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 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。

EGFR HER2-IN-5 是一种不可逆的、口服具有活力的双重抑制剂，能够抑制 EGFR 的活性 (IC50: 0.6 nM)。EGFR HER2-IN-4 对 L858R 和 T790M 突变显示出有效的 EGFR 激酶抑制活性。EGFR HER2-IN-4 在体内表现出明显的抗肿瘤作用，能够用于研究肺癌。

PROTACEGFRdegrader 5 (Compound 10) 是一种 PROTACEGFR 降解剂，可有效降解 HCC827 细胞中的 EGFRDel19，DC50为 34.8 nM。PROTACEGFRdegrader 5 显著诱导 HCC827 细胞凋亡 (apoptosis) 并将细胞阻滞在 G1 期。

EGFRT790M L858R-IN-5 (example 52) 作为EGFRT790M L858R的高效抑制剂表现出色，当浓度达到0.05 μM时，其抑制效果可达92.9%。

[pTyr5]EGFR(988-993) TFA 来源于表皮生长因子受体 (EGFR 988-993) 的自磷酸化位点 (Tyr992)。[pTyr5] EGFR(988-993) TFA 常与催化活性低的蛋白-酪氨酸磷酸1B (PTP1B) 结合。

[pTyr5] EGFR (988-993) is a compound obtained from the auto-phosphorylation site, Tyr992, located within the sequence of the epidermal growth factor receptor (EGFR 988-993). This compound is frequently found bound with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B).

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。

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.

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.

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)

EGFR peptide (myristoylated) 是一种合成的肽类PKC抑制剂，其IC50值为5µM，与EGFR内部区域的氨基酸序列相对应。当浓度为1µM时，可以逆转紫外线-2237M (UV-2237M-ADRR) 成纤维细胞瘤细胞对多柔比星的抗药性。

EGFRvIII peptide是一种合成肽，对应于特异性肿瘤、具有持续激活性的EGFR变体EGFRvIII的融合接头，该变体缺少野生型EGFR的第6至273个氨基酸。在25 µg/ml的浓度下，它能与MHC I类亚型HLA-A*0201阳性的T2细胞结合。在用于分离的人外周血单个核细胞（PBMCs）衍生的树突状细胞中，EGFRvIII peptide可诱导抗原呈递，进而刺激CD8+细胞毒性T淋巴细胞的激活和IFN-γ产生。与toll样受体5（TLR5）激动剂鞭毛蛋白B共同免疫EGFRvIII peptide（15 µg/动物），在正交GL261胶质母细胞瘤小鼠异种移植模型中，增加了CD8+ T细胞数量，减少了调节性T细胞（Tregs）数量，减少了肿瘤体积，并提高了生存率。