Belinostat (PXD101)

For research use only.

Catalog No.S1085 Synonyms: NSC726630, PX-105684

74 publications

Belinostat (PXD101) Chemical Structure

CAS No. 414864-00-9

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.

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10mM (1mL in DMSO) EUR 157 In stock
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Selleck's Belinostat (PXD101) has been cited by 74 publications

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Choose Selective HDAC Inhibitors

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 M2L5c2Z2dmO2aX;uJGF{e2G7 MYKwMlnDqM7:TdMg NFW0V5MzPCCq M3HMS4Rwf25vcnXneYxifHNiVGOgdJJwfGWrbjDs[ZZmdHNiYX\0[ZIhPsLiaDDpcoN2[mG2aX;u MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzF{NEW5OEc,OTdzMkS1PVQ9N2F-
HCT116 NEHXPGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXK0PEBp M{DuT2VEPTB;MD6yPEDPxE1? NEftZ409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyOFU6PCd-MUexNlQ2QTR:L3G+
Granta-519 Mom4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrXNlQhcA>? M4Pm[mlEPTB;NU[uN{DPxE1? M1LERlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyME[4NFgxLz5{MEC2PFA5ODxxYU6=
Jeko-1 M2TTWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWeyOEBp NUnQendoUUN3ME2wMlIh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB4OEC4NEc,OjByNkiwPFA9N2F-
HBL-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzvdotFOjRiaB?= NG\tcHVKSzVyPUCuOEDPxE1? MkDXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNkiwPFAoRjJyME[4NFgxRC:jPh?=
Panc-1  NYHLXmRESXCxcITvd4l{KEG|c3H5 MVKxNFAwPTByL{GwNFAhdk1? NFPVW4E1QCCq MYnpcoR2[2W|IHTvd4Uh\GWyZX7k[Y51KGGyb4D0c5Nqew>? Ml2yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
AsPC-1 Mk\kRZBweHSxc3nzJGF{e2G7 MkjaNVAxNzVyMD:xNFAxKG6P MkDaOFghcA>? M1TZWIlv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| NWSzZZE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
T3M4 MULBdI9xfG:|aYOgRZN{[Xl? NFHOUm4yODBxNUCwM|ExODBibl2= MUS0PEBp MWHpcoR2[2W|IHTvd4Uh\GWyZX7k[Y51KGGyb4D0c5Nqew>? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ6MU[5PEc,OjJ4OEG2PVg9N2F-
Panc-1  M2TsTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDNXosxNThyMDDuUS=> NVXUbotGPDhiaB?= M3fFU4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M1jWW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
AsPC-1 M3G4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW0XG0xNThyMDDuUS=> MWm0PEBp MlLvbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ6MU[5PEc,OjJ4OEG2PVg9N2F-
T3M4 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnNcXJqOC16MECgcm0> M3;1TVQ5KGh? MYHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ6MU[5PEc,OjJ4OEG2PVg9N2F-
MiaPaCa2 NIXuRWlHfW6ldHnvckBCe3OjeR?= NVHRUGVXOS9zMDFOwG0> MXuyOEBp MnXZbY5lfWOnczCg[5Jwf3SqIHHydoV{fGWmIHnuJGczN01? NGDtZmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
AsPc1 M2fmNGZ2dmO2aX;uJGF{e2G7 NWfjWndFOS9zMDFOwG0> M2ryT|I1KGh? MX3pcoR2[2W|IDDndo94fGhiYYLy[ZN1\WRiaX6gS|IwVQ>? NUPlWIE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc0403 M37re2Fxd3C2b4Ppd{BCe3OjeR?= Mm[xNUDPxE1? MX:yOEBp MnTnbY5lfWOnczDhdI9xfG:|aYO= M2O5eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
Panc1005 NGTsXVJCeG:ydH;zbZMhSXO|YYm= M1;QW|Eh|ryP MlK0NlQhcA>? MWnpcoR2[2W|IHHwc5B1d3Orcx?= Mo\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc0327 MmTSRZBweHSxc3nzJGF{e2G7 NVf4e3hvOSEQvF2= MmW1NlQhcA>? MV\pcoR2[2W|IHHwc5B1d3Orcx?= NF3GOpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0203 MnK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHVOFghcA>? MVjFR|UxRTJ{LkKg{txO MnjmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
PL45 M3PmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jzfVQ5KGh? Mk\HSWM2OD1{MD64JO69VQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc1005 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPPWZdjPDhiaB?= NGqwRWFGSzVyPUGuNUDPxE1? NHfRWnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0403 NV76bFh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;tfpU1QCCq NXTpSpU6TUN3ME2xMlEh|ryP MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
