T41100
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Volasertib (BI 6727) trihydrochloride is a dihydropteridinone derivative that exhibits potent and selective inhibition of Polo-like kinase 1 (PLK1), PLK2, and PLK3. It acts as an orally active ATP-competitive inhibitor with an IC50 of 0.87 nM against PLK1. Additionally, Volasertib trihydrochloride demonstrates IC50 values of 5 nM and 56 nM against PLK2 and PLK3, respectively. Its mechanism of action includes inducing mitotic arrest and apoptosis. Furthermore, Volasertib trihydrochloride has been shown to possess significant antitumor activity in various cancer models. |
T61431
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Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1]. |
T63984
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PF-3758309 dihydrochloride 是一种有效的、可逆的、口服具有活力的、 ATP 竞争性的 PAK4 抑制剂,其 Kd 值为 2.7 nM,Ki 值为 18.7 nM。PF-3758309 dihydrochloride 显示出 PAK4 抑制剂的预期细胞功能,能够抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。 |
T71097
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DC-120 is an ATP competitive AKT kinase inhibitor that suppressed proliferation and induced apoptosis in liver cancer cells both in vitro and in vivo. DC120 blocked the phosphorylation of downstream molecules in the AKT signal pathway in dose- and time-dependent manners both in vitro and in vivo. DC120 inhibits AKT activity in vitro with an EC(50) of 153 nM. DC120 at 20 mg/kg/day inhibited the CNE2 xenograft tumor growth with a treated group/control group ratio of 38.1%, accompanied by increasing terminal deoxynucleotidyl transferasedUTP nick-end labeling-positive cells in the tumor sample. |
T74000
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VEGFR
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CP-547632 TFA是一款口服效果显著的ATP競爭性抑制劑,针对VEGFR-2和FGF激酶具有高度选择性,IC50值分别为11 nM和9 nM。该化合物相较于EGFR和PDGFRβ,对VEGFR2和bFGF展现出更高的选择性,优于相关的酪氨酸激酶(TKs)。CP-547632 TFA还显示了显著的抗肿瘤活性。 |
T72431
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Theliatinib (Xiliertinib) tartrate 是一种有效、ATP 竞争性、口服活性和高度选择性的EGFR 抑制剂,Ki 为 0.05 nM,IC50为 3 nM。Theliatinib 对EGFRT790M/L858R 突变体的IC50值为 22 nM。Theliatinib 对EGFR 的选择性是其他激酶的 50 倍以上。 |
T21675
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Adezmapimod (SB 203580) hydrochloride 是一种选择性的,ATP 竞争性的 p38 MAPK 抑制剂,其对于SAPK2a/p38和SAPK2b/p38β2的IC50分别为 50 nM 和 500 nM。Adezmapimod hydrochloride 抑制 LCK,GSK3β 和 PKBα,IC50比 SAPK2a/p38 高 100-500 倍。Adezmapimod hydrochloride 也是一种自噬 (autophagy) 和有丝分裂 (mitophagy) 激活剂。 |
T68546
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PF-00337210 is an orally available ATP-competitive inhibitor of the vascular endothelial growth factor receptor type 2 (VEGFR2), with potential anti-angiogenesis and antineoplastic activities. Upon administration, the VEGFR2 tyrosine kinase inhibitor PF-00337210 selectively binds to VEGFR2 and prevents its phosphorylation which may result in an inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and may eventually cause tumor cell death. VEGFR2, a receptor tyrosine kinase, is frequently overexpressed by a variety of tumor types. |
T78753
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Aurora Kinase
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Aurora Kinases-IN-4(Compound 11c)是共价ATP竞争型aurora kinaseA抑制剂,具有IC50为1.7 nM。该化合物对SJSA-1、MDA-MB-231、A549和HeLa细胞系的增殖抑制效果显著,其IC50分别为4.27、1.54、3.08和6.99 μM。Aurora Kinases-IN-4适用于三阴性乳腺癌(TNBC)的相关研究。 |
T38653
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HG-7-85-01 is a type II ATP competitive inhibitor targeting wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. It effectively inhibits T315I mutant Bcr-Abl kinase, as well as KDR and RET kinases with IC50 values of 3 nM, 20 nM, and 30 nM, respectively. In contrast, HG-7-85-01 exhibits weak or no inhibition towards other kinases (IC50 >2 μM). Furthermore, this compound inhibits cell proliferation through the induction of apoptosis and by impeding cell-cycle progression. |