EGFR-IN-11

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.

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. 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.EGFR-IN-11 (1 μM; 24 h) potently induces the apoptosis of HCC827 cells.EGFR-IN-11 (1 μM; 24 h) induces cell cycle arrests in HCC827 cell.Cell Proliferation Assay 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 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 Cell Line:HCC827 cells Concentration:1 μM Incubation Time:24 hours Result:The percentages of apoptotic cells is 56.91%.Cell Cycle Analysis Cell Line:HCC827 cells Concentration:1 μM Incubation Time:24 hours Result:The number of HCC827 cells in G0/G1 phase was increased significantly.

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Angiogenesis

EGFR

EGFR

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2463200-44-2

573.71

C29H35N9O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (217.88 mM; 超声助溶 )

CN1CCN(CC1)c1ccc(Nc2ncc3nc(Nc4ccccc4)n([C@@H]4CCN(C4)S(=O)(=O)C4CC4)c3n2)cc1

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(-20℃)

With Ice Pack

≥ 2 years