| Stereochemistry | ACHIRAL |
| Molecular Formula | C30H33N7O |
| Molecular Weight | 507.6293 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCN1C=C(C(=N1)C2=CC=C(NC(=O)N(C)C)C=C2)C3=C4C=C(NC4=NC=C3)C5=CC=CC(CN(C)C)=C5
InChI
InChIKey=QTBWCSQGBMPECM-UHFFFAOYSA-N
InChI=1S/C30H33N7O/c1-6-37-19-26(28(34-37)21-10-12-23(13-11-21)32-30(38)36(4)5)24-14-15-31-29-25(24)17-27(33-29)22-9-7-8-20(16-22)18-35(2)3/h7-17,19H,6,18H2,1-5H3,(H,31,33)(H,32,38)
GSK1070916 is a novel, azaindole derived, reversible and ATP-competitive inhibitor of the Aurora B/C kinases. GSK1070916 inhibits the proliferation of tumor cells and has antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models. Nemucore Medical Innovations and Cancer Research UK are developing NMI 900 (previously GSK 1070916) for the intravenous treatment of cancer. The product was originally developed by GlaxoSmithKline. A phase I/II trial in patients with solid tumours has been completed in the UK. Phase II development in ovarian cancer is underway in the US.
Originator
Approval Year
Doses
AEs
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
Drug as victim
Sourcing
PubMed
Sample Use Guides
Nemucore Medical Innovations and Cancer Research UK are developing NMI 900 (previously GSK 1070916A), a selective Aurora kinase B/C inhibitor, for the intravenous treatment of cancer, however, dosage of the drug is not disclosed. GSK1070916 was evaluated for its ability to inhibit the growth of various tumor xenografts in nude mice. Repeated i.p. administration at 25, 50, or 100 mg/kg once daily (5 consecutive days with 2 days off for up to three cycles) produced antitumor activity in all models evaluated with regressions (complete or partial).
Route of Administration:
Other
ACTIVE MOIETY
