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Datasheet of RGB286638
Description:. RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6. RGB-286638 inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. RGB-286638 demonstrated equimolar (50nM) activity in freshly isolated tumor cells from MM patients, while manifesting less cytotoxicity in healthy donor PBMCs. Treatment with RGB-286638 resulted in rapid downregulation of p-RNAPII S2/S5 across all tested MM cell lines. RGB-286638 (50nM) reduced the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but had no effects on p-Rb S780. in vivo: Dose-finding studies with RGB-286638 identified 40 mg/kg/day IV treatment as the maximum tolerated dose in SCID mice. Five days IV treatment with RGB-286638 significantly suppressed MM tumor growth, with maximum TGI (%) noted at day 14 following end of treatment at 85.06% and 86.34% in the 30 mg/kg and 40 mg/kg treated cohorts respectively.
Chemical Information Catalog
DC7768
Purity of current batch:
>98%
Molecular Weight (MW)
545.6
Molecular Formula
C29H37Cl2N7O4
CAS No.
784210-88-4
Solubility (25°C)
DMSO
Storage
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.