Description

Product Description

Abemaciclib is a small-molecule, ATP-competitive inhibitor that selectively targets cyclin-dependent kinases CDK4 and CDK6. These kinases are key regulators of the G1-to-S phase transition in the cell cycle. By inhibiting CDK4/6 activity, abemaciclib prevents phosphorylation of the retinoblastoma protein (Rb), maintaining it in its active form and enforcing G1 phase arrest.

In laboratory research, abemaciclib is used to investigate:

• Cell-cycle checkpoints and proliferation control in cancer cells.

• Mechanisms of CDK4/6-dependent transcriptional regulation.

• Resistance pathways and compensatory signaling in tumor models.

• Combination studies with hormone receptor modulators, chemotherapeutics, or targeted therapies.

Chemically, abemaciclib is defined as N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-(4-fluorophenyl)-2-[(pyrimidin-2-yl)amino]benzamide. Its design allows high selectivity for CDK4/6 over other CDKs, minimizing off-target effects and enabling precise studies of G1 arrest and cell proliferation dynamics.

Researchers frequently utilize abemaciclib to model tumor suppression mechanisms, investigate Rb-dependent transcriptional regulation, and explore synergistic effects with inhibitors of signaling pathways such as PI3K/AKT/mTOR or ER signaling. In vitro and ex vivo assays often measure phosphorylation status of Rb, downstream cyclins, and transcription factors as readouts of CDK4/6 inhibition.

Product Specifications

Mechanism of Action

Abemaciclib is a selective ATP-competitive inhibitor of CDK4 and CDK6, preventing phosphorylation of the retinoblastoma protein (Rb). This blockade halts progression from G1 to S phase in the cell cycle, suppressing DNA synthesis and cell proliferation.

1. CDK4/6 Inhibition

Abemaciclib binds to the ATP-binding pocket of CDK4/6, inhibiting kinase activity and preventing cyclin D-mediated phosphorylation of Rb. This maintains Rb in its hypophosphorylated, active state.

2. Cell-Cycle Arrest

The active Rb inhibits E2F transcription factors, reducing the expression of genes required for S-phase entry, resulting in G1 phase arrest. Researchers monitor cell-cycle profiles using flow cytometry or molecular assays to quantify G1 accumulation.

3. Downstream Effects

Inhibition of CDK4/6 modulates downstream cyclins (Cyclin E, Cyclin A) and other cell-cycle regulators. Additionally, transcriptional changes affect apoptosis, DNA repair pathways, and tumor suppressor signaling, providing a platform to study compensatory mechanisms in cancer models.

4. Research Applications

• Modeling tumor response to CDK4/6 inhibition.

• Studying resistance mechanisms to kinase-targeted therapy.

• Evaluating combination effects with endocrine therapies or chemotherapy agents.

• Investigating transcriptional and epigenetic regulation in G1-arrested cells.

  

Side Effects

In preclinical research, abemaciclib exhibits potent G1 arrest with minimal off-target cytotoxicity at appropriate concentrations. Observed laboratory effects may include:

• Dose-dependent reduction in proliferation of Rb-positive cells.

• Mild induction of apoptosis in sensitive cancer cell lines.

• Changes in mitochondrial function or ROS levels at high doses.

These are experimental observations; the compound is not intended for human or veterinary use.

Keywords

Abemaciclib, CAS 1231929-97-7, CDK4/6 inhibitor, G1 phase arrest, cell-cycle regulation, tumor proliferation research, oncology research chemical, high-purity small molecule, research chemical supplier, OEM & bulk production China.

Shipping Guarantee

All Abemaciclib shipments are handled using validated cold-chain logistics to preserve compound integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We Abemaciclib ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

Payment Support

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Disclaimer

All Abemaciclib products listed are intended for laboratory research use only and not for human or veterinary use. They are not drugs, medical devices, or diagnostics and should not be administered to humans or animals. Researchers must handle all materials in accordance with institutional biosafety and chemical safety guidelines. The information provided is for scientific reference only and does not imply therapeutic efficacy, safety, or regulatory approval.