| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Molecular Weight | |
| Product Type | |
| Signaling Pathway | |
| Target |
Compound Overview
AG-012986 HCl (CAS 486414-32-8) is a research-grade small molecule supplied by TargetMol.
Physical Properties
| CAS Number | 486414-32-8 |
|---|---|
| Molecular Formula | C22H25Cl2F2N5O2S |
| Molecular Weight | 532.43 g/mol |
| Form | Solid |
| Shipping | Room Temperature (RT) |
Biological Activity
AG-012986 HCl 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 HCl 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 HCl was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 HCl also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.
Safety & Regulatory
For Research Use Only (RUO). Not for therapeutic, diagnostic, or clinical use. Wear appropriate PPE and consult the Safety Data Sheet (SDS) prior to handling.
It is not recommended to store DMSO stock solutions at room temperature. Once the stock solution is prepared, aliquot into single-use volumes and store at −20 °C (or −80 °C for sensitive compounds). Room-temperature storage accelerates chemical degradation and moisture uptake. When ready to use, thaw an aliquot at room temperature, use immediately, and avoid repeated freeze-thaw cycles.
Sonication time depends on compound solubility and concentration. In most cases, 1–3 minutes of intermittent bath sonication is sufficient to dissolve small molecule compounds in DMSO. For poorly soluble compounds, warming the solvent to 37–50 °C combined with brief vortexing between sonication pulses can improve dissolution. If the compound remains undissolved, prepare a more dilute stock solution.
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- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
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