RGB-286638 is a multitargeted cyclin-dependent kinase inhibitor. RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. GB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo. RGB-286638 displayed caspase-dependent apoptosis in both wt-p53 and mutant-p53 cells that was closely associated with the downregulation of RNA polymerase II phosphorylation and inhibition of transcription. RGB-286638 triggered p53 accumulation via nucleolar stress and loss of Mdm2, accompanied by induction of p53 DNA-binding activity.
MedKoo Cat#: 206738
Name: RGB-286638 free base
CAS#: 784210-88-4 (free base)
Chemical Formula: C29H35N7O4
Exact Mass: 545.2751
Molecular Weight: 545.64
Elemental Analysis: C, 63.84; H, 6.47; N, 17.97; O, 11.73
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 2.6 | 4.77 |
The following data is based on the product molecular weight 545.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