BxPc3 NWK2PYNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXKUHA1QCCq NVHuZlJMTUN3ME2xMlAh|ryP M{n1OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
MiaPaCa2 NHjBSJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL5cmNkPDhiaB?= NYHHUXBKTUN3ME2wMlch|ryP NGLGXmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0327 NWL2[IkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYi0PEBp MoXVSWM2OD1yLkWg{txO M1W1RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
AsPc1 M{D0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XnT|Q5KGh? MoXKSWM2OD1yLkOg{txO NWru[|NlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
PC9 M3LWWGZ2dmO2aX;uJGF{e2G7 NFLHWY8xNjVxMT:yJO69VQ>? NX3MNWQxPCCq MlX3SG1UVw>? MYLpcohq[mm2czD0bIUhdGW4ZXzzJI9nKEGtdDCodE1Cc3RrIHHu[EBGT0[U M1W3fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H1650 NXvW[Y5LTnWwY4Tpc44hSXO|YYm= NUm4[2FzOC53L{GvNkDPxE1? NHuyc2k1KGh? NEC4O3VFVVOR NUX3THZbcW6qaXLpeJMhfGinIHzleoVteyCxZjDBb5QhMHBvQXv0LUBidmRiRVfGVi=> M4LGZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H460 NWDufppzTnWwY4Tpc44hSXO|YYm= NW\SS2NSOC53L{GvNkDPxE1? MVO0JIg> MVXEUXNQ MUnpcohq[mm2czD0bIUhdGW4ZXzzJI9nKEGtdDCodE1Cc3RrIHHu[EBGT0[U MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
PC9 NUC4VlZbTnWwY4Tpc44hSXO|YYm= M{mzVVUxOMLibl2= M4TIZlI1yqCq MWHEUXNQ NXTJdIkx\GWlcnXhd4V{KEWJRmKg[ZhxemW|c3nvci=> M4H3e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H1650 MX7GeY5kfGmxbjDBd5NigQ>? MWq1NFDDqG6P NEm4fHAzPMLiaB?= NFjUOnNFVVOR M1Owb4Rm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= NX3BUWJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H460 NFPKcVdHfW6ldHnvckBCe3OjeR?= NHTYbYU2ODEEoH7N NUHFO|BjOjUEoHi= NVqxWnF4TE2VTx?= NFL5Tlhl\WO{ZXHz[ZMhTUeIUjDlfJBz\XO|aX;u MkLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
HCC4006 M{G0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLXPVM4OsLiaB?= MnruSG1UVw>? MonETWM2OD1yLkS2JO69VQ>? NGLiV2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
HCC2935 M4f1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC5[4M2PzMEoHi= M2HmO2ROW09? MmnVTWM2OD1yLkm3JO69VQ>? NXjKOmJDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
HCC827 NH7uNY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\NcFczyqCq M{\hTWROW09? MnnSTWM2OD1yLkK5JO69VQ>? NUXtPHpjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
HCC2279 NGrHWpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVG3NuKhcA>? MX3EUXNQ NW\mT5JTUUN3ME2wMlQh|ryP M{DU[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
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H820 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HGR|czyqCq M1nOS2ROW09? NHnrd2dKSzVyPUCuOEDPxE1? NH34bXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H1650 M4jqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TPVFczyqCq Mkf0SG1UVw>? MX3JR|UxRTBwOEig{txO MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
H1975 NYXP[|F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[3NuKhcA>? M2LFfGROW09? M{fLXmlEPTB;MD62PEDPxE1? NFP5ZYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H520 NFjPUXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq5O|LDqGh? M1f2cmROW09? NUDyUnJ4UUN3ME2wMlc2KM7:TR?= M3vFZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
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H460 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[3NuKhcA>? MXnEUXNQ M{D4fGlEPTB;MD64OkDPxE1? MoXNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H1666 MnHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu3[otTPzMEoHi= Mmj4SG1UVw>? NFqxTnVKSzVyPkGwJO69VQ>? NH3VWlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
PANC-1 M4HFO2Z2dmO2aX;uJGF{e2G7 NIi5XlMyOMLizszN MV6yM|QhcA>? M2nGbWROW09? M2PMOIlv[3KnYYPld{BqdnS{YXPlcIx2dGG{IGLPV{Bt\X[nbB?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd2M{G5PEc,OjN5NEOxPVg9N2F-
