Belinostat (PXD101)

Catalog No.S1085 Synonyms: NSC726630, PX-105684

For research use only.

Belinostat (PXD101, NSC726630, PX-105684) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.

Belinostat (PXD101) Chemical Structure

CAS No. 414864-00-9

Selleck's Belinostat (PXD101) has been cited by 84 publications

Purity & Quality Control

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Biological Activity

Description Belinostat (PXD101, NSC726630, PX-105684) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
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
HCT116 MYXGeY5kfGmxbjDBd5NigQ>? MoHBNE46yqEQvF5CpC=> MVqyOEBp MUnkc5dvNXKnZ4XsZZR{KFSVIIDyc5RmcW5ibHX2[Yx{KGGodHXyJFbDqGhiaX7jeYJifGmxbh?= M3jaNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MUK0OVk1Lz5zN{GyOFU6PDxxYU6=
HCT116 MofES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInCXYU1QCCq MoD2SWM2OD1yLkK4JO69VQ>? NGr1Tmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyOFU6PCd-MUexNlQ2QTR:L3G+
Granta-519 M37HfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmSxNlQhcA>? NHLSWXFKSzVyPUW2MlMh|ryP MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB4OEC4NEc,OjByNkiwPFA9N2F-
Jeko-1 NH[5XGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfmV25uOjRiaB?= NUPJR4ptUUN3ME2wMlIh|ryP M3q1e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyME[4NFgxLz5{MEC2PFA5ODxxYU6=
HBL-2 NWS2OlJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSyOEBp M13pcmlEPTB;MD60JO69VQ>? M2jOd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyME[4NFgxLz5{MEC2PFA5ODxxYU6=
Panc-1  MUjBdI9xfG:|aYOgRZN{[Xl? MVqxNFAwPTByL{GwNFAhdk1? NXfFdXZiPDhiaB?= M2XLfolv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ6MU[5PEc,OjJ4OEG2PVg9N2F-
AsPC-1 MkjaRZBweHSxc3nzJGF{e2G7 M2L0elExOC93MECvNVAxOCCwTR?= M{jqTFQ5KGh? MVLpcoR2[2W|IHTvd4Uh\GWyZX7k[Y51KGGyb4D0c5Nqew>? MoDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
T3M4 MoLERZBweHSxc3nzJGF{e2G7 NGrFO5oyODBxNUCwM|ExODBibl2= Mnf0OFghcA>? NIm2fY1qdmS3Y3XzJIRwe2ViZHXw[Y5l\W62IHHwc5B1d3Orcx?= M1:2c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
Panc-1  MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWwMVgxOCCwTR?= NHXET2E1QCCq MXXpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M1HjSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
AsPC-1 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLSNE05ODBibl2= M4PMT|Q5KGh? MYfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NH:4e249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[4NVY6QCd-MkK2PFE3QTh:L3G+
T3M4 M1\JOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPQOnhoOC16MECgcm0> MmqyOFghcA>? MVPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M1HLNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
MiaPaCa2 MlO5SpVv[3Srb36gRZN{[Xl? MoPUNU8yOCEQvF2= NWHJSoNCOjRiaB?= MUjpcoR2[2W|IDDndo94fGhiYYLy[ZN1\WRiaX6gS|IwVQ>? MlTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
AsPc1 MWPGeY5kfGmxbjDBd5NigQ>? NX;yPJdpOS9zMDFOwG0> M4XHdlI1KGh? MmPibY5lfWOnczCg[5Jwf3SqIHHydoV{fGWmIHnuJGczN01? NIfHUFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0403 MXnBdI9xfG:|aYOgRZN{[Xl? MmrYNUDPxE1? MX2yOEBp M3Ljbolv\HWlZYOgZZBweHSxc3nz MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc1005 M3HEdWFxd3C2b4Ppd{BCe3OjeR?= MnzxNUDPxE1? NGfxSlAzPCCq NWj0Z5J5cW6mdXPld{BieG:ydH;zbZM> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc0327 M3\D[mFxd3C2b4Ppd{BCe3OjeR?= NVz6UnlpOSEQvF2= M{HUfFI1KGh? MljFbY5lfWOnczDhdI9xfG:|aYO= NELsT3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0203 MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUewXnlOPDhiaB?= MXHFR|UxRTJ{LkKg{txO NUXSZ2w3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
PL45 NIXTTHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXG0PEBp NVXINWhxTUN3ME2yNE45KM7:TR?= NUnXVXhvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc1005 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVO0PEBp MVjFR|UxRTFwMTFOwG0> NYXCfo5VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc0403 MkjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TWOVQ5KGh? M13CZmVEPTB;MT6xJO69VQ>? MmHLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
BxPc3 NVPGWZZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfwUG13PDhiaB?= M3XI[2VEPTB;MT6wJO69VQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
