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/C797S的IC50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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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 : 125 mg/mL(217.88 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7430 mL | 8.7152 mL | 17.4304 mL | | 5 mM | 0.3486 mL | 1.7430 mL | 3.4861 mL | | 10 mM | 0.1743 mL | 0.8715 mL | 1.7430 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。 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。
|
m.cnreagent.com