Belinostat (PXD101)|cas 414864-00-9|DC Chemicals

Cas No.:	414864-00-9
Chemical Name:	Belinostat
Synonyms:	Belinostat;Belinostat (PXD101);(E)-N-Hydroxy-3-(3-(N-phenylsulfamoyl)phenyl)acrylamide;(E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide;Belinostat (PXD101, PX105684, NSC726630);Belinostat (PXD-101);N-HYDROXY-3-[3-[(PHENYLAMINO)SULFONYL]PHENYL]-2-PROPENAMIDE;PXD101;N-Hydroxy-3-(3-phenylsulfamoylphenyl)acrylamide;Beleodaq;PXD 101;NSC726630;PX105684;PX 105684;F4H96P17NZ;(2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide;N-Hydroxy-3-(3-phenylsulphamoylphenyl)acrylamide;N-Hyd;2-Propenamide, N-hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-, (2E)-;Belinostat(Random Configuration);(2E)-N-hydro
SMILES:	S(C1=C([H])C([H])=C([H])C(/C(/[H])=C(\[H])/C(N([H])O[H])=O)=C1[H])(N([H])C1C([H])=C([H])C([H])=C([H])C=1[H])(=O)=O
Formula:	C₁₅H₁₄N₂O₄S
M.Wt:	318.3477
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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. A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA. 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. 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. Combining with bortezomib, Belinostat results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft. [5]For the detailed information of Belinostat (PXD101), the solubility of Belinostat (PXD101) in water, the solubility of Belinostat (PXD101) in DMSO, the solubility of Belinostat (PXD101) in PBS buffer, the animal experiment (test) of Belinostat (PXD101), the cell expriment (test) of Belinostat (PXD101), the in vivo, in vitro and clinical trial test of Belinostat (PXD101), the EC50, IC50,and Affinity of Belinostat (PXD101), Please contact DC Chemicals.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
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DC3110	CUDC-907 (PI3K/HDAC InhibitorI)	CUDC-907 (PI3K/HDAC Inhibitor I) is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.
DC8252	Vorinostat (SAHA)	Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.
DC8663	UF010	UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs.
DC6303	Tubastatin A HCl	Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC6304	Tubastatin A	Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC5178	Tubacin (BML-GR362)	Tubacin is a selective inhibitor of HDAC6 via inhibition of the second deacetylase domain (DD2).
DC8134	Trichostatin A (TSA)	Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not affected by TSA.
DC7716	TMP269	TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs.
DC10210	TMP195	TMP195 is the most potent and selective class IIa HDAC inhibitor.