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Cat. No. | Product Name | Target | Signaling Pathways |
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T40183 |
FAK-IN-1
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FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27)). | |||
T64167 |
Ifebemtinib
IN-10018,BI-853520 |
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Ifebemtinib (BI-853520) 是一种具有口服活性和强效性的粘附斑激酶 (FAK) 抑制剂 (IC50=1 nM),具有抗肿瘤活性,可抑制恶性胸膜间皮瘤中的球状体形成和原位肿瘤生长,可用于研究乳腺癌和卵巢癌。 | |||
T61410 |
FAK-IN-8
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FAK-IN-8 (化合物 5h) 是一种FAK 抑制剂 (IC50=5.32 μM)。FAK-IN-8 具有较好的抗增殖活性,可用于癌症的研究。 | |||
T74802 | FAK-IN-9 | ||
FAK-IN-9 (Compound 8f) 是一种有效的和具有口服活性的FAK 抑制剂,其IC50为 27.44 nM。FAK-IN-9 诱导三阴性乳腺癌 (TNBC) 细胞凋亡(apoptosis)。 | |||
T63545 | FAK-IN-3 | ||
FAK-IN-3 是一种有效的粘着斑激酶 (FAK) 抑制剂。FAK-IN-3 能够减少 PA-1 细胞的迁移和侵袭,并抑制 MMP-2 和 MMP-9 的表达。FAK-IN-3 对肿瘤生长和转移具有抑制作用,且没有明显不良反应。FAK-IN-3 对卵巢癌表现出研究潜力。 | |||
T82420 |
FAK-IN-12
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FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
FAK-IN-12(Compound 12S)为FAK抑制剂,具有47 nM的IC50值。该化合物对MGC-803、HCT-116及KYSE30细胞系的增殖具有抑制作用(IC50值分别为0.24、0.45、0.44 μM),并可诱导细胞凋亡和细胞衰老。 | |||
T61019 | FAK-IN-4 | ||
FAK-IN-4 (Compound 7d) 具有抗癌活性,可以诱导细胞凋亡。FAK-IN-4 是FAK 的潜在抑制剂。 | |||
T79363 | APG-2449 | ROS Kinase | Tyrosine Kinase/Adaptors |
APG-2449为口服活性的ALK/ROS1/FAK抑制剂,在非小细胞肺癌(NSCLC)的小鼠模型中显示出显著的抗肿瘤效果。 | |||
T79688 |
FAK-IN-11
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FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
FAK-IN-11 (Compound 4l) 作为FAK抑制剂,与FAK的ATP结合袋相结合,进而抑制其蛋白磷酸化。该化合物对MDA-MB-231细胞具有细胞毒性,IC50值为 13.73μM,并能诱导该细胞通过非凋亡途径死亡。 | |||
T76736 | Abituzumab | ||
Abituzumab (DI17E6) 是一种人源化抗integrinαV 单克隆抗体 (IgG2 型)。Abituzumab 能有效减少FAK、Akt 和ERK 的磷酸化。Abituzumab 可用于癌症,尤其是前列腺癌的研究。 | |||
T73039 |
CYP1B1-IN-3
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CYP1B1-IN-3为选择性CYP1B1抑制剂,其IC50值分别针对CYP1B1、CYP1A1、CYP1A2为6.6, 347.3, >10000 nM。该化合物能够抑制细胞迁移与侵袭,并作用于P-gp、AKT/ERK、FAK/SRC及EMT信号通路。 | |||
T17133 |
Tos-PEG4-t-butyl ester
Tos-PEG4-Boc |
Others | Others |
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker characterized by its PEG composition. This compound plays a crucial role in the synthesis of a range of PROTACs, including BI-3663, a highly selective PTK2/FAK PROTAC. It employs cereblon ligands to target E3 ligases for the degradation of PTK2, exhibiting potent inhibitory activity with an IC50 of 18 nM[1]. | |||
T70352 |
PH11
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PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL... | |||
T83680 |
Azurin (50-77) (P. aeruginosa) TFA
Azurin p28,p28 |
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Azurin (50-77)是一种含铜细菌蛋白azurin的肽段,存在于P. aeruginosa中,具有细胞周期停滞、抑制癌细胞增殖和调节血管生成活性。作为VEGFR2的抑制剂(IC20约为10.7 µM),Azurin (50-77)(20 µM)能在MCF-7乳腺癌细胞中诱导G2/M期的细胞周期停滞。在50 µM的浓度下,减少MCF-7和ZR-75-1乳腺癌细胞的增殖。Azurin (50-77)以25 µM的浓度减少VEGF-A诱导的毛细管管腔形成(IC50 = 12 µM),降低人脐静脉内皮细胞(HUVECs)中与细胞膜相关的F-actin、焦点粘附激酶(FAK)和paxillin的水平,并增加胞外的血小板内皮细胞粘附分子-1(PECAM-1)的水平。在体内,Azurin (50-77)(每日10 mg/kg)在MCF-7小鼠异种移植模型中减少肿瘤体积。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T5S0761 |
Nitidine chloride
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Apoptosis; ERK; FAK; p38 MAPK; NF-κB; Topoisomerase; STAT; Parasite | Angiogenesis; Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors |
Nitidine chloride 是从Zanthoxylum nitidum (Roxb) DC 中分离得到的,具有抗疟疾活性。它通过多个靶点通路,起抗癌作用,抑制STAT3、DNA 拓扑异构酶1和2A、ERK 和c-Src/FAK 相关信号通路。它通过MAPK 和NF-kB 途径抑制Lps 诱导的炎性细胞因子的产生。 |