Belinostat (PXD101)

Catalog No.S1085 Synonyms: NSC726630, PX-105684

Belinostat (PXD101) Chemical Structure

Molecular Weight(MW): 318.35

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

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 370 In stock
USD 570 In stock
USD 970 In stock

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5 Customer Reviews

  • Inhibition of LSD1 activity by HDAC inhibitors. a MDA-MB-231 and MDA-MB-468 cells were exposed to indicated HDAC inhibitors for 24 h.

    Breast Cancer Res Treat 2012 131, 777-789. Belinostat (PXD101) purchased from Selleck.

    LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.

     

     

    Breast Cancer Res Treat 2010 131(3), 777-789. Belinostat (PXD101) purchased from Selleck.

  • HDACIs That Simultaneously Inhibit HDACs 1 and 6 Showed Greater Antileukemic Activities than HDACIs that Don,t at Cmax Concentrations. THP-1 cells were treated with LBH-589, PXD101, SAHA, VPA, MS-275 and MGCD0103 at Cmax concentrations for 3 h and 24 h, respectively. The cells post 3 h treatments were washed three times with complete medium and divided into two halves. One half of the cells was resuspended in complete media and cultured for up to 24 h to determine the effects of the 3 h treatments on cell proliferation and apoptosis. The other half of the cells was used to prepare whole cell lysates. Whole cell lysates from the 3 h and 24 h treatments were extracted and subjected to Western blots probed by anti-ac-tubulin or-β-actin antibody (panels A&B), or subjected to HDAC1 enzymatic assays post IP as described in the Materials and Methods (Panels C&D). The effects of the 3 h and 24 h HDACI treatments on cell proliferation, as reflected by percent decrease of live cells relative to untreated cells (panel E), and apoptosis (panel F) were determined by flow cytometry analysis as described in the Materials and Methods.

     

     

    PLoS One 2011 6, e17138. Belinostat (PXD101) purchased from Selleck.

    Induction of DNA Damage and Bim Is Critical for HDACI-Induced Apoptosis in Pediatric AML Cells. THP-1 cells were treated with the HDACIs at Cmax concentrations for 3 (panel A) and 24 h (panel B), respectively. Whole cell lysates were extracted and subjected to Western blots probed by anti-p21, -c-Myc, -cH2AX, -Bim, or -β-actin antibody.

     

     

    PLoS One 2011 6, e17138. Belinostat (PXD101) purchased from Selleck.

  • MDA-MB-231 Breast cancer cells were pretreated with Acetyl-H3 and H3, and then treated with the indicated concentrations of  PXD101.