MiaPaCa2 NWnWUXlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVm0PEBp M3LHTWVEPTB;MD63JO69VQ>? NYTwbm5ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc0327 MoTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLaXoJIPDhiaB?= MnjoSWM2OD1yLkWg{txO NYLYUJJnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
AsPc1 MmXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUG0PEBp M3mxUWVEPTB;MD6zJO69VQ>? NH3Lb2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
PC9 MY\GeY5kfGmxbjDBd5NigQ>? NIfTdVYxNjVxMT:yJO69VQ>? MmS1OEBp M{HlUmROW09? MnjCbY5pcWKrdIOgeIhmKGyndnXsd{Bw\iCDa4SgLJAuSWu2KTDhcoQhTUeIUh?= NFvyV4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H1650 MUnGeY5kfGmxbjDBd5NigQ>? NELlRXoxNjVxMT:yJO69VQ>? NWj0c41mPCCq MmPaSG1UVw>? NV;BNo81cW6qaXLpeJMhfGinIHzleoVteyCxZjDBb5QhMHBvQXv0LUBidmRiRVfGVi=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
H460 Ml;ISpVv[3Srb36gRZN{[Xl? NISwd|QxNjVxMT:yJO69VQ>? M2[3UlQhcA>? M3PFVGROW09? NFO4d2hqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S M1\CVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
PC9 MojISpVv[3Srb36gRZN{[Xl? MXi1NFDDqG6P M4fOTFI1yqCq M2rGcGROW09? MmTK[IVkemWjc3XzJGVITlJiZYjwdoV{e2mxbh?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
H1650 NFztSIxHfW6ldHnvckBCe3OjeR?= MnOzOVAxyqCwTR?= NEDwU4szPMLiaB?= NELDdVhFVVOR NHi4XXJl\WO{ZXHz[ZMhTUeIUjDlfJBz\XO|aX;u MlzWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H460 NUnzOHFITnWwY4Tpc44hSXO|YYm= MX:1NFDDqG6P M4f2VVI1yqCq MYXEUXNQ MkPO[IVkemWjc3XzJGVITlJiZYjwdoV{e2mxbh?= MmjMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
HCC4006 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[3NuKhcA>? NYXMS3l2TE2VTx?= M3ewbWlEPTB;MD60OkDPxE1? M1PkcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
HCC2935 NVzSZ2JyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDRe484OsLiaB?= M4e2WGROW09? Ml3CTWM2OD1yLkm3JO69VQ>? MonSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
HCC827 NXXWdXRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkO0O|LDqGh? MX;EUXNQ NV\rdnBFUUN3ME2wMlI6KM7:TR?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
HCC2279 M1HPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHSZXNUPzMEoHi= NI\3TlhFVVOR NYrtUG9UUUN3ME2wMlQh|ryP NILCc4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
PC9 M{DMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS2codFPzMEoHi= M4H5N2ROW09? M1vPemlEPTB;MD6yPUDPxE1? NUfXZ2xKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H820 MnvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfZR5k4OsLiaB?= NXPJU|hoTE2VTx?= Mk\0TWM2OD1yLkSg{txO NITzSIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H1650 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUG3NuKhcA>? NVvTenJETE2VTx?= MnjrTWM2OD1yLki4JO69VQ>? NUiwRW5RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H1975 M{fkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjWNJBmPzMEoHi= M{PCWWROW09? NGm0[HhKSzVyPUCuOlgh|ryP M1L0R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H520 MkfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX63NuKhcA>? NInOZVRFVVOR Ml;WTWM2OD1yLke1JO69VQ>? NYTKcY5ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H1299 MoTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPjO|LDqGh? MmDCSG1UVw>? MXvJR|UxRTFwMjFOwG0> NEf4bIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H460 NVHMZWF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[3NuKhcA>? NFzPb3VFVVOR NGLsWINKSzVyPUCuPFYh|ryP MlLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H1666 NWXzeJFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe1O|LDqGh? NI\ZWpRFVVOR NWK3SVlIUUN3ME6xNEDPxE1? Ml7xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
PANC-1 MVvGeY5kfGmxbjDBd5NigQ>? MlXZNVDDqM7:TR?= NI\6XmwzNzRiaB?= Mln6SG1UVw>? MUDpcoNz\WG|ZYOgbY51emGlZXzseYxieiCUT2OgcIV3\Wx? MlXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NEOxPVgoRjJ|N{SzNVk5RC:jPh?=
PANC-1 NI[zU5RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEm4W4cyNzFywrFOwG0> MYK0PEBp MoH2SG1UVw>? NYnKNGhn\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd2M{G5PEc,OjN5NEOxPVg9N2F-
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NFF MWLDfZRwfG:6aXPpeJkh[XO|YYm= NH3NVFg4OiCqcoO= MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOSmYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IEGuOEDPxE1w M37zT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkSxNVEzLz5{OEK0NVEyOjxxYU6=