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HL60 MY\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Mnf0OFghcHK| MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m1NEA:KDFwMEmg{txONg>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN2NES4O{c,Ojd|NES0PFc9N2F-
K562 NV6yVJBrSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4fpcFQ5KGi{cx?= MkTORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkGg{txONg>? NX3aToZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1N|M5PzNpPkK5OVM{QDd|PD;hQi=>
PC3 NH6x[3RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NIDPd4k1QCCqcoO= MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS5|IN88UU4> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV|M{i3N{c,Ojl3M{O4O|M9N2F-
NFF M2WzVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NG[2V4k4OiCqcoO= NIjnXpREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPTkZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFEvPCEQvF2u NEHHV5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK0NVEyOid-MkiyOFEyOTJ:L3G+
HEK293 NYHWT|lrS3m2b4TvfIlkcXS7IHHzd4F6 M3HrRVQ5KGi{cx?= MnHiR5l1d3SxeHnjbZR6KGGpYXnud5QhUEWNMkmzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSC{ZYPhfpVzcW5iYYPzZZktKEmFNUCgQUAyNjRizszNMi=> M2HPcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkSxNVEzLz5{OEK0NVEyOjxxYU6=
NFF M2PSZWN6fG:2b4jpZ4l1gSCjc4PhfS=> Mo\TO|IhcHK| NWfUPXRRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVk[IIHPlcIx{KGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxKD1iMT60NkDPxE1w MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ2NUSwNkc,OzB{NEW0NFI9N2F-
HEK293 M3zpVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHHHcpc1QCCqcoO= NFjoc|FEgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IILld4F7fXKrbjDkfYUh[mG|ZXSgZZN{[XluIFnDOVAhRSBzLkSyJO69VS5? M2X5elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkS1OFAzLz5|MEK0OVQxOjxxYU6=
RAW264.7 NUDkT3dySW62aT3pcoZt[W2vYYTvdpkh[XO|YYm= M2DuU|EhcHJ? NGDa[3dCdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCwaYTybYMhd3irZHWgdJJw\HWldHnvckBxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCOUGOgd5RqdXWuYYTpc44h\m:{IEK0JIhzeyCkeTDHdolme3NicnXh[4VvfCCkYYPl[EBie3OjeTygTWM2OCB;IEKuNkDPxE1w NEHrdJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGxN|g4PSd-MkWxNVM5PzV:L3G+
RAW264.7 M2noN2FvfGlvaX7mcIFudWG2b4L5JIF{e2G7 NH7sSJoyKGi{ NFvBOm9CdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh[mWob4LlJGxRWyC|dHnteYxifGmxbjDmc5IhOjRiaILzJIJ6KEWOSWPBJI1mfGixZDygTWM2OCB;IESuO{DPxE1w NWjOO21pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNVM5PzVpPkK1NVE{QDd3PD;hQi=>
RAW264.7 NWL4b|MxSW62aT3pcoZt[W2vYYTvdpkh[XO|YYm= NU\mfZgzOSCqch?= M2q0UWFvfGlvaX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKEySUz3zeIlufWyjdHXkJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKFCJRUKgdJJw\HWldHnvckBxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCOUGOgd5RqdXWuYYTpc44h\m:{IEK0JIhzeyCkeTDlcpp6dWViaX3teY5w[XO|YYmgcYV1cG:mLDDJR|UxKD1iOD6yPEDPxE1w NVXyTJdIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNVM5PzVpPkK1NVE{QDd3PD;hQi=>
Huh-luc/neo7 MojRSpVv[3Srb36gZZN{[Xl? M1r2NFEhfU1? NVW2V5BlOSC2bzCzJIhzew>? NWTZTJNFUW6qaXLpeIlwdiCxZjDISGFEKGOuYYPzJFEhcW5iaIXtZY4hUHWqLXz1Z{9v\W95IHPlcIx{KGG|c3Xzd4VlKGG|IHjpd5RwdmViSEOgZYNmfHmuYYTpc44h[XRiMTD1UUBi\nSncjCxJJRwKDNiaILzJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> Mn;NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{ewNVcoRjJ3OUO3NFE4RC:jPh?=
PC3 MWTGeY5kfGmxbjDhd5NigQ>? MWWwMlMhfU1? NFTFdW41QCCqcoO= MY\Jcohq[mm2aX;uJI9nKEiGQVOgbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHHtc5VvfCCxZjDhZ4V1gWyjdHXkJIhqe3SxbnWgTFMh[XRiMD6zJJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN2NES4O{c,Ojd|NES0PFc9N2F-
HCT116 M{jEXmZ2dmO2aX;uJIF{e2G7 M3W3fFAvOyC3TR?= M1\3TVQ5KGi{cx?= NV7UdlRNUW6qaXLpeIlwdiCxZjDISGFEKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCjbX;1cpQhd2ZiYXPleJlt[XSnZDDobZN1d26nIFizJIF1KDBwMzD1UUBi\nSncjC0PEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN2NES4O{c,Ojd|NES0PFc9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-H2AX(Ser139) / KU70 / KU80 / RAD51 / RAD52 / ERCC1 ; 