    Dr. Zhang of Tianjin Medical University. Belinostat (PXD101) purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M1TCWWNmdGxiVnnhZoltcXS7IFHzd4F6 NUDKNVVYOC5{L{NCpO69VQ>? MW[yOE81QC95MjDo NWLtWmJ4\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGKxdHigeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MWWyOVg3PDd|Mh?=
HL-60  NHrUPJlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGDnUVAxNjJxMtMg{txO NVTEOYNGOjRxNEivO|IhcA>? MVvk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NIq3cJUzPTh4NEezNi=>
NB4 M{\tPGZ2dmO2aX;uJGF{e2G7 M1fxe|LDqM7:TR?= Ml3jNlQwPDhiaB?= NFvKOYljdG:la4OgZ4VtdCCleXPs[UBqdiCVIIDoZZNm M3fRblI2QDZ2N{Oy
HL-60  NXTzVXhiTnWwY4Tpc44hSXO|YYm= NWTHUpdjOsLizszN NISwNGIzPC92ODDo MmW1Zoxw[2u|IHPlcIwh[3mlbHWgbY4hWyCyaHHz[S=> NXjRPXVTOjV6NkS3N|I>
NB4 NVvHbYdCTnWwY4Tpc44hSXO|YYm= NFK0N5gxNjMEoN88US=> M2\OU|I1NzR6L{eyJIg> MUTlcohidmOnczDSRU1qdmS3Y3XkJIdz[W63bH;jfZRq[yCmaX\m[ZJmdnSrYYTpc44> MlzENlU5PjR5M{K=
HL-60  NILvfmJHfW6ldHnvckBCe3OjeR?= Mn;uNE4zyqEQvF2= NHT0RnIzPC92OD:3NkBp NVLpeIMy\W6qYX7j[ZMhWkFvaX7keYNm\CCpcnHueYxw[3m2aXOg[Iln\mW{ZX70bYF1cW:w NELRXWIzPTh4NEezNi=>
PANC-1 MlvxSpVv[3Srb36gRZN{[Xl? NH;2W4syOMLizszN NYHFemx1Oi92L{[gbC=> Mn\pSG1UVw>? NYjuZZdWcW6mdXPld{BCVVCNIHHjeIl3[XSrb36= M{jtfVI{PzR|MUm4
PANC-1 NUHMfHZqS2WubDDWbYFjcWyrdImgRZN{[Xl? MV6xM|ExyqEQvF2= MmK5OFghcA>? M1O5e2ROW09? NGS1R5Fl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MofhNlM4PDNzOUi=
PANC-1 NYC3RXBtTnWwY4Tpc44hSXO|YYm= M1yzclExyqEQvF2= NYO2OYpuOi92IHi= MmH2SG1UVw>? M1zYU4lv[3KnYYPld{BqdnS{YXPlcIx2dGG{IGLPV{Bt\X[nbB?= MlnBNlM4PDNzOUi=
H1666 M4PLV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnVTIJ{PzMEoHi= M1GzSmROW09? NWjaXmZKUUN3ME6xNEDPxE1? MlXwNlM2OTV5NUK=
H460 MlHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjW[5M4OsLiaB?= MVPEUXNQ NETad21KSzVyPUCuPFYh|ryP NUDpNnd2OjN3MUW3OVI>
H1299 M4PvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\2O|LDqGh? NFPTfI1FVVOR MY\JR|UxRTFwMjFOwG0> NYLo[moxOjN3MUW3OVI>
H520 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[wZlczyqCq NEDqdY1FVVOR MY\JR|UxRTBwN{Wg{txO M2n6flI{PTF3N{Wy
H1975 NH3wOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP2Nlg4OsLiaB?= M4X4VmROW09? MlvyTWM2OD1yLk[4JO69VQ>? M375WVI{PTF3N{Wy
H1650 NYPPWFFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYS3NuKhcA>? M3nqOmROW09? MWDJR|UxRTBwOEig{txO NX3YRW42OjN3MUW3OVI>
H820 M{L3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnrS2lPPzMEoHi= MlT6SG1UVw>? NVKwOHl6UUN3ME2wMlQh|ryP MkLjNlM2OTV5NUK=
PC9 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUW3NuKhcA>? MnHpSG1UVw>? M4\ueGlEPTB;MD6yPUDPxE1? NUeyU2FLOjN3MUW3OVI>
HCC2279 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGW3Soo4OsLiaB?= NWjTTVd7TE2VTx?= MXzJR|UxRTBwNDFOwG0> NXrVfmxiOjN3MUW3OVI>
HCC827 NGHvXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGiyXpY4OsLiaB?= MV\EUXNQ M{PGPWlEPTB;MD6yPUDPxE1? MUeyN|UyPTd3Mh?=
HCC2935 NYK2[5BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1:wdlczyqCq MVHEUXNQ NXHBNFZTUUN3ME2wMlk4KM7:TR?= M1XLelI{PTF3N{Wy
HCC4006 NEDiU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV23NuKhcA>? MYLEUXNQ M{XQZWlEPTB;MD60OkDPxE1? NF64OHUzOzVzNUe1Ni=>
H460 MVHGeY5kfGmxbjDBd5NigQ>? M131b|UxOMLibl2= NF;NUWUzPMLiaB?= NYr1PYtYTE2VTx?= MnTF[IVkemWjc3XzJGVITlJiZYjwdoV{e2mxbh?= MorzNlM2OTV5NUK=
H1650 NGrsSlZHfW6ldHnvckBCe3OjeR?= MlX5OVAxyqCwTR?= M1XEV|I1yqCq MmXJSG1UVw>? M4qzcIRm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= MWeyN|UyPTd3Mh?=
PC9 Mkn6SpVv[3Srb36gRZN{[Xl? MV21NFDDqG6P NIrYZoszPMLiaB?= M3LyemROW09? M4L6bIRm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= NEfqSm8zOzVzNUe1Ni=>
