ωpentadecalactone

CDK4 6 1 Inhibitor (Crozbaciclib) is a type of CDK4 6 inhibitor (IC50s: 3 and 1 nM). CDK4 6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4 6, exhibiting IC50 values of 1.5 μM for CDK4 cyclin D1, 5.6 μM for CDK6 cyclin D1, and 25 μM for Cdk5 p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

PU02 (6-[(1-Naphthalenylmethyl)thio]-9H-purine) is a potent and selective antagonist of 5-HT3 receptor.

Trilaciclib hydrochloride (G1T28 hydrochloride) is an inhibitor of CDK4 6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6).

CDK4 6-IN-22 (Compound 1-A) is a dual inhibitor of CDK4 and CDK6.

Trilaciclib is an inhibitor of CDK4 6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6, respectively).

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 of use. WO2017185031A1.

CDK4 6-IN-17 (compound 12) is an orally bioavailable inhibitor of CDK4 6, exhibiting potent activity with IC50 values between 10-100 nM in BE(2) cells, and has demonstrated efficacy in inhibiting tumor growth in the COLO205 xenograft model [1].

MAPK-IN-2 (compound 3h) is an efficacious MAPK inhibitor with antineoplastic properties that significantly hinders proliferation across various cancer cell lines. It demonstrates robust suppression of the MAPK pathway (EGFR WT IC50 = 281 nM, c-MET IC50 = 205 nM, B-RAF WT IC50 = 112 nM, CDK4 6 IC50 = 95 and 184 nM, respectively) and exhibits pronounced activity against mutated forms of EGFR and B-RAF (EGFR T790M IC50 = 69 nM and B-RAF V600E IC50 = 83 nM) [1].

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].

CDK4 6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4 6), with inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It shows over 60-fold selectivity for CDK4 6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against 205 other kinases.

Crozbaciclib fumarate is a CDK4 6 inhibitor with IC50 values of 3 and 1 nM, respectively.

YY173 is a dual inhibitor of CDK4 and CDK6, with IC50 values of 7.7 and 88 nM, respectively. It inhibits the proliferation of Jurkat cells with an IC50 of 1.46 μM. Additionally, YY173 can be utilized in the synthesis of PROTAC CDK4 6 degrader 1.

CDK-IN-12 (Example 20), a CDK inhibitor, effectively inhibits CDK4 6, demonstrating IC50 values below 20 nM [1].

Abemaciclib metabolite M18 (LSN3106729) is a potent cyclin-dependent kinase (CDK) inhibitor with antitumor properties. It has been incorporated alongside a cereblon (CRBN) ligand to develop a proteolysis-targeting chimera (PROTAC) that selectively degrades CDK4 6 [1] [2].

CDK4 6-IN-12 is a potent cyclin-dependent kinase 4 6 (CDK4 6) inhibitor with enzymatic inhibitory activity against CDK4 and CDK6, having IC50 values of 592.3 nM and 3090 nM, respectively. CDK4 6-IN-12 can be used in cancer research[1].