ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors 5-Pyrimidinecarboxamide, N-hydroxy-2-[4-(2-naphthalenylsulfonyl)-1-piperazinyl]- (9CI)

5-Pyrimidinecarboxamide, N-hydroxy-2-[4-(2-naphthalenylsulfonyl)-1-piperazinyl]- (9CI)

Product Name5-Pyrimidinecarboxamide, N-hydroxy-2-[4-(2-naphthalenylsulfonyl)-1-piperazinyl]- (9CI)
CAS604769-01-9
MFC19H19N5O4S
MW413.45
EINECS
MOL File604769-01-9.mol

Chemical Properties

Density	1.466
storage temp.	Store at 0-8 °C
form	Solid
pka	8.10±0.10(Predicted)
color	White to off-white

Usage And Synthesis

Uses

JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study[1].

in vivo

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 p21^waf1, ^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.

IC 50

HDAC1: 3.3 nM (IC₅₀); HDAC8: 23 nM (IC₅₀)

References

[1] Arts J, et al. R306465 is a novel potent inhibitor of class I histone deacetylases with broad-spectrum antitumoral activity against solid and haematological malignancies. Br J Cancer. 2007;97(10):1344-1353. DOI:10.1038/sj.bjc.6604025

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