H460 NHzKTIpHfW6ldHnvckBCe3OjeR?= NWjnTII5OC53L{GvNkDPxE1? NWLrcHdSPCCq M2HKemROW09? NGfWdWJqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S Mk\uNlM2OTV5NUK=
H1650 MYDGeY5kfGmxbjDBd5NigQ>? NVXZOGUxOC53L{GvNkDPxE1? M{e5dFQhcA>? NEm4U3hFVVOR M4nQSolvcGmkaYTzJJRp\SCuZY\lcJMhd2ZiQXv0JEhxNUGtdDmgZY5lKEWJRmK= NYDUNYhUOjN3MUW3OVI>
PC9 NWjLdIlnTnWwY4Tpc44hSXO|YYm= MUiwMlUwOS9{IN88US=> NEjLdnQ1KGh? NFS5eVRFVVOR NFrvS3FqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S M{LWXFI{PTF3N{Wy
AsPc1 MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TVTlQ5KGh? NUHNcHN2TUN3ME2wMlMh|ryP M3;a[|I{PDd3Nkm1
Panc0327 MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NESxZZQ1QCCq M3XtNWVEPTB;MD61JO69VQ>? MUiyN|Q4PTZ7NR?=
MiaPaCa2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;3R|Q5KGh? NXrFd2x7TUN3ME2wMlch|ryP NWnDR5k{OjN2N{W2PVU>
BxPc3 NH:2cppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmS0OFghcA>? MnPwSWM2OD1zLkCg{txO M1e3bVI{PDd3Nkm1
Panc0403 NHrxOnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVG0PEBp NV;PUmVuTUN3ME2xMlEh|ryP NYT6b|BSOjN2N{W2PVU>
Panc1005 M3jm[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\2Vok1QCCq NVGwSIk3TUN3ME2xMlEh|ryP Mn\0NlM1PzV4OUW=
PL45 M4jQWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnoPZo1QCCq MXTFR|UxRTJyLkig{txO MWKyN|Q4PTZ7NR?=
Panc0203 M4facmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfUdVFUPDhiaB?= NIT5ZndGSzVyPUKyMlIh|ryP NHG3W3YzOzR5NU[5OS=>
Panc0327 NYCwZnNXSXCxcITvd4l{KEG|c3H5 NFOwS|kyKM7:TR?= MkjWNlQhcA>? M13jOIlv\HWlZYOgZZBweHSxc3nz NGHyb2czOzR5NU[5OS=>
Panc1005 MYHBdI9xfG:|aYOgRZN{[Xl? M3LIS|Eh|ryP NHLBemMzPCCq NX\EUoZicW6mdXPld{BieG:ydH;zbZM> MkDrNlM1PzV4OUW=
Panc0403 MlzJRZBweHSxc3nzJGF{e2G7 M33PUlEh|ryP M1jqRlI1KGh? NIDPcIlqdmS3Y3XzJIFxd3C2b4Ppdy=> NYn2XYl{OjN2N{W2PVU>
AsPc1 MnfBSpVv[3Srb36gRZN{[Xl? MlS0NU8yOCEQvF2= Ml\zNlQhcA>? NX7lPZZJcW6mdXPld{Ah\3Kxd4ToJIFzemW|dHXkJIlvKEd{L12= M33Fc|I{PDd3Nkm1
MiaPaCa2 M4fkZ2Z2dmO2aX;uJGF{e2G7 NFz3enQyNzFyIN88US=> MWOyOEBp NEnGXZZqdmS3Y3XzJEBoem:5dHigZZJz\XO2ZXSgbY4hTzJxTR?= NIrMe4YzOzR5NU[5OS=>
T3M4 Mke3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuwMVgxOCCwTR?= MV20PEBp M2jDdolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NYPmW2dXOjJ4OEG2PVg>
AsPC-1 M2nlcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\wO|AuQDByIH7N Mk\oOFghcA>? MVzpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M1;tZ|IzPjhzNkm4
Panc-1  NHLsSHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nGcFAuQDByIH7N M2LB[VQ5KGh? NI\RTHNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NELyeIUzOjZ6MU[5PC=>
T3M4 MUfBdI9xfG:|aYOgRZN{[Xl? Mli4NVAxNzVyMD:xNFAxKG6P NYPpT|R3PDhiaB?= NFHLfXdqdmS3Y3XzJIRwe2ViZHXw[Y5l\W62IHHwc5B1d3Orcx?= MUGyNlY5OTZ7OB?=
AsPC-1 M2TxdmFxd3C2b4Ppd{BCe3OjeR?= MoHtNVAxNzVyMD:xNFAxKG6P MYi0PEBp M2rJdYlv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| M1jmV|IzPjhzNkm4
Panc-1  NWW1epJmSXCxcITvd4l{KEG|c3H5 Mke0NVAxNzVyMD:xNFAxKG6P M2LrN|Q5KGh? MYXpcoR2[2W|IHTvd4Uh\GWyZX7k[Y51KGGyb4D0c5Nqew>? MonNNlI3QDF4OUi=
HBL-2 M2H1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGyOEBp Mo\ETWM2OD1yLkSg{txO NGHCd20zODB4OEC4NC=>
Jeko-1 M4qyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOyOEBp M{\yRWlEPTB;MD6yJO69VQ>? M{LHc|IxODZ6MEiw
Granta-519 NI\Pe5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHDNW0zPCCq M3HsVGlEPTB;NU[uN{DPxE1? NIDt[|MzODB4OEC4NC=>
HCT116 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\LNFQ5KGh? MmDsSWM2OD1yLkK4JO69VQ>? NWrKZlZCOTdzMkS1PVQ>
HCT116 NIe0WY5HfW6ldHnvckBCe3OjeR?= M{fNVlAvQcLizszNxsA> MVeyOEBp NYLVXXF{\G:5bj3y[Yd2dGG2czDUV{Bxem:2ZXnuJIxmfmWuczDh[pRmeiB4wrDoJIlv[3WkYYTpc44> NHf1NmsyPzF{NEW5OC=>

