egfr-in-5

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-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-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。

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.

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-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。

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.

MS 39是突变型表皮生长因子受体(EGFR)的高效、高亲和力和选择性降解剂，具有的高效、高亲和力和选择性。MS 39 由吉非替尼通过连接物偶联至 VHL 配体，能有效地诱导突变型 EGFR 的降解（在 HCC827(外显子19 del)和 H3255 (L858R 突变)肺癌细胞系中的 DC50值分别为5 nM 和3.3 nM)，但在浓度高达10 μM 的野生型 EGFR 细胞系中无显著作用。MS 39在体外抑制 H3255肺癌细胞的增殖，并且在给药后在小鼠中具有生物利用性。

EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R T790M C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect.

EGFR VEGFR2-IN-5 (Compound 14) 是一种具口服活性的EGFR和VEGFR2双重抑制剂，其对VEGFR2的IC50为1.15 µM，对EGFRT790M的IC50为0.28 μM。它具有显著的抗癌活性。

EGFR-TK-IN-5 (Compound NCE 2) 是噻唑基吡唑啉的衍生物，对EGFR展现出强效的抑制作用和稳定性，并适用于肿瘤研究。

Icotinib Hydrochloride (BPI-2009H) 是一种口服的基于喹唑啉的表皮生长因子受体 (EGFR) 抑制剂，IC50值为5 nM，具有潜在的抗肿瘤活性。

7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)

Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J.Pharmacol.Exp.Ther. 345 393 PMID:23528611 |Kaspersen et al (2012) Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 44 35 PMID:22832269

Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable thioethers as odorless products.2 1.Yamada, T., Iritani, M., Ohishi, H., et al.Pericosines, antitumour metabolites from the sea hare-derived fungus Periconia byssoides. Structures and biological activitiesOrg. Biomol. Chem.5(24)3979-3986(2007) 2.Du, L., Munteanu, C., King, J.B., et al.An electrophilic natural product provides a safe and robust odor neutralization approach to counteract malodorous organosulfur metabolites encountered in skunk sprayJ. Nat. Prod.82(7)1989-1999(2019)