Cat. No. | Product Name | Target | Signaling Pathways |
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T11160 |
EGFR-IN-5
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
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。 | |||
T64254 | EGFR/HER2-IN-5 | ||
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。 | |||
T2307 |
Icotinib Hydrochloride
埃克替尼盐酸盐,盐酸埃克替尼,BPI-2009H |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
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。 | |||
T74524 | PROTAC EGFR degrader 5 | ||
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。 | |||
T11164 |
EGFR mutant-IN-1
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
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. | |||
T83692 |
EGFR Peptide (human, mouse) (myristoylated) TFA
Myr-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH,Epidermal Growth Factor Receptor Peptide,N-myristoyl-RKRTLRRL |
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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。 | |||
T41156 |
MS 39
|
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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。 | |||
T35855 |
AAA
|
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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... | |||
T35897 |
ASK120067
|
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ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT... | |||
T36643 |
PKI-166 hydrochloride
|
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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 ... | |||
T35423 |
7-oxo Staurosporine
|
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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 gr... | |||
T37594 |
Pericosine A
|
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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 t... | |||
T83852 |
EGFRvIII Peptide TFA
PEGFRvIII (9-mer),Epidermal Growth Factor Receptor Variant III Peptide |
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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。 |