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Cat. No. | Product Name | Target | Signaling Pathways |
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T11161 |
EGFR-IN-7
TQB3804 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-7 (TQB3804) 是一种有效选择性的EGFR 激酶抑制剂,对 EGFR (WT) 和 EGFR (mutant C797S/T790M/L858R) 的IC50值分别为 7.92 和 0.218 nM,具有抗肿瘤活性。 | |||
T61272 | EGFR/HER2-IN-7 | ||
EGFR/HER2-IN-7 is a highly selective and potent anticancer compound specifically designed to target MCF-7 breast cancer cells. It functions as a dual inhibitor, targeting both EGFR/HER2 kinases and DHFR (dihydrofolate reductase). Its inhibitory activities are measured with IC50 values of 0.18 μM for EGFR, 0.146 μM for HER2, and 0.907 μM for DHFR [1]. | |||
T77746 |
Tyrosine kinase-IN-7
|
EGFR; Antiviral | Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Tyrosine kinase-IN-7 是一种有效的酪氨酸激酶 EGFR 抑制剂,抑制 EGFR(WT) 和 EGFR(T790M) ,在多种癌细胞系中显示出抗癌和抗肿瘤活性。Tyrosine kinase-IN-7 具有潜在的抗炎和抗病毒活性。 | |||
T11163 |
EGFR-IN-9
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-9 是一种有效的 EGFR 激酶抑制剂,对于野生型 EGFR 激酶和双重突变型 EGFR 激酶 (L858R/T790M) 的 IC50 分别为 7 nM 和 28 nM。EGFR-IN-9 具有抗肿瘤活性。 | |||
T62446 | EGFR-IN-63 | ||
EGFR- IN-63 是一种 EGFR 抑制剂,其 IC50 值为 0.096 μM。EGFR- IN-63 对 MCF-7 细胞 (IC50: 2.49 μM) 表现出抗癌效果。 | |||
T60574 | EGFR-IN-53 | ||
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。 | |||
T79729 |
EGFR/CDK2-IN-4
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/CDK2-IN-4(化合物4c)是一种EGFR与CDK-2的双重抑制剂,其IC50值分别为89.6 nM和165.4 nM。该化合物在MCF-7细胞中能诱导(apoptosis)凋亡,并导致细胞周期在S期停滞。EGFR/CDK2-IN-4显示出显著的抗癌细胞毒性,对MCF-7细胞的IC50为2.74 μM。 | |||
T79651 |
EGFR-IN-83
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-83(化合物9)为EGFR抑制剂,IC50为2.53 nM。该化合物对MCF-7及MDA-MB-231细胞显示出抗增殖作用,其IC50值分别为2.50 μM及1.96 μM。此外,EGFR-IN-83能够诱导细胞凋亡。 | |||
T74623 | PROTAC EGFR degrader 7 | ||
PROTACEGFRdegrader 7 (compound 13b) 是一种有效的、选择性 CRBN 招募的 PROTACEGFRL858R/T790M 降解剂,其 DC50为 13.2 nM。PROTACEGFRdegrader 7 抑制 NCI-H1975 细胞增殖,IC50为 46.82 nM。PROTACEGFRdegrader 7 显著诱导 NCI-H1975 细胞凋亡 (apoptosis) 和 G2/M 期阻滞。PROTACEGFRdegrader 7 具有抗肿瘤活性,可用于非小细胞肺癌 (NSCLC) 研究。 | |||
T79727 |
EGFR/CDK2-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/CDK2-IN-2(compound 6a)是一种针对EGFR和CDK-2的双重抑制剂,具有19.6 nM和87.9 nM的IC50s。该化合物能在MCF-7细胞内诱导凋亡,并在S期引发细胞周期停滞。此外,EGFR/CDK2-IN-2展现出IC50为0.39 μM的显著抗癌活性,对MCF-7细胞具有强效的细胞毒性。 | |||
T79728 |
EGFR/CDK2-IN-3
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/CDK2-IN-3(compound 4b)是一种针对EGFR与CDK-2的双重抑制剂,分别具有71.7 nM和113.7 nM的IC50s。该化合物在MCF-7细胞中能诱导凋亡,导致细胞周期在S期停滞,并显示出对癌细胞的明显毒性,其对MCF-7细胞的IC50值为3.16 μM。 | |||
T62503 |
EGFR/BRAFV600E-IN-1
|
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EGFR/BRAFV600E-IN-1 (Compound 23) 是一种有效的 EGFR (IC50: 0.08 μM) 和 BRAFV600E (IC50: 0.15 μM) 双重抑制剂。EGFR/BRAFV600E-IN-1 在 G1 前和 G2/M 期均诱导细胞凋亡 (apoptosis) 及细胞周期停滞。EGFR/BRAFV600E-IN-1 对 A-549 (IC50: 1.2 μM)、MCF-7 (IC50: 0.79 μM)、Panc-1 (IC50: 1.3 μM)、HT-29 (IC50: 1.23 μM) 表现出抗增殖作用。 | |||
T79327 |
EGFR-IN-81
