| Stereochemistry | ACHIRAL |
| Molecular Formula | C29H35N7O4 |
| Molecular Weight | 545.6327 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COCCN1CCN(CC2=CC=C(C=C2)C3=NNC4=C3C(=O)C5=C4C=CC=C5NC(=O)NN6CCOCC6)CC1
InChI
InChIKey=XLSYZSRXVVCHLS-UHFFFAOYSA-N
InChI=1S/C29H35N7O4/c1-39-16-13-34-9-11-35(12-10-34)19-20-5-7-21(8-6-20)26-25-27(32-31-26)22-3-2-4-23(24(22)28(25)37)30-29(38)33-36-14-17-40-18-15-36/h2-8H,9-19H2,1H3,(H,31,32)(H2,30,33,38)
| Molecular Formula | C29H35N7O4 |
| Molecular Weight | 545.6327 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
RGB-286638 is a multi-targeted protein kinase inhibitor currently in Phase 1 clinical testing. In vitro cell-free kinase assays indicated that RGB-286638 inhibits CDK1, 2, 3, 4, 5, and 9 and is less active against CDK6 and 7. The RGB-286638 compound has been shown to inhibit the processes controlling cell division in cancer cells by targeting multiple cyclin-dependent kinase proteins involved in regulating the cell cycle. RGB-286638 has also been shown to induce apoptosis (programmed cell death) and to inhibit other important protein kinases involved in the proliferation of cancer cells. RGB-286638 treatment results in tumor regression and increased survival in a number of pre-clinical models of solid and hematological tumors.
Originator
Approval Year
AUC
T1/2
PubMed
Patents
Sample Use Guides
The dose levels studied
were 10, 20, 40, 80, 120, and 160 mg administered i.v. on
days 1 to 5 within 1 hour, with cycles repeated once every
28 days. In this first in human phase I study in patients with solid
tumors the recommended dose of RGB-286638 for phase II
studies was identified at 120 mg/d i.v. at 1 to 5 days every 4
weeks, given through a central venous line preceded by
antiemetics.
Route of Administration:
Intravenous
