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Cat. No.	Product Name	Target	Signaling Pathways
T39957	CDK4/6-IN-6	CDK	Cell Cycle/Checkpoint
	CDK4/6-IN-6 是CDK4/CDK6的有效抑制剂，结合CDK4/Cyclin D1 和 CDK6/Cyclin D3 的 Ki 为 0.6 nM 和 13.9 nM。
T10736	CDK4/6-IN-2	CDK	Cell Cycle/Checkpoint
	CDK4/6-IN-2 是一种CDK4和CDK6抑制剂，IC50分别为 2.7 和 16 nM。
T39956	CDK4/6-IN-5 CDK4/6-IN-5
	CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively (WO2019207463A1, example A93).
T10737	CDK4/6-IN-3	CDK	Cell Cycle/Checkpoint
	CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM) used for the treatment of glioblastoma. It inhibits CDK1 with a Ki of 110 nM.
T10738	Abemaciclib metabolite M20 CDK4/6-IN-4,LSN3106726	CDK	Cell Cycle/Checkpoint
	Abemaciclib metabolite M20 (CDK4/6-IN-4) 是 Abemaciclib 的活性代谢物。 Abemaciclib metabolite M20 是一种特异性 CDK4/6 抑制剂，可用于癌症治疗的相关研究。
T67780	AM5992 CDK4/6-IN-16	CDK	Cell Cycle/Checkpoint
	AM5992 (化合物195) 是有效的CDK4和CDK6抑制剂（CDK4，IC50=0.013μM）。AM5992可用于CDK4介导的疾病的研究。
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。
T74370	CDK4/6-IN-11
	CDK4/6-IN-11 是一种有效的PROTACCDK4/6降解剂。
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。
T64244	CDK4/6-IN-10
	CDK4/6-IN-10 是一种选择性的、有效的、口服具有活力的 CDK4 (IC50: 22 nM) 和 CDK6 (IC50: 10 nM) 抑制剂，具有抗肿瘤效果。CDK4/6-IN-10 具有潜力进行多发性骨髓瘤 (MM) 的研究。
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。
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].
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。
T62192	CDK4/6-IN-9
	CDK4/6-IN-9 (compound 10) 是一种 CDK4/6 的选择性抑制剂，能够作用于 CDK6/cyclin D1 (IC50: 905 nM)。CDK4/6-IN-9 对多发性骨髓瘤 (MM) 具有潜在的研究价值。
T61892	CDK4/6-IN-8
	CDK4/6-IN-8 (Compound 7p) 是选择性的CDK4（IC50= 5.01 nM）和CDK6（IC50= 3.97 nM）抑制剂。
T72928	CDK4/6-IN-15
	CDK4/6-IN-15 是一种口服有效和选择性 CDK4/6抑制剂。CDK4/6-IN-15 能有效抑制癌细胞生长。CDK4/6-IN-15 将细胞周期阻滞在 G1 期，并抑制视网膜母细胞瘤肿瘤抑制蛋白 (Rb) 在 S780 位点的磷酸化和 E2 因子 (E2F) 调控的基因表达。
T62605	CDK4/6-IN-13
	作为CDK4/6抑制剂。化合物10b 和10c 在CDK4/6上表现出低纳摩尔范围的活性，理想的抗增殖活性，优异的代谢性质和可接受的药代动力学特性。
T75029	HEMTAC CDK4/6 degrader 1
	HEMTAC CDK4/6 degrader 1 是一种通过连接HSP90的配体和CDK4/6而形成的PROTAC，其Kd值为35.7 µM。在B16F10黑色素瘤细胞中，该化合物能够诱导CDK4/6的降解，从而将细胞周期阻滞在G0/G1期，并引发细胞凋亡。因此，HEMTAC CDK4/6 degrader 1可被应用于癌症研究领域。
T36694	XY028-140 XY028-140	CDK; Ligand for E3 Ligase	Cell Cycle/Checkpoint; PROTAC
	XY028-140 是一种特异性 CDK4/CDK6 降解，抑制 CDK4/6 在癌细胞中的表达和活性。 XY028-140 是一种 PROTAC，由 Cereblon 配体和 CDK 配体相连接。
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。
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。
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...
T63199	Dalpiciclib hydrochloride
	Dalpiciclib (SHR-6390) hydrochloride 是高度选择性的、口服具有活力的CDK4/6抑制剂，他们的IC50值分别为 12.4 nM 和 9.9 nM，能够作用于乳腺癌和食道鳞状细胞癌，具有出抗肿瘤作用。
T35476	BSJ-04-132
	Selective Cdk4 degrader. Degrades Cdk4 in Molt-4 cells, with no effect on Cdk6 levels. Displays cereblon-dependent degradation. Jiang et al (2019) Development of dual and selective degraders of cyclin-dependent kinases 4 and 6. Angew.Chem.Int.Ed.Engl. 58 6321 PMID:30802347
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）。

化合物

Cat.No: T39957

Target: CDK

Cat.No: T10736

Target: CDK

Cat.No: T39956

Synonym: CDK4/6-IN-5

Cat.No: T10737

Target: CDK

Abemaciclib metabolite M20

Cat.No: T10738

Synonym: CDK4/6-IN-4,LSN3106726

Target: CDK

Cat.No: T67780

Synonym: CDK4/6-IN-16

Target: CDK

CDK4/6/1 Inhibitor

Cat.No: T10735

Synonym: Crozbaciclib

Target: CDK

Cat.No: T74370

Cat.No: T72951

Cat.No: T64244

Cat.No: T79112

Target: CDK

Cat.No: T61738

Cat.No: T60328

Cat.No: T62192

Cat.No: T61892

Cat.No: T72928

Cat.No: T62605

HEMTAC CDK4/6 degrader 1

Cat.No: T75029

Cat.No: T36694

Synonym: XY028-140

Target: CDK, Ligand for E3 Ligase

Cat.No: T21720

Synonym: Cdk4/6 Inhibitor IV,CINK4

Target: CDK

Cat.No: T75127

LSN3106729 hydrochloride

Cat.No: T36967

Dalpiciclib hydrochloride

Cat.No: T63199

Cat.No: T35476

Cat.No: T69197

Cat.No: T69196

Cat.No: T79572

Target: EGFR

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