egfrin5

EGFR-IN-5 是 EGFR 的特异性抑制剂。 EGFR、EGFR(L858R)、EGFR(L858R/T790M) 和 EGFR(L858R/T790M/C797S) 的 IC50 分别为 10.4、1.1、34、7.2 nM。

EGFR-IN-542 is a novel EGFR inhibitor. EGFR-IN-542 significantly reduces myocardial inflammation, fibrosis, apoptosis and dysfunction. It shows promise for use in the treatment of obesity-induced cardiac complications.

EGFR-IN-53 (Compound 7) 是EGFR 的有效抑制剂，IC50值为 8.264 μM，它对癌细胞系显示细胞毒性。

EGFR-IN-51 (Compound 6) is a highly potent EGFR inhibitor, demonstrating strong affinity with IC50 values of 0.493, 102.60, and 461.63 μM, respectively, against EGFR, EGFR L858R-TK, and EGFR T790M-TK targets. Additionally, EGFR-IN-51 exhibits cytotoxicity against cancer cell lines, effectively inducing apoptosis [1].

EGFR-IN-52 (Compound 4) is a highly effective inhibitor of the epidermal growth factor receptor (EGFR). It exhibits IC50 values of 0.358, 86.02, and 432.67 μM against EGFR, EGFR L858R-TK, and EGFR T790M-TK, respectively. Additionally, EGFR-IN-52 demonstrates potent cytotoxic effects on cancer cell lines and triggers apoptosis [1].

EGFR-IN-57 (Compound 25a) 是一种有效的、具有口服活性的EGFR-TK 抑制剂，IC50值为 0.054 μM。EGFR-IN-57 也抑制VEGFR-2、CK2α、topoisomerase IIβ和tubulin polymerization，IC50值分别为 0.087、0.171、0.13 和 3.61 μM。EGFR-IN-57 诱导细胞 G2/M 和 pre-G1 期周期阻滞，诱导癌细胞凋亡 (apoptosis)。

EGFR-IN-54 (Compound 3c) 是一种 EGFR 的有效抑制剂 (IC50: 1.623 μM)，对癌细胞具有毒性。

EGFR-IN-56 (Compound 13a) 是一种 EGFR 的有效抑制剂，能够作用于 EGFRT790M (IC50: 541.7 nM) 和 EGFRT790M/L858R (IC50: 132.1 nM)。EGFR-IN-56 能够将癌细胞的细胞周期阻滞在 G2/M 期，并诱导细胞凋亡 (apoptosis)。

EGFR-IN-59 是 EGFR 抑制剂，其IC50值为190 nM，也是一直凋亡 (apoptosis) 诱导剂。EGFR-IN-59 对非小肺癌细胞系 (A549) 和正常肺成纤维细胞 (WI38) 表现出细胞毒性的IC50分别为 8.62 和 52.6 μM。EGFR-IN-59 能够用于研究非小细胞肺癌 (NSCLC)、头颈癌、乳腺癌和结直肠癌等多种癌症。

EGFR-IN-55 是 EGFR 的有效抑制剂，能够作用于 EGFRWT (IC50: 70 nM) 和 EGFRL858R/T790M (IC50: 3.9 nM) 。EGFR-IN-55 能够将 NCI-H1975 细胞的细胞周期阻滞在 G0/G1 期，表现出抗癌效果。

EGFR-IN-58 是一种有效的、选择性的、 ATP 竞争性的 EGFR 抑制剂。EGFR-IN-58 对黑色素瘤、结肠癌和血癌表现出显著的细胞毒性。

EGFR-IN-50 是一种针对 L858R 抗性突变的强效 EGFR 抑制剂，能够作用于 TEL-EGFR-L858R-BaF3 及 TEL-EGFR-T790M-L858R-BaF3，他们的 GI50 值分别为 8 nM、6.03 μM。EGFR-IN-50 对癌细胞表现出抗增殖作用。

Diethanolamine Fusidate is a bacteriostatic antibiotic with similar activity and better absorption after oral administration (in animals) than the sodium salt of Fusidic Acid. This product inhibits protein synthesis in prokaryotes by inhibiting the ribosome-dependent activity of G factor and translocation of peptidyl-tRNA.

EGFR-IN-557 is an EGFR inhibitor, attenuating Ang II-induced Kidney Fibrosis.

VEGFR-IN-5 (compound 9k) 作为VEGFR2的高效抑制剂,展现出了 8.4 nM 的IC50值,并具备可观的口服生物利用度.此外,VEGFR-IN-5 能够抑制人脐静脉内皮细胞 (HUVEC) 的迁移和侵袭行为,同时诱导其细胞凋亡.