cdk4/cyclind3

Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1 2 4 with Ki of 2 nM 3 nM 1 nM. It is less potent to CDK7 and GSK3α β, while inactive to other kinases. Phase 1.

ZDLD20 is an orally active and selective CDK4 inhibitor, a β-carboline analog with anti-HCT116 and anticancer activity that inhibits colony formation, inhibits invasion and migration, induces apoptosis, and prevents the G1 phase of the cell cycle.

AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11 16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

FD2056 is a potent, orally active PI3K inhibitor, with IC50 values of 0.30, 0.80, 1.10, and 0.42 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Additionally, it exhibits inhibitory effects on CDK2-CyclinA2 and CDK4-CyclinD3 with IC50s of 115.95 nM and 2782.15 nM. FD2056 effectively inhibits the proliferation of various breast cancer cell lines, such as MDA-MB-231, MDA-MB-468, and MCF-7, with IC50s of 1.06 μM, 0.04 μM, and 1.40 μM, respectively. The compound also promotes apoptosis in cancerous cells and has been shown to suppress tumor growth [1].

Palbociclib (PD 0332991) dihydrochloride is an orally active, selective inhibitor of CDK4 (IC50: 11 nM) and CDK6 (IC50: 16 nM), exhibiting anti-proliferative activity and inducing cell cycle arrest in HR-positive and HER2-negative breast cancers and hepatocellular carcinoma studies.

SR-3029 is a highly potent and specific inhibitor of CK1δ CK1ε.

AT7519 Hydrochloride (AT7519 HCl) is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.

Palbociclib-d8 (PD 0332991 D8) is the 2H-labeled form of Palbociclib. Palbociclib is an orally active CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11 16 nM). Palbociclib has anti-tumor activity and is used in research for estrogen receptor-positive and HER2-negative breast cancer.

RGB-286638 is a multi-target CDK inhibitor that effectively hampers the kinase activity of a range of cyclin-CDK complexes, including cyclin T1-CDK9 (IC50 = 1 nM), cyclin B1-CDK1 (IC50 = 2 nM), cyclin E-CDK2 (IC50 = 3 nM), cyclin D1-CDK4 (IC50 = 4 nM), cyclin E-CDK3 (IC50 = 5 nM), and p35-CDK5 (IC50 = 5 nM). Additionally, it inhibits other kinases such as GSK-3β (IC50 = 3 nM), TAK1 (IC50 = 5 nM), Jak2 (IC50 = 50 nM), and MEK1 (IC50 = 54 nM), showcasing its versatile inhibitory potential.

Palbociclib hydrochloride (pabociclib hydrochloride) is the salt form of Palbociclib, a selective and orally available CDK4 and CDK6 inhibitor with anti-tumor proliferative activity for use in breast and hepatocellular carcinoma.

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM 2 nM 3 nM 4 nM 5 nM for cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2 cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

AT7519 is a kinase inhibitor (IC50: 0.19, 0.044, 0.51, 0.067, 0.66 and 0.018 μM for CDK1/cyclinB, CDK2/CyclinA, CDK2/Cyclin E, CDk4/CyclinD1, CDK6/Cyclin D3, CDk5/p35).

Lerociclib (G1T38) is a selective and highly potent CDK4 6 inhibitor with anticancer and antitumor activity, inhibits CDK4 CyclinD1 and CDK6 CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended.

Ulecaciclib is an orally active, blood-brain barrier-transparent, cell cycle protein-dependent kinase (CDK) inhibitor that exhibits favorable pharmacokinetic profiles, with ki of 0.62 μM (CDK2 Cyclin A), 3 nM (CDK6 Cyclin D3), 0.2 nM (CDK4 Cyclin D1) and 0.63 μM (CDK7 Cyclin H) for CDKs. D1) and 0.63 μM (CDK7 Cyclin H).

Palbociclib (PD 0332991) orotate, an orally active selective inhibitor of CDK4 and CDK6, exhibits IC50 values of 11 and 16 nM, respectively. This compound demonstrates potent anti-proliferative effects and induces cell cycle arrest in cancer cells, applicable in research concerning HR-positive, HER2-negative breast cancer, and hepatocellular carcinoma [1] [3] [4].

Riviciclib hydrochloride (P276-00) is a novel inhibitor of CDK1, CDK4, and CDK9, with IC50 values of 79 nM, 63 nM, and 20 nM, respectively, currently in Phase 2 3.

RGB-286147 is a potent, selective, ATP-competitive Cdks inhibitor.

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

ZDLD13 is a β-carboline that exhibits potent anti-HCT116 activity inclusive of inhibition of invasion and migration, inhibition of colony formation, inducing of apoptosis as well as arresting of G1 phase in cell cycle. ZDLD13 is an orally active and selective inhibitor of CDK4 CycD3 (IC 50 = 0.38 μM) which exhibits significant inhibition of tumor growth in HCT116 tumor xenograft model [1].

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective CDK4 CDK6 inhibitor, with IC50 values of 2 nM for CDK6 CyclinD3 and 1 nM for CDK4 CyclinD1.