| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H21F2N7O2 |
| Molecular Weight | 417.4125 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)C1=NC2=C(C=CC=C2)N1C3=NC(=NC(=N3)N4CCOCC4)N5CCOCC5
InChI
InChIKey=HGVNLRPZOWWDKD-UHFFFAOYSA-N
InChI=1S/C19H21F2N7O2/c20-15(21)16-22-13-3-1-2-4-14(13)28(16)19-24-17(26-5-9-29-10-6-26)23-18(25-19)27-7-11-30-12-8-27/h1-4,15H,5-12H2
| Molecular Formula | C19H21F2N7O2 |
| Molecular Weight | 417.4125 |
| 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 |
ZSTK474 is a new PI3K inhibitor with strong antitumor activity against human cancer xenografts without toxic effects in critical organs. Specifically, ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. ZSTK474 blocks VEGF-induced cell migration and the tube formation in human umbilical vein endothelial cells (HUVECs), and inhibits the expression of HIF-1α and secretion of VEGF in RXF-631L cells, exhibiting potent in vitro antiangiogenic activity. ZSTK474 demonstrated prophylactic efficacy in a rat model of rheumatoid arthritis (RA) through inhibition of T cell and FLS functions.
CNS Activity
Originator
Approval Year
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
Drug as victim
Sourcing
PubMed
Patents
Sample Use Guides
ZSTK474 at 100, 200, or 400 mg/kg of mice body weight was orally administered daily from days 0 to 13.
Route of Administration:
Oral
Human prostate cancer PC3 cells growth inhibition was determined using the WST-8 assay kit. One hundred uL of cells (6 × 104 cells/mL) was seeded in 96-well plate and incubated at 37 °C. Twenty four hours later, 0.5 uL of various stock solutions of ZSTK474 was added. After further incubation for 48 h, 10 uL of WST-8 was added to each well and the cells were further incubated at 37 °C. Three hours later, the absorbances at 450 nm were measured with a microplate spectrophotometer.
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