T77440
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Codrituzumab (GC3)是一种人源化针对 glypican-3 肝癌蛋白的抗体,可与索拉非尼联合使用来研究不可治愈的晚期肝细胞癌 (HCC) 。 |
T14997
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FAK
PYK2
ALK
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Conteltinib (CT-707) 是一种靶向FAK、ALK 和 Pyk2 的酶抑制剂,具有抗肿瘤活性。Conteltinib 对 FAK 有明显的抑制作用,通过抑制 YAP 信号传导来克服肝细胞癌中缺氧介导的索拉非尼耐药性,可用于晚期 ALK 阳性非小细胞肺癌和淋巴癌。 |
T7897
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Others
Antibacterial
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PK150 是一种 Sorafenib 类似物,具有抗菌活性。它抑制甲氧西林敏感金黄色葡萄球菌,耐甲氧西林金黄色葡萄球菌,万古霉素中介金黄色葡萄球菌的 MIC 分别为 0.3,0.3-1,0.3 µM。 |
T8478
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Apoptosis
Phosphatase
STAT
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SC-43 是一种具有口服活性的SHP-1 (PTPN6)激动剂。它是Sorafenib 的衍生物,可抑制STAT3的磷酸化并诱导细胞凋亡,具有抗纤维化和抗癌作用。 |
T28697
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SC-2001 is a MCL-1 inhibitor. SC-2001 inhibits STAT3 phosphorylation through enhancing SHP-1 expression and induces apoptosis in human breast cancer cells. SC-2001 overcomes STAT3-mediated sorafenib resistance through RFX-1/SHP-1 activation in hepatocellu |
T79407
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Others
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HL23是一种HDAC抑制剂,对抗HCC具有活性。通过增强TXNIP启动子乙酰化,此化合物上调TXNIP表达,进而介导钾通道活性并触发TXNIP依赖性钾剥夺,抑制HCC的进展和转移。HL23与Sorafenib联合应用时显示出协同作用,并且其效力超过Sorafenib与Vorinostat的联用。 |
T71783
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Oxythiamine chloride HCl is a thiamine antimetabolite that has anticancer activities. It is converted by thiamine pyrophosphokinase to oxythiamine pyrophosphate, a transketolase inhibitor. Oxythiamine decreases transketolase activity in breast cancer. It inhibits the nonoxidative synthesis of ribose and decreases RNA and DNA synthesis in pancreatic cancer. In vivo, oxythiamine induces cell cycle arrest at the G1 phase and apoptosis in an adenocarcinoma model. Oxythiamine, in combination with sorafenib, reduces tumor growth in an SMMC mouse xenograft model and has also been used to induce thiamine deficiency in mice. |
T36882
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CAY10773 is a derivative of the ferroptosis inducer sorafenib .1It selectively inhibits proliferation of BEL-7402, MGC803, and T24 bladder cancer cells (IC50s = 5.77, 5.21 and 3.97 μM, respectively) over non-cancerous HCV-29 cells (IC50= 23.19 μM). CAY10773 induces apoptosis in T24 cells when used at concentrations ranging from 2 to 6 μM but induces ferroptosis at concentrations greater than or equal to 6 μM with 10 hour or longer incubation times. It increases the production of reactive oxygen species (ROS) and decreases the mitochondrial membrane potential in T24 cells. CAY10773 (≥6 μM) also induces autophagy with incubation times longer than eight hours.
1.Chen, J.-N., Li, T., Cheng, L., et al.Synthesis and in vitro anti-bladder cancer activity evaluation of quinazolinyl-arylurea derivativesEur. J. Med. Chem.205112661(2020) |