JNJ-16241199 (R306465) inhibits proliferation in acute lymphoblastic leukaemia (ALL), AML, chronic lymphoblastic leukaemia (CLL), chronic myeloid leukaemia (CML), lymphoma and myeloma tumour cells (IC50 values = 15–486 nM) [1].
JNJ-16241199 inhibits the primary human mammary epithelial cell (HMEC) proliferation with the IC50 of 32 nM, and is insensitive to quiescent, non-proliferative HMEC cells (IC50 = 7815 nM) [1].
JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) induces apoptosis and inhibits angiogenesis in A2780 cell line[1].
| Animal Model: | Human A2780, H460 and HCT116 orthotopic xenograft tumor models[1] |
| Dosage: | 10-40 mpk/day for 28 days |
| Administration: | Oral gavage (p.o.) |
| Result: | Induced H3 acetylation and p21waf1, cip1 promoter activity in A2780 ovarian tumour tissue.
Decreased tumour volume in three orthotopic xenograft tumor models.
Reached maximal decrease in final tumour volume to 76–87% in human A2780 orthotopic xenograft tumor models.
|
![5-Pyrimidinecarboxamide, N-hydroxy-2-[4-(2-naphthalenylsulfonyl)-1-piperazinyl]- (9CI) Structure](https://www.chemicalbook.com/CAS/GIF/604769-01-9.gif)