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NFF NWTQeG5nS3m2b4TvfIlkcXS7IHHzd4F6 NWLOT3A1PzJiaILz NVHkN4hlS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVk[IIHPlcIx{KGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxKD1iMT60NkDPxE1w MlLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NEW0NFIoRjNyMkS1OFAzRC:jPh?=
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RAW264.7 NInFU3pCdnSrLXnu[oxidW2jdH;yfUBie3OjeR?= NY\z[mtkOSCqch?= Ml[wRY51cS2rbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hVFCVLYP0bY12dGG2ZXSgcY92e2ViUlHXNlY1NjdiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4Yhdmm2cnnjJI95cWSnIIDyc4R2[3Srb36gdJJmNWmwY4XiZZRm\CCob4KgNUBpeiCkZX\vdoUhVFCVIIP0bY12dGG2aX;uJIZweiB{NDDodpMh[nliR4Lp[ZN{KHKnYXflcpQh[mG|ZXSgZZN{[XluIFnDOVAhRSB{LkKg{txONg>? Mk[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUO4O|UoRjJ3MUGzPFc2RC:jPh?=
RAW264.7 MoD5RY51cS2rbn\sZY1u[XSxcomgZZN{[Xl? MUGxJIhz NED2OGxCdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh[mWob4LlJGxRWyC|dHnteYxifGmxbjDmc5IhOjRiaILzJIJ6KEWOSWPBJI1mfGixZDygTWM2OCB;IESuO{DPxE1w MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTFzM{i3OUc,OjVzMUO4O|U9N2F-
RAW264.7 M{\hN2FvfGlvaX7mcIFudWG2b4L5JIF{e2G7 MmPJNUBpeg>? M2rCe2FvfGlvaX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKEySUz3zeIlufWyjdHXkJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKFCJRUKgdJJw\HWldHnvckBxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCOUGOgd5RqdXWuYYTpc44h\m:{IEK0JIhzeyCkeTDlcpp6dWViaX3teY5w[XO|YYmgcYV1cG:mLDDJR|UxKD1iOD6yPEDPxE1w MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTFzM{i3OUc,OjVzMUO4O|U9N2F-
Huh-luc/neo7 NVHZZWVnTnWwY4Tpc44h[XO|YYm= M1zWcVEhfU1? M4LYNlEhfG9iMzDodpM> MXnJcohq[mm2aX;uJI9nKEiGQVOgZ4xie3NiMTDpckBpfW2jbjDIeYgudHWlL37lc|ch[2WubIOgZZN{\XO|ZXSgZZMhcGm|dH;u[UBJOyCjY3X0fYxifGmxbjDheEAyKHWPIHHmeIVzKDFidH:gN{BpenNiYomgW4V{fGW{bjDicI91fGmwZzDhcoFtgXOrcx?= M{\BR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUO3NFE4Lz5{NUmzO|AyPzxxYU6=
PC3 NEL0W4FHfW6ldHnvckBie3OjeR?= NILYb20xNjNidV2= NUXKcYl4PDhiaILz M2PZWGlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZY1wfW62IH;mJIFk\XS7bHH0[YQhcGm|dH;u[UBJOyCjdDCwMlMhfU1iYX\0[ZIhPDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NV7V[4dHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezOFQ1QDdpPkK3N|Q1PDh5PD;hQi=>
HCT116 MVfGeY5kfGmxbjDhd5NigQ>? NET1OHYxNjNidV2= NUXBXmlyPDhiaILz NUflWZpzUW6qaXLpeIlwdiCxZjDISGFEKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCjbX;1cpQhd2ZiYXPleJlt[XSnZDDobZN1d26nIFizJIF1KDBwMzD1UUBi\nSncjC0PEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M4LxOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{S0OFg4Lz5{N{O0OFQ5PzxxYU6=
Assay
Methods Test Index PMID
Western blot p-H2AX(Ser139) / KU70 / KU80 / RAD51 / RAD52 / ERCC1 ; Acetyl Histone H3 / Acetyl Histone H4 / Acetyl tubulin ; p21 / p27 ; SOS1 / SOS2 ; PARP / p-ERK / p-p38 / p38 / p-BRAF / p-MEK / MEK 24155971 23982416 28397399
Growth inhibition assay Cell viability ; IC50 24155971 28397399
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 (from reference)

Kinase Assay:[1]
  • 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:[1]
  • 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:[1]
  • Animal Models: A2780, A2780/cp70 and HCT116 cells are injected s.c. into the right flank of CD1 nu/nu mice.
  • 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 Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

10mg/mL

* 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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma May 3 2021 Phase 1
NCT04703920 Recruiting Drug: Talazoparib|Drug: Belinostat Metastatic Breast Cancer|Metastatic Castration-resistant Prostate Cancer|Metastatic Ovarian Carcinoma University of Michigan Rogel Cancer Center|Pfizer|Acrotech Biopharma LLC March 4 2021 Phase 1
NCT03772925 Recruiting Drug: Belinostat|Drug: Pevonedistat Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome|Refractory Acute Myeloid Leukemia|Refractory Myelodysplastic Syndrome National Cancer Institute (NCI) February 28 2019 Phase 1
NCT02680795 Completed Drug: Belinostat IV Solid Tumors|Hematological Malignancies Acrotech Biopharma LLC|Axis Clinicals Limited April 27 2016 Phase 1
NCT02679131 Terminated Drug: Belinostat Relapsed/Refractory Solid Tumors/Hematological Malignancies Acrotech Biopharma LLC|Axis Clinicals Limited March 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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