IIIM-290 is a potent and Orally Active Cyclin-dependent Kinase Inhibitor. IIIM-290 showed strong inhibition of Cdk-9/T1 (IC50 1.9 nM) kinase and Molt-4/MIAPaCa-2 cell growth (GI50 < 1.0 µM) and was found to be highly selective for cancer cells over normal fibroblast-cells. It inhibited the cell growth of MIAPaCa-2 cells via caspase-dependent apoptosis. IIIM-290 achieved 71% oral bioavailability with in-vivo efficacy in pancreatic, colon and leukemia xenografts at 50 mg/kg, po. IIIM-290 did not have CYP/ efflux-pump liability, was not mutagenic/genotoxic or cardiotoxic and was metabolically-stable.
MedKoo Cat#: 407878
Name: IIIM-290
CAS#: 2231082-67-8 (free base)
Chemical Formula: C23H21Cl2NO5
Exact Mass: 461.0797
Molecular Weight: 462.32
Elemental Analysis: C, 59.75; H, 4.58; Cl, 15.34; N, 3.03; O, 17.30
The following data is based on the product molecular weight 462.32 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 |
