IIIM-290 (CAS: 2213468-64-3 )
Background Information of IIIM-290
IIIM-290 is an orally active potent cyclin-dependent kinase inhibitor. IIIM-290 shows strong inhibition of Cdk-9/T1 (IC50 1.9 nM) kinase and Molt-4/MIAPaCa-2 cell growth (GI50<1.0 μM) and is found to be highly selective for cancer cells over normal fibroblast-cells. IIIM-290 inhibits the cell growth of MIAPaCa-2 cells via caspasedependent apoptosis. IIIM-290 achieves 71% oral bioavailability with in-vivo efficacy in pancreatic, colon and leukemia xenografts at 50 mg/kg, po.
Storage Condition of IIIM-290
Quality Control and Spectral Data
Mechanism and Indications
||Sponsor & Collaborators
||IIIM-290; IIIM 290; IIIM290.
Structure Information of IIIM-290
||C1(O)C2C(C=C(/C=C/C3C(Cl)=CC=CC=3Cl)OC=2C([[email protected]@]2([H])CCN(C)C[[email protected]]2O)=C(O)C=1)=O |&1:19,26|
Other Form Products of IIIM-290
Recommended Products in Same Target
Recommended Products in the Same Indication
Chemical and Physical Properties
||Solubility:Soluble in DMSO
.Bharate SB, et al. Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-dependent Kinase Inhibitor. J Med Chem. 2018 Jan 25.
Rohitukine (1), a chromone alkaloid isolated from Indian medicinal plant Dysoxylum binectariferum has inspired the discovery of flavopiridol and riviciclib, both of which are bioavailable only via IV route. With the objective to address oral bioavailability issue of this scaffold, four series of rohitukine derivatives were prepared and screened for Cdk inhibition and cellular antiproliferative activity. The 2,6-dichloro-styryl derivative IIIM-290 (11d) 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. It achieved 71% oral bioavailability with in-vivo efficacy in pancreatic, colon and leukemia xenografts at 50 mg/kg, po. It did not have CYP/ efflux-pump liability, was not mutagenic/genotoxic or cardiotoxic and was metabolically-stable. The preclinical data presented herein indicates the potential of 11d for advancement in clinical studies.