Belinostat (PXD101)

Catalog No.S1085 Synonyms: PXD101,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 88 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 Mlq5SpVv[3Srb36gRZN{[Xl? MkDYNE46yqEQvF5CpC=> MYWyOEBp MX;kc5dvNXKnZ4XsZZR{KFSVIIDyc5RmcW5ibHX2[Yx{KGGodHXyJFbDqGhiaX7jeYJifGmxbh?= MkX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdzMkS1PVQoRjF5MUK0OVk1RC:jPh?=
HCT116 M{TwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPuVnI1QCCq NH;le|FGSzVyPUCuNlgh|ryP NGLzVHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyOFU6PCd-MUexNlQ2QTR:L3G+
Granta-519 NHnESVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK3NlQhcA>? NX22VGU6UUN3ME21Ok4{KM7:TR?= M3y5PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyME[4NFgxLz5{MEC2PFA5ODxxYU6=
Jeko-1 NYfhb5RVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;yOXdjOjRiaB?= M3HyUWlEPTB;MD6yJO69VQ>? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB4OEC4NEc,OjByNkiwPFA9N2F-
HBL-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXkNlQhcA>? NFv2ZotKSzVyPUCuOEDPxE1? Mne2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNkiwPFAoRjJyME[4NFgxRC:jPh?=
Panc-1  NVTuXVJxSXCxcITvd4l{KEG|c3H5 MmrxNVAxNzVyMD:xNFAxKG6P MYe0PEBp NYi2[JBLcW6mdXPld{Bld3OnIHTldIVv\GWwdDDhdI9xfG:|aYO= Ml\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
AsPC-1 NVLkdmdMSXCxcITvd4l{KEG|c3H5 NFf3fpEyODBxNUCwM|ExODBibl2= NFfNUIU1QCCq MWXpcoR2[2W|IHTvd4Uh\GWyZX7k[Y51KGGyb4D0c5Nqew>? M4fpc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
T3M4 M3ewR2Fxd3C2b4Ppd{BCe3OjeR?= NGn0RpYyODBxNUCwM|ExODBibl2= NV;KSVQ4PDhiaB?= Ml;tbY5lfWOnczDkc5NmKGSncHXu[IVvfCCjcH;weI9{cXN? M1HNNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
Panc-1  NFTibIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFeyZWgxNThyMDDuUS=> M1vjT|Q5KGh? NGXROmpqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ6MU[5PEc,OjJ4OEG2PVg9N2F-
AsPC-1 NUfhbZlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnCVVUxNThyMDDuUS=> MXu0PEBp MlrkbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy Mo\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
T3M4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvvNE05ODBibl2= NFjWW3A1QCCq NFSxNlhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Mn\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
MiaPaCa2 Mnz6SpVv[3Srb36gRZN{[Xl? NFHCNHMyNzFyIN88US=> Ml36NlQhcA>? NYW1OpZ3cW6mdXPld{Ah\3Kxd4ToJIFzemW|dHXkJIlvKEd{L12= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
AsPc1 MXzGeY5kfGmxbjDBd5NigQ>? M1vqW|EwOTBizszN NY\tOWoyOjRiaB?= MWPpcoR2[2W|IDDndo94fGhiYYLy[ZN1\WRiaX6gS|IwVQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc0403 MX3BdI9xfG:|aYOgRZN{[Xl? M3W0fFEh|ryP M{nXfFI1KGh? NIT2OFZqdmS3Y3XzJIFxd3C2b4Ppdy=> Mnr5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc1005 MVLBdI9xfG:|aYOgRZN{[Xl? M4XzVFEh|ryP NF[yXXUzPCCq NHSwUYpqdmS3Y3XzJIFxd3C2b4Ppdy=> NGnuTVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0327 NWjkcHN{SXCxcITvd4l{KEG|c3H5 M3OxflEh|ryP MlvUNlQhcA>? NWnqWJB2cW6mdXPld{BieG:ydH;zbZM> NIDuTpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0203 M1zvdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfSNZM1QCCq M4HHNmVEPTB;MkKuNkDPxE1? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
PL45 M1vWbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkSyOFghcA>? MXnFR|UxRTJyLkig{txO M4\CTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
Panc1005 NEfZdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYW0TFZlPDhiaB?= MonlSWM2OD1zLkGg{txO NWj2Zmt4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc0403 NW\BUYtIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDaVZUyPDhiaB?= NES2N2FGSzVyPUGuNUDPxE1? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
BxPc3 NHToXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MomxOFghcA>? M1nQfGVEPTB;MT6wJO69VQ>? M1zKXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
MiaPaCa2 NXfSXZo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUC0PEBp MVTFR|UxRTBwNzFOwG0> M4HrOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