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-81(Compound 10i)是一种选择性EGFR抑制剂,针对EGFRWT和L858R/T790M的抑制作用表现IC50值分别为4.38 nM和5.69 nM。此外,EGFR-IN-81对MCF-7和HCT116细胞株展示了细胞毒性,其有效浓度分别达到2.07 μM和6.72 μM。 | |||
T63810 | BTK-IN-7 | ||
BTK-IN-7 是选择性的、有效的 BTK 抑制剂,其 IC50 值为 4.0 nM。BTK-IN-7 在酶 (ITK>250-fold, EGFR>2500-fold) 和细胞水平 (ITK>227-fold,EGFR27-fold) 都表现出较高的选择性。BTK-IN-7 表现出较高的抗肿瘤作用。 | |||
T61596 | EGFR/HER2/DHFR-IN-1 | ||
EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1]. | |||
T63205 |
HSP90-IN-13
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HSP90-IN-13(compound 5k)是一种有效的HSP90抑制剂,具有25.07 nM的IC50值,并对EGFR、VEGFR-2以及Topoisomerase-2展现出多靶点作用。此外,HSP90-IN-13能够在G2/M期阻滞MCF-7细胞周期,并通过线粒体途径诱导细胞凋亡(apoptosis)。 | |||
T63492 |
BI-1622
|
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BI-1622 是具有高度选择性的、口服具有活力的 HER2(ERBB2) 抑制剂 (IC50: 7 nM)。BI-1622对EGFR 的选择性大于 25 倍。在转染 H2170 和 PC9 细胞的移植瘤小鼠模型中,BI-1622 表现出较高的体内的抗肿瘤作用,具有良好的药物代谢和药代动力学特性。 | |||
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... | |||
T76721 | Zalutumumab | ||
Zalutumumab 是一种高亲和力的纯人类IgG1单克隆抗体,靶向EGFR。Zalutumumab 与表皮生长因子受体的结构域 III 结合,通过阻断表皮生长因子的结合和干扰受体的活性构象发挥作用。Zalutumumab 与IgG 及其 Fab 区段的EC50值分别为 7 和 19 nM。Zalutumumab 可用于癌症的研究。 | |||
T81380 | PROTAC EGFR degrader 7 diTFA | PROTACs | PROTAC |
PROTACEGFRdegrader 7 diTFA (compound 13b) 是高效且选择性的 CRBN 招募 PROTACEGFRL858R/T790M 降解剂,DC50 值为 13.2 nM。它在抑制 NCI-H1975 细胞增殖方面表现出强效,IC50 值为 46.82 nM,并且能够显着诱导这些细胞发生凋亡以及 G2/M 期的阻滞。PROTACEGFRdegrader 7 diTFA 展现了潜在的抗肿瘤活性,适合应用于非小细胞肺癌 (NSCLC) 的相关研究。 | |||
T81739 | Multi-target kinase inhibitor 2 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Multi-target kinase inhibitor 2 (compound 5K) 作为一种multi-targeted kinase抑制剂,对EGFR、Her2、VEGFR2和CDK2酶表现出强效活性,IC50值在40至204 nM之间。此化合物对包括HepG2、HeLa、MDA-MB-231 和 MCF-7在内的多种细胞系均显示出显著的细胞毒性,其IC50值分别为41、57、51 和 59 μM。此外,Multi-target kinase inhibitor 2 还能诱导HepG2细胞发生周期阻滞和凋亡 (apoptosis)。 | |||
T78792 |
Multi-kinase-IN-4
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Multi-kinase-IN-4 (compound 5d) 是一种针对VEGFR2、EGFR、HER2和CDK2的多靶点激酶抑制剂,其IC50值依次为0.33、0.22、0.18和2.09 μM。该化合物对包括HepG2、MCF-7、MDA-231 和 HeLa 在内的多种细胞系展现出强效的抗癌活性,IC50值范围为1.94至7.1 µM,对WI-38细胞线则显示较低毒性,IC50值为40.85 µM。它能诱导HepG2细胞发生apoptosis并在S期阻滞细胞周期,适用于癌症相关的生物学研究。 | |||
T79714 |
HDAC3-IN-2
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC3-IN-2 (compound 4i) 是一种具有纳摩尔级效力的吡嗪酰肼基HDAC3抑制剂,IC50值为14 nM,针对三阴性乳腺癌细胞表现出高效抑制作用。该化合物在细胞内毒性测定中显示,对4T1细胞株的IC50为0.55 μM,对MDA-MB-231细胞株的IC50为0.74 μM。HDAC3-IN-2通过增加乙酰化水平(如H3K9、H3K27和H4K12),促进细胞凋亡(涉及caspase-3、caspase-7和细胞色素c的水平提升),并抑制细胞增殖相关蛋白(如Bcl-2、CD44、EGFR和Ki-67)的表达,从而在荷瘤小鼠模型中表现出显著的体内抗肿瘤作用。 | |||
T81922 | LM2I | ||
LM2I是一种多杀菌素(SPA)衍生物,兼具精氨酸琥珀酸合成酶(ASS1)激活剂和针对ASS1的直接作用的肿瘤抑制剂功能。在7种结直肠癌细胞系和结直肠癌异种移植肿瘤中,LM2I展现出明显的抗增殖活性,并且通过EGFR途径阻断结直肠癌细胞增长。 | |||
T71082 |
DW532
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DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human ca... | |||
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... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T4S0544 |
Furanodienone
呋喃二烯酮,莪术呋喃二烯酮 |
Apoptosis; HER | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Furanodienone 是来源于姜黄根茎的一种主要生物活性成分,可诱导细胞凋亡。 |