T74127
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Others
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N-Desethyl Sunitinib (SU-12662) (hydrochloride) 是 Sunitinib 的代谢物。Sunitinib 是有效的,ATP 竞争的VEGFR,PDGFRβ和KIT 抑制剂,能够抑制VEGFR-1,VEGFR-2,VEGFR-3,PDGFRβ和 KIT 的活性,Ki 值分别为 2,9,17,8 和 4 nM。 |
T74001
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PROTACs
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INY-03-041 trihydrochloride 是一种有效的、高选择性的、基于PROTAC 的泛-AKT 降解剂,由ATP 竞争性AKT 抑制剂Ipatasertib 结合Lenalidomide 组成。INY-03-041 trihydrochloride 可抑制AKT1,AKT2和AKT3,IC50分别为 2.0 nM,6.8 nM 和 3.5 nM。 |
T72270
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Others
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WYE-687 dihydrochloride 是一种 ATP 竞争性的 mTOR 抑制剂,IC50为 7 nM。WYE-687 dihydrochloride 抑制mTORC1和mTORC2活化。WYE-687 也抑制PI3Kα和PI3Kγ,IC50分别为 81 nM 和 3.11 μM。 |
T38927
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Others
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SR-1277 is a highly potent, selective, and ATP competitive inhibitor of CK1δ/ε, with IC50 values of 49 nM and 260 nM, respectively. Additionally, SR-1277 exhibits inhibitory effects on FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K, with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. Taken together, SR-1277 represents a valuable tool for cancer research. |
T38462
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Others
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PF-04577806 is a potent, selective, and ATP competitive inhibitor of the protein kinase C (PKC). It exhibits significant inhibitory activity against various isoforms of PKC, including PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, with IC50 values of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. Furthermore, PF-04577806 has the ability to reverse retinal vascular leakage in diabetic rats. |
T68267
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Others
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RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf/MEK/ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation. |
T71736
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Others
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AMG-628, (R)- is the R isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation. |
T78934
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c-Met/HGFR
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c-Met-IN-18 是对 WT(Wild Type)和 D1228V 变异型 c-MET 具有 ATP 竞争性抑制作用的 III 型 c-MET 抑制剂。该化合物对 WT/D1228V 显示出不同程度的抑制活性,其 IC50 值分别为 0.013/0.20μM。c-Met-IN-18 主要用于研究 c-MET 驱动的癌症。 |
T63650
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Others
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Samuraciclib (CT7001) hydrochloride hydrate 是有效的、选择性、ATP 竞争性的、口服具有活力的 CDK7 抑制剂 (IC50: 41 nM)。Samuraciclib hydrochloride hydrate 对 CDK7的选择性分别是 CDK1,CDK2 (IC50为 578 nM),CDK5 和 CDK9 的 45 倍,15 倍,230 倍和 30 倍。Samuraciclib hydrochloride hydrate 能够抑制乳腺癌细胞系的生长 (GI50: 0.2-0.3 μM),表现出有效的抗肿瘤效果。 |
T68523
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Others
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AMG-628, (S)-, is the S isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation. |