Panc0327 M{Hvcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXxfnc1QCCq MYfFR|UxRTBwNTFOwG0> NWHlZWt5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
AsPc1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HnOVQ5KGh? M1z5S2VEPTB;MD6zJO69VQ>? NX3Ee2VlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
PC9 NEP2[llHfW6ldHnvckBCe3OjeR?= NHmxcZcxNjVxMT:yJO69VQ>? MV60JIg> MVnEUXNQ NFruRpNqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S NVHTb|V[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H1650 MkXWSpVv[3Srb36gRZN{[Xl? MXSwMlUwOS9{IN88US=> MoXSOEBp NXrjTHZPTE2VTx?= Ml33bY5pcWKrdIOgeIhmKGyndnXsd{Bw\iCDa4SgLJAuSWu2KTDhcoQhTUeIUh?= NUjYTpdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H460 NF3LWY1HfW6ldHnvckBCe3OjeR?= MXuwMlUwOS9{IN88US=> MofwOEBp NVexVZlZTE2VTx?= MmDBbY5pcWKrdIOgeIhmKGyndnXsd{Bw\iCDa4SgLJAuSWu2KTDhcoQhTUeIUh?= Mn\aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
PC9 NGnjd4VHfW6ldHnvckBCe3OjeR?= MXW1NFDDqG6P MkX5NlTDqGh? M4LxPWROW09? NFLFNmNl\WO{ZXHz[ZMhTUeIUjDlfJBz\XO|aX;u MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
H1650 M4DlSmZ2dmO2aX;uJGF{e2G7 NGTndGc2ODEEoH7N MkT0NlTDqGh? MoH0SG1UVw>? NHPJVWFl\WO{ZXHz[ZMhTUeIUjDlfJBz\XO|aX;u MlrmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H460 M4rjSGZ2dmO2aX;uJGF{e2G7 MWS1NFDDqG6P NGfYSlczPMLiaB?= M3j6PWROW09? NH\1cY1l\WO{ZXHz[ZMhTUeIUjDlfJBz\XO|aX;u MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
HCC4006 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrpS2VWPzMEoHi= M1TXNGROW09? MYPJR|UxRTBwNE[g{txO Ml3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
HCC2935 MlTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDGO|LDqGh? M3HBUGROW09? NXy2NFhuUUN3ME2wMlk4KM7:TR?= NUTCRYdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
HCC827 M2\3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTXRoFqPzMEoHi= Ml3HSG1UVw>? MmT5TWM2OD1yLkK5JO69VQ>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
HCC2279 M2XUb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnnWXo4OsLiaB?= NGjFcGNFVVOR M124bWlEPTB;MD60JO69VQ>? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
PC9 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf1ToE4OsLiaB?= Mn21SG1UVw>? MWrJR|UxRTBwMkmg{txO MlXuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H820 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fMcFczyqCq MlnFSG1UVw>? MVTJR|UxRTBwNDFOwG0> MofXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H1650 NVrvXnRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;UfFI4OsLiaB?= MmCySG1UVw>? NEO1WpNKSzVyPUCuPFgh|ryP MoG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H1975 M13iSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DwSFczyqCq MoDBSG1UVw>? NWPDdG9WUUN3ME2wMlY5KM7:TR?= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
H520 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVmyV4RXPzMEoHi= NIPhNIZFVVOR M2GzUmlEPTB;MD63OUDPxE1? NEPPUow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H1299 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDVR2w4OsLiaB?= M4jjd2ROW09? M3fFbWlEPTB;MT6yJO69VQ>? MlLTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H460 M1TaTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HDW|czyqCq M3;nRmROW09? NV35coFZUUN3ME2wMlg3KM7:TR?= M1u1SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H1666 M1XkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[4OYw4OsLiaB?= M1:5e2ROW09? NX2z[YFLUUN3ME6xNEDPxE1? Ml:yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
PANC-1 MnLLSpVv[3Srb36gRZN{[Xl? Ml7iNVDDqM7:TR?= M1rpUVIwPCCq MmL2SG1UVw>? MmSzbY5kemWjc3XzJIlvfHKjY3XscJVt[XJiUl;TJIxmfmWu NIDhZpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e0N|E6QCd-MkO3OFMyQTh:L3G+
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K562 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGOwV|Q1QCCqcoO= MojGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkGg{txONg>? MknzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3M{O4O|MoRjJ7NUOzPFc{RC:jPh?=
