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 87 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 NWf5fFh3TnWwY4Tpc44hSXO|YYm= M3PuS|AvQcLizszNxsA> M{nRVlI1KGh? M{nrWoRwf25vcnXneYxifHNiVGOgdJJwfGWrbjDs[ZZmdHNiYX\0[ZIhPsLiaDDpcoN2[mG2aX;u M1vZWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MUK0OVk1Lz5zN{GyOFU6PDxxYU6=
HCT116 NHXuW|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[0PEBp NVi1ZpJCTUN3ME2wMlI5KM7:TR?= NIf6UXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyOFU6PCd-MUexNlQ2QTR:L3G+
Granta-519 M3\C[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLkNlQhcA>? NYnMXY5KUUN3ME21Ok4{KM7:TR?= Mn7hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNkiwPFAoRjJyME[4NFgxRC:jPh?=
Jeko-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjXS3FVOjRiaB?= NYXFXmhTUUN3ME2wMlIh|ryP M{PlRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyME[4NFgxLz5{MEC2PFA5ODxxYU6=
HBL-2 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrqSVEzPCCq NHjjSplKSzVyPUCuOEDPxE1? NHy2Tmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC2PFA5OCd-MkCwOlgxQDB:L3G+
Panc-1  MVnBdI9xfG:|aYOgRZN{[Xl? M2K4e|ExOC93MECvNVAxOCCwTR?= M1zkSlQ5KGh? M3nDXIlv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| NYnX[GR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
AsPC-1 MWPBdI9xfG:|aYOgRZN{[Xl? NVrkZ2ZQOTByL{WwNE8yODByIH7N Mn3FOFghcA>? NHvZRnRqdmS3Y3XzJIRwe2ViZHXw[Y5l\W62IHHwc5B1d3Orcx?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ6MU[5PEc,OjJ4OEG2PVg9N2F-
T3M4 M1nrT2Fxd3C2b4Ppd{BCe3OjeR?= M3nqUlExOC93MECvNVAxOCCwTR?= NGfRcmM1QCCq MmjubY5lfWOnczDkc5NmKGSncHXu[IVvfCCjcH;weI9{cXN? M{fGZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
Panc-1  MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKwMVgxOCCwTR?= NEK4WXc1QCCq MUXpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M4m1clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
AsPC-1 MlXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnlSmMxNThyMDDuUS=> NF:wPIM1QCCq M4fofolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M33xXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
T3M4 M33kN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[wMVgxOCCwTR?= M3rSeFQ5KGh? NGL2NnhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MmLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
MiaPaCa2 NFK2clRHfW6ldHnvckBCe3OjeR?= NUDIXGJJOS9zMDFOwG0> MnfjNlQhcA>? NWftcY42cW6mdXPld{Ah\3Kxd4ToJIFzemW|dHXkJIlvKEd{L12= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
AsPc1 MXrGeY5kfGmxbjDBd5NigQ>? NFzTR|cyNzFyIN88US=> NWLq[Y85OjRiaB?= M2nqNYlv\HWlZYOgJIdzd3e2aDDhdpJme3SnZDDpckBIOi:P NIDnSJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0403 NU\PWGFJSXCxcITvd4l{KEG|c3H5 NWDNc2FROSEQvF2= NETpNlIzPCCq NFfQWIFqdmS3Y3XzJIFxd3C2b4Ppdy=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc1005 M2PaU2Fxd3C2b4Ppd{BCe3OjeR?= NXT2clNQOSEQvF2= M{nmfVI1KGh? NWLXOpNycW6mdXPld{BieG:ydH;zbZM> MkDWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc0327 NI\qTG5CeG:ydH;zbZMhSXO|YYm= MkDlNUDPxE1? NIntS3gzPCCq MXfpcoR2[2W|IHHwc5B1d3Orcx?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc0203 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[0PEBp MkDqSWM2OD1{Mj6yJO69VQ>? MnPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
PL45 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWi0PEBp MYrFR|UxRTJyLkig{txO MmfHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc1005 MnTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVO0PEBp MUjFR|UxRTFwMTFOwG0> MnL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc0403 NXfCb