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Belinostat (PXD101)

(CAS No:414864-00-9)
Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.
CAS No:414864-00-9
Molecular Weight(MW):318.35
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 414864-00-9
Molecular formula(MF) C15H14N2O4S
Molecular Weight(MW): 318.35
Alias
Solubility
In vitro DMSO 64 mg/mL (201.03 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 10mg/mL
Biological Activity
Description Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.
Features Lead compound of Topotarget.
Targets
HDAC [1]
(Cell-free assay)
27 nM
In vitro

Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780 cells. Belinostat could induce apoptosis through PARP cleavage and acetylation of histones H3/H4. [1] Belinostat inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase and increase in G2-M phase. [2] The growth inhibitory activity of belinostat on cell lines is not strongly influenced by the multidrug-resistant phenotype, whereas the activity of docetaxel is clearly affected. Belinostat could enhance the growth inhibitory activity of docetaxel or carboplatin in OVCAR-3 and A2780 cells. Belinostat also shows enhanced tubulin acetylation in ovarian cancer cell lines. [3] A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB4 Cell Viability Assay 0.2/2 μM 24/48/72 h decreases cell viability in both time and dose dependent manner 25864732
HL-60  Cell Viability Assay 0.2/2 μM 24/48/72 h decreases cell viability in both time and dose dependent manner 25864732
NB4 Function Assay 2 μM 24/48 h blocks cell cycle in S phase 25864732
HL-60  Function Assay 2 μM 24/48 h blocks cell cycle in S phase 25864732
NB4 Function Assay 0.2 μM 24/48/72 h enhances RA-induced granulocytic differentiation 25864732
HL-60  Function Assay 0.2 μM 24/48/72 h enhances RA-induced granulocytic differentiation 25864732
PANC-1 Function Assay 10 μM 2/4/6 h DMSO induces AMPK activation 23743198
PANC-1 Cell Viability Assay 1/10 μM 48 h DMSO decreases cell viability in a dose dependent manner 23743198
PANC-1 Function Assay 10 μM 2/4 h DMSO increases intracellular ROS level 23743198
H1666 Growth Inhibition Assay 72 h DMSO IC50>10 μM 23515752
H460 Growth Inhibition Assay 72 h DMSO IC50=0.86 μM 23515752
H1299 Growth Inhibition Assay 72 h DMSO IC50=1.2 μM 23515752
H520 Growth Inhibition Assay 72 h DMSO IC50=0.75 μM 23515752
H1975 Growth Inhibition Assay 72 h DMSO IC50=0.68 μM 23515752
H1650 Growth Inhibition Assay 72 h DMSO IC50=0.88 μM 23515752
H820 Growth Inhibition Assay 72 h DMSO IC50=0.4 μM 23515752
PC9 Growth Inhibition Assay 72 h DMSO IC50=0.29 μM 23515752
HCC2279 Growth Inhibition Assay 72 h DMSO IC50=0.4 μM 23515752
HCC827 Growth Inhibition Assay 72 h DMSO IC50=0.29 μM 23515752
HCC2935 Growth Inhibition Assay 72 h DMSO IC50=0.97 μM 23515752
HCC4006 Growth Inhibition Assay 72 h DMSO IC50=0.46 μM 23515752
H460 Function Assay 500 nM 24 h DMSO decreases EGFR expression 23515752
H1650 Function Assay 500 nM 24 h DMSO decreases EGFR expression 23515752
PC9 Function Assay 500 nM 24 h DMSO decreases EGFR expression 23515752
H460 Function Assay 0.5/1/2 μM 4 h DMSO inhibits the levels of Akt (p-Akt) and EGFR 23515752
H1650 Function Assay 0.5/1/2 μM 4 h DMSO inhibits the levels of Akt (p-Akt) and EGFR 23515752
PC9 Function Assay 0.5/1/2 μM 4 h DMSO inhibits the levels of Akt (p-Akt) and EGFR 23515752
AsPc1 Growth Inhibition Assay 48 h EC50=0.3 μM 23475695
Panc0327 Growth Inhibition Assay 48 h EC50=0.5 μM 23475695
MiaPaCa2 Growth Inhibition Assay 48 h EC50=0.7 μM 23475695
BxPc3 Growth Inhibition Assay 48 h EC50=1.0 μM 23475695
Panc0403 Growth Inhibition Assay 48 h EC50=1.1 μM 23475695
Panc1005 Growth Inhibition Assay 48 h EC50=1.1 μM 23475695
PL45 Growth Inhibition Assay 48 h EC50=20.8 μM 23475695
Panc0203 Growth Inhibition Assay 48 h EC50=22.2 μM 23475695
Panc0327 Apoptosis Assay 1 μM 24 h induces apoptosis 23475695
Panc1005 Apoptosis Assay 1 μM 24 h induces apoptosis 23475695
Panc0403 Apoptosis Assay 1 μM 24 h induces apoptosis 23475695
AsPc1 Function Assay 1/10 μM 24 h induces growth arrested in G2/M 23475695
MiaPaCa2 Function Assay 1/10 μM 24 h induces growth arrested in G2/M 23475695
T3M4 Growth Inhibition Assay 0-800 nM 48 h inhibits cell proliferation in a dose dependent manner 22681698
AsPC-1 Growth Inhibition Assay 0-800 nM 48 h inhibits cell proliferation in a dose dependent manner 22681698
Panc-1  Growth Inhibition Assay 0-800 nM 48 h inhibits cell proliferation in a dose dependent manner 22681698
T3M4 Apoptosis Assay 100/500/1000 nM 48 h induces dose dependent apoptosis 22681698
AsPC-1 Apoptosis Assay 100/500/1000 nM 48 h induces dose dependent apoptosis 22681698
Panc-1  Apoptosis Assay 100/500/1000 nM 48 h induces dose dependent apoptosis 22681698
HBL-2 Growth Inhibition Assay 24 h IC50=0.4 μM 20068080
Jeko-1 Growth Inhibition Assay 24 h IC50=0.2 μM 20068080
Granta-519 Growth Inhibition Assay 24 h IC50=56.3 μM 20068080
HCT116 Growth Inhibition Assay 48 h EC50=0.28 μM 17124594
HCT116 Function Assay 0.9 μM  24 h down-regulats TS protein levels after 6 h incubation 17124594

... Click to View More Cell Line Experimental Data
In vivo Belinostat indicates significant tumor growth delay in A2780 and A2780/cp70 xenograft at a dose of 10mg/kg with no effects on the body weight. [1] Belinostat also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. [2] Belinostat monotherapy induces dose-proportional antitumor effects with TGI of 47% at a dose of 100mg/kg in A2780 xenograft. The combination of Belinostat (100 mg/kg) with carboplatin (40 mg/kg) could delay tumor growth from 18.6 days to 22.5 days. [3] Combining with bortezomib, Belinostat results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft. [5]
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