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NFF MoH2R5l1d3SxeHnjbZR6KGG|c3H5 MkfEO|IhcHK| MkHsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmZHKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCxMlQh|ryPLh?= NVj5NXM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyOFEyOTJpPkK4NlQyOTF{PD;hQi=>
HEK293 MnLCR5l1d3SxeHnjbZR6KGG|c3H5 MXe0PEBpenN? Mni3R5l1d3SxeHnjbZR6KGGpYXnud5QhUEWNMkmzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSC{ZYPhfpVzcW5iYYPzZZktKEmFNUCgQUAyNjRizszNMi=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ2MUGxNkc,Ojh{NEGxNVI9N2F-
NFF MWnDfZRwfG:6aXPpeJkh[XO|YYm= M3XsbVczKGi{cx?= MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOSmYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEmFNUCgQUAyNjR{IN88UU4> NHn5do09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK0OVQxOid-M{CyOFU1ODJ:L3G+
HEK293 MmnoR5l1d3SxeHnjbZR6KGG|c3H5 NFLjZYM1QCCqcoO= NH;yRoxEgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IILld4F7fXKrbjDkfYUh[mG|ZXSgZZN{[XluIFnDOVAhRSBzLkSyJO69VS5? MmnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NEW0NFIoRjNyMkS1OFAzRC:jPh?=
RAW264.7 MYTBcpRqNWmwZnzhcY1ifG:{eTDhd5NigQ>? MV2xJIhz M{P6OWFvfGlvaX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKEySUz3zeIlufWyjdHXkJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKG6rdILpZ{BwgGmmZTDwdo9lfWO2aX;uJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKEySUzDzeIlufWyjdHnvckBnd3JiMkSgbJJ{KGK7IFfybYV{eyC{ZXHn[Y51KGKjc3XkJIF{e2G7LDDJR|UxKD1iMj6yJO69VS5? MlS2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUO4O|UoRjJ3MUGzPFc2RC:jPh?=
RAW264.7 M2nsTWFvfGlvaX7mcIFudWG2b4L5JIF{e2G7 NGG2RXIyKGi{ M{nnXGFvfGlvaX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKEySUz3zeIlufWyjdHXkJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKFSQRnHsdIhiKHC{b3T1Z5Rqd25icILlMYlv[3WkYYTl[EBnd3JiMTDodkBj\W[xcnWgUHBUKHO2aX31cIF1cW:wIH\vdkAzPCCqcoOgZpkhTUyLU1GgcYV1cG:mLDDJR|UxKD1iND63JO69VS5? MkLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUO4O|UoRjJ3MUGzPFc2RC:jPh?=
RAW264.7 MXfBcpRqNWmwZnzhcY1ifG:{eTDhd5NigQ>? M2DEe|EhcHJ? M1;QT2FvfGlvaX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKEySUz3zeIlufWyjdHXkJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKFCJRUKgdJJw\HWldHnvckBxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCOUGOgd5RqdXWuYYTpc44h\m:{IEK0JIhzeyCkeTDlcpp6dWViaX3teY5w[XO|YYmgcYV1cG:mLDDJR|UxKD1iOD6yPEDPxE1w NH\GNZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGxN|g4PSd-MkWxNVM5PzV:L3G+
Huh-luc/neo7 NYHWdHY6TnWwY4Tpc44h[XO|YYm= MlnQNUB2VQ>? MX2xJJRwKDNiaILz MXzJcohq[mm2aX;uJI9nKEiGQVOgZ4xie3NiMTDpckBpfW2jbjDIeYgudHWlL37lc|ch[2WubIOgZZN{\XO|ZXSgZZMhcGm|dH;u[UBJOyCjY3X0fYxifGmxbjDheEAyKHWPIHHmeIVzKDFidH:gN{BpenNiYomgW4V{fGW{bjDicI91fGmwZzDhcoFtgXOrcx?= M2D6T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUO3NFE4Lz5{NUmzO|AyPzxxYU6=
PC3 NUe1ZnJWTnWwY4Tpc44h[XO|YYm= NU\QXpRIOC5|IIXN M{HqVFQ5KGi{cx?= NEnuN2FKdmirYnn0bY9vKG:oIFjERWMhcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJIFud3WwdDDv[kBi[2W2eXzheIVlKGirc4TvcoUhUDNiYYSgNE4{KHWPIHHmeIVzKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= Mof6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|NES0PFcoRjJ5M{S0OFg4RC:jPh?=
HCT116 MlrvSpVv[3Srb36gZZN{[Xl? Mo\DNE4{KHWP M1rvXFQ5KGi{cx?= MnX0TY5pcWKrdHnvckBw\iCKRFHDJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBidW:3boSgc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|IHH0JFAvOyC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NF\HPJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O0OFQ5Pyd-MkezOFQ1QDd:L3G+
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.
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.

Solubility (25°C)

In vitro

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

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 2022-08-01)

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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