... 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]

Protocol

Kinase Assay
+ Expand

Histone Deacetylase Activity:

Subconfluent cultures are harvested and washed twice in ice cold PBS and pelleted by centrifugation at 200 × g for 5 min. The cell pellet is resuspended in two volumes of lysis buffer [60 mM Tris buffer (pH 7.4) containing 30% glycerol and 450 mM NaCl] and lysed by three freeze (dry ice) thaw (30 °C water bath) cycles. Cell debris is removed by centrifugation at 1.2 × 104 g for 5 min, and the supernatant is stored at −80 °C. Histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRK corresponding to the 20 NH2-terminal residues) is acetylated by a recombinant protein containing the hypoxanthine-aminopterin-thymidine domain of p300, using [3H]acetyl CoA as a source of acetate. H4 peptide (100 μg) is mixed with hypoxanthine-aminopterin-thymidine buffer (50 mM Tris HCl pH 8.0, 5% glycerol, 50 mM KCl, and 0.1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoethyl) benzenesulfonylfluoride, 1 × complete protease inhibitors, 50 μL of purified p300, and 1.85 m [3H]acetyl CoA (4.50Ci/mmol) in a final volume of 300 μL and incubated at 30 °C for 45 min. The p300 protein is removed by incubation with 20 μL of 50% Ni-agaroase beads for 1 hour at 4 °C and centrifugation. The supernatant is applied to a 2 mL Sephadex G15 column, and the flow through is collected. One milliliter of distilled H2O is gently applied, and three drop fractions are collected; this is repeated until 4–5 mL of distilled H2O has been added, and ∼40 fractions are collected. Three microliters of each fraction are diluted in 2 mL of scintillation fluid and counted in a scintillation counter to identify the fractions containing the labeled peptide. These fractions are pooled, and 1 μL of the combined sample is measured to assess the radioactivity in every peptide batch (3-7×103 cpm/μL). For activity assays, the reaction is carried out in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] containing 2 μL of cell extract and, where used, 2 μL of belinostat. The reaction is started by the addition of 2 μL of [3H] labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples are incubated at 37 °C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12 M final concentrations, respectively). Released [3H]acetate is extracted into 750 μL of ethyl acetate, and samples are centrifuged at 1.2× 104 g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted.
Cell Research
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  • Cell lines: A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852
  • Concentrations: 0.016 - 10 μM
  • Incubation Time: 24 hours
  • Method: Tumor cell lines are seeded in 5 mL of medium at a density of 8 × 104 cells/25 cm2 flask and incubated for 48 hours. Cells are exposed to Belinostat (0.016 to 10 μM) for 24 hours. The medium is removed, and 1 mL of trypsin/EDTA is added to each flask. Once the cells have detached, 1 mL of medium is added, the cells are resuspended, and those from the control untreated flask are counted. Cells are diluted and plated into 6-cm Petri dishes (three per flask) at a density of 0.5-2× 103 cells/dish depending on the cell line. Cells from the drug-treated flasks are diluted and plated as for the control flasks. Dishes are incubated for 10–15 days at 37 °C. Cells are washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 defined as the concentration of belinostat required to reduce the number of colonies to 50% of that of the control untreated cells.
    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: A2780, A2780/cp70 and HCT116 cells are injected s.c. into the right flank of CD1 nu/nu mice.
  • Formulation: Dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10%
  • Dosages: ≤40 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

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

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 318.35
Formula

C15H14N2O4S

CAS No. 414864-00-9
Storage powder
in solvent
Synonyms NSC726630, PX-105684

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02737046 Not yet recruiting Adult T-cell Leukemia-Lymphoma|ATLL University of Miami August 2016 Phase 2
NCT02701673 Withdrawn Lymphoma M.D. Anderson Cancer Center June 2016 Phase 1|Phase 2
NCT02680795 Recruiting Solid Tumors|Hematological Malignancies Spectrum Pharmaceuticals, Inc March 2016 Phase 1
NCT02679131 Recruiting Relapsed/Refractory Solid Tumors/Hematological Malignancies Spectrum Pharmaceuticals, Inc March 2016 Phase 1
NCT02532192 Withdrawn Lymphoma M.D. Anderson Cancer Center|Spectrum Pharmaceuticals, Inc December 2015 Phase 1
NCT02381548 Recruiting Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia National Cancer Institute (NCI) August 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Could you please give some suggestions for the use of Belinostat in vivo (i.p. injection)?

  • Answer:

    For I.P. injection, S1085 Belinostat (PXD101) can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 10 mg/ml clearly. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water. Hope this information is useful to you.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID