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Signaling Pathway

Belinostat

HY-10225

(PXD101; PX105684; PXD-101; PXD 101; PX-105684)

Belinostat

Belinostat Chemical Structure

Belinostat (PXD101) is a novel pan-HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors.

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10 mM * 1 mL in DMSO $72 In-stock
10 mg $65 In-stock
50 mg $207 In-stock
100 mg $315 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €71 In-stock
10 mg €64 In-stock
50 mg €203 In-stock
100 mg €309 In-stock
200 mg Get quote
500 mg Get quote

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Product name: Belinostat
Cat. No.: HY-10225

Belinostat Data Sheet

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    Purity: 99.66%

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Biological Activity of Belinostat

Belinostat (PXD101) is a novel pan-HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors.
IC50 Value: 27 nM
Target: pan-HDAC
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. 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. 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.
in vivo:  Belinostat also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. 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.

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 318.35 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C15H14N2O4S
CAS No 866323-14-0
Solvent & Solubility

DMSO ≥60mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 3.1412 mL 15.7060 mL 31.4120 mL
5 mM 0.6282 mL 3.1412 mL 6.2824 mL
10 mM 0.3141 mL 1.5706 mL 3.1412 mL

Clinical Information of Belinostat

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Belinostat TopoTarget A/S Carcinoma 28-FEB-09 31-DEC-12 Phase 2 30-JAN-13
National Cancer Institute Fallopian tube cancer 31-DEC-09 Phase 2 17-JAN-13
Dartmouth-Hitchcock Medical Center Follicle center lymphoma 31-OCT-10 31-DEC-20 Phase 2 28-AUG-13
University of Arizona Non-Hodgkin lymphoma 30-SEP-12 01-MAR-15 Phase 2 11-SEP-13
Spectrum Pharmaceuticals Inc Peripheral T-cell lymphoma 31-DEC-08 30-JUN-13 Phase 2 15-NOV-13

References on Belinostat

Inhibitor Kit

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