Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10735 |
CDK4/6/1 Inhibitor
Crozbaciclib |
CDK | Cell Cycle/Checkpoint |
CDK4/6/1 Inhibitor (Crozbaciclib) 是一种 CDK4/6 抑制剂 (IC50s: 3 and 1 nM). CDK4/6抑制剂是一类用于治疗一些类型的激素受体阳性、her2阴性乳腺癌的化合物,可阻断了乳腺癌细胞分裂和繁殖的过程。 | |||
T13202 |
Trilaciclib hydrochloride
G1T28 hydrochloride |
CDK | Cell Cycle/Checkpoint |
Trilaciclib hydrochloride (G1T28 hydrochloride) 是一种CDK4/6的抑制剂,对 CDK4 和 CDK6 的IC50值分别为 1 nM 和 4 nM。 | |||
T21720 |
GP-82996
Cdk4/6 Inhibitor IV,CINK4 |
CDK | Cell Cycle/Checkpoint |
GP-82996 (CINK4) (CINK4) 是 CDK4/6的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡,可用于癌症研究。 | |||
T13202L |
Trilaciclib
G1T28 |
CDK | Cell Cycle/Checkpoint |
Trilaciclib is an inhibitor of CDK4/6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6, respectively). | |||
T60328 | CDK4/6-IN-12 | ||
CDK4/6-IN-12 是一种有效的细胞周期蛋白依赖性激酶 4/6 抑制剂。CDK4/6-IN-12 对 CDK4 和 CDK6 具有抑制活性,IC50值分别为 592.3 nM 和 3090 nM。 CDK4/6-IN-12 可用于癌症的研究。 | |||
T72393 | Crozbaciclib fumarate | ||
Crozbaciclib fumarate 是 CDK4/6的抑制剂,IC50值分别为 3 和 1 nM。 | |||
T11345 |
Lerociclib
G1T38 |
CDK | Cell Cycle/Checkpoint |
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 2nM, 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively. | |||
T75127 | CDK-IN-12 | ||
CDK-IN-12 (Example 20) 是一种CDK 抑制剂。CDK-IN-12 抑制 CDK4/6 的IC50值小于 20 nM。 | |||
T72951 |
CDK4/6-IN-14
|
||
CDK4/6-IN-14 是一种有效且高度选择性的 CDK4和 CDK6(CDK) 抑制剂,IC50分别为 10 nM 和 16 nM。CDK4/6-IN-14 的选择性是 CDK1、2、7 和 9 的 60 多倍,并且在其他 205 种激酶中表现出高选择性。 | |||
T61738 | CDK4/6-IN-7 | ||
CDK4/6-IN-7, a highly potent and selective orally active inhibitor of CDK4/6, demonstrates impressive inhibition activity with IC50 values of 1.58 nM and 4.09 nM respectively. This compound is particularly valuable for breast cancer research [1]. | |||
T79112 |
CDK4/6-IN-17
|
CDK | Cell Cycle/Checkpoint |
CDK4/6-IN-17(compound 12)为具有口服活性的CDK4/6抑制剂,在BE(2)细胞的IC50为10-100 nM。CDK4/6-IN-17在COLO205异种移植模型中有效抑制肿瘤生长。 | |||
T36967 |
LSN3106729 hydrochloride
|
||
LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods o... | |||
T73909 |
Abemaciclib metabolite M18
LSN3106729 |
Ligands for Target Protein for PROTAC | PROTAC |
Abemaciclibmetabolite M18 (LSN3106729) 是一种CDK抑制剂,具有抗肿瘤活性。作为Abemaciclib的代谢物,Abemaciclibmetabolite M18 能与CRBN配体结合,用于设计PROTAC CDK4/6降解剂。 | |||
T69197 | AG-012986 HCl | ||
AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hy... | |||
T69196 |
AG-012986
|
||
AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hy... | |||
T79572 |
MAPK-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MAPK-IN-2 (化合物3h)是一种携带抗肿瘤活性的高效MAPK抑制剂。它在多个癌细胞系中有效抑制了细胞增殖,并对MAPK途径表现出强大的抑制效果(EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, CDK4/6 IC50=95和184 nM),对突变型EGFR和B-RAF亦展现出高效力(EGFRT790M IC50=69 nM, B-RAFV600E IC50=83 nM)。 |