PubMed: 24155971     


increasing doses of PXD101 enhanced degradation of KU70, KU80 and RAD51, and enhanced expression of p-H2AX (Ser139), RAD52 and ERCC1 in BHP7-13, WRO82-1 and 8505C.

Acetyl Histone H3 / Acetyl Histone H4 / Acetyl tubulin; 

PubMed: 24155971     


PXD101 induced acetylation of histone H3 and histone H4 in a dose-dependent manner. PXD101 also increased acetylation of tubulin in BHP7-13, WRO82-1 and 8505C.

p21 / p27 ; 

PubMed: 23982416     


(A and B) The cell lines shown were treated with PXD101 for 0, 2, 4, 8, 24, 48, and 72 h. Whole cell extracts were generated and subjected to western blotting with antibodies against p21, p27, hsp90, α-tubulin, or GAPDH. PXD101-resistant cell lines are shown in (A, left) while PXD101-sensitive cell lines are shown in (B, right). 

SOS1 / SOS2; 

PubMed: 28397399     


(A) Cell lysates were harvested from lung SCC cells after treatment with increasing doses of belinostat (PXD101) (0.1, 0.2, 0.3, 1, 3 μm) to evaluate the changes in SOS1 and SOS2. 

PARP / p-ERK / p-p38 / p38 / p-BRAF / p-MEK / MEK ; 

PubMed: 28397399     


Cell lysates were harvested from lung SCC cells after treatment with increasing doses of belinostat (0.1, 0.2, 0.3, 1, 3 μm). Immunoblotting was performed to evaluate the changes in phosphorylated protein levels of the targets identified in 1D (ERK1/2, p38, B‐Raf, MEK1/2) as well as PARP. β‐Actin shown as loading control. 

24155971 23982416 28397399
Growth inhibition assay
Cell viability; 

PubMed: 24155971     


Dose-response curves were obtained on day 4 from cells treated with a series of six 1:1 dilutions of PXD101. 

IC50; 

PubMed: 28397399     


Lung SCC cell lines and normal lung fibroblast cell lines were treated with belinostat (PXD101) for 72 h, and cell viability was determined with CellTiter assay. Data are represented as mean IC50 ± SD (n = 3).

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

Kinase Assay:[1]
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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]
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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:[1]
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  • 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 powder
in solvent
Synonyms NSC726630, PX-105684
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

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)
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma October 29 2020 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 Recruiting Drug: Belinostat IV Solid Tumors|Hematological Malignancies Acrotech Biopharma LLC|Axis Clinicals Limited March 2016 Phase 1
NCT02679131 Terminated Drug: Belinostat Relapsed/Refractory Solid Tumors/Hematological Malignancies Acrotech Biopharma LLC|Axis Clinicals Limited March 2016 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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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