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PF-07104091 is an orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon administration, CDK2 inhibitor PF-07104091 selectively targets, binds to and inhibits the activity of CDK2. This may lead to cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. CDKs are serine/threonine kinases that are important regulators of cell cycle progression and cellular proliferation and are frequently overexpressed in tumor cells. CDK2/cyclin E complex plays an important role in retinoblastoma (Rb) protein phosphorylation and the G1-S phase cell cycle transition. CDK2/cyclin A complex plays an important role in DNA synthesis in S phase and the activation of CDK1/cyclin B for the G2-M phase cell cycle transition.
| Cell Experiment | |
|---|---|
| Cell lines | 1014 or B16F10 melanoma cells |
| Preparation method | After culturing 1014 or B16F10 melanoma cells in DMEM/F12 (1:1) with 10% FBS to 75% confluence, cells were treated with 20 μM Palbociclib and 20 μM PF-07104091 for 24 hours. |
| Concentrations | 20 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Female BALB/c nude mice |
| Formulation | Not mentioned |
| Dosages | 50 mg/kg |
| Administration | i.g. |
| Molecular Weight | 404.46 |
| Formula | C19H28N6O4 |
| CAS Number | 2460249-19-6 |
| Solubility (25°C) | DMSO 41 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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Flavopiridol (Alvocidib) is a competitive broad-spectrum CDK inhibitor with IC50 of 30,170,100 nM against CDK1, CDK2 and CDK4, respectively. |
| R547
R547 is a potent and selective ATP-competitive CDK inhibitor, with Ki values of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively. |
| JNJ-7706621
JNJ-7706621 is a dual cell cycle inhibitor with activity against cyclin-dependent kinases (CDK1, 2, 3, 6) with an IC50 of 3-175 nM and Aurora kinases (A and B) with an IC50 of 11-15 nM respectively. |
| PD 0332991 HCL
PD-0332991 HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. |
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