Belinostat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 HDAC 抑制剂，IC50 为 27 nM。

A potent HDAC inhibitor with IC50 of 27 nM (HeLa cell extracts); inhibits histone deacetylase activity in cell lysates with IC50 of 9-100 nM, increases the acetylation of histone H4 and induces apoptosis in tumor cell lines; inhibits the growth of a range of human tumor cell lines in vitro (IC50=0.2-3.4 uM); shows antitumor activity in vivo with no apparent toxicity.Blood Cancer Approved.

Belinostat (PXD101) induces a concentration-dependent (0.2-5 μM) increase in acetylation of histone H4 in tumor cell lines. Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range 0.2-3.4 μM as determined by a clonogenic assay and induces apoptosis. Belinostat inhibits the growth of a number of human tumor cell lines in vitro with IC50s determined by a clonogenic assay in the range 0.2-3.4 μM. Belinostat (PXD101) is a potent histone deacetylase (HDAC) inhibitor, potently inhibits the enzymatic activity of purified recombinant HDAC6 (IC50 of 82 nM).

Treatment of nude mice bearing human ovarian and colon tumor xenografts with Belinostat (10-40 mg/kg/day i.p.) daily for 7 days causes a significant dose-dependent growth delay with no obvious signs of toxicity to the mice. Growth delay is also observed for xenografts of cisplatin-resistant ovarian tumor cells. A marked increase in acetylation of H4 is detected in blood and tumor of mice 3 h after treatment with Belinostat (PXD101). The inhibition of growth of human tumor xenografts in mice, with no apparent toxicity. Belinostat (PXD101) displays single-agent antitumor activity on human A2780 ovarian cancer s.c. xenografts which is enhanced via combination therapy with Carboplatin.

PXD101 | PX105684 | PXD-101 | PXD 101 | PX-105684

Cell Cycle/DNA Damage

HDAC

HDAC

Cancer

Blood cancer

866323-14-0

318.3477

C15H14N2O4S

>98% (HPLC)

10 mM in DMSO

O=C(NO)/C=C/C1=CC=CC(S(=O)(NC2=CC=CC=C2)=O)=C1

2-Propenamide, N-hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-, (2E)-

(-20℃)

With Ice Pack

≥ 2 years