosis, and arrest cell cycle at G0/G1[1].

IC50& Target[1]

EGFRL858R/T790M/C797S

18 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-11 (Compound D9; 0.0001-10 μM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 μM, respectively[1].
EGFR-IN-11 (0.01-1.00 μM for HCC827 cells; 0.1-10.00 μM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line[1].
EGFR-IN-11 (1 μM; 24 h) potently induces the apoptosis of HCC827 cells.[1]
EGFR-IN-11 (1 μM; 24 h) induces cell cycle arrests in HCC827 cell[1].

Cell Proliferation Assay[1]

Cell Line:Human lung cancer cell lines HCC827 (EGFRDel E746-A750), H1975 (EGFRL858R/T790M) and A549 (EGFRWT); epidermoid carcinoma cell line A431 (EGFRWT)
Concentration:0.0001, 0.0003, 0.001, 0.003, 0.01, 0.1, 1, 10 μM
Incubation Time:72 hours
Result:Inhibited HCC827 H1975 A549 cells proliferation with IC50s of 0.88±0.09 nM, 0.20±0.01 μM, 2.91±0.61 μM, and >10 μM, respectively.

Western Blot Analysis[1]

Cell Line:HCC827, H1975 and A549 cells
Concentration:1.00, 0.10 and 0.01 μM for HCC827 cells; 10.00, 1.00 and 0.10 μM for H1975 and A549 cells
Incubation Time:8 hours
Result:Suppressed EGFR phosphorylation in a concentration-dependent manner. EGFR phosphorylation in the HCC827 cell line was more remarkably suppressed than in the H1975 and A549 cell lines.

Apoptosis Analysis[1]

Cell Line:HCC827 cells
Concentration:1 μM
Incubation Time:24 hours
Result:The percentages of apoptotic cells is 56.91%.

Cell Cycle Analysis[1]

Cell Line:HCC827 cells
Concentration:1 μM
Incubation Time:24 hours
Result:The number of HCC827 cells in G0/G1 phase was increased significantly.
分子量

573.71

性状

Solid

Formula

C29H35N9O2S

CAS 号

2463200-44-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL(217.88 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7430 mL8.7152 mL17.4304 mL
5 mM0.3486 mL1.7430 mL3.4861 mL
10 mM0.1743 mL0.8715 mL1.7430 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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 (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 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%corn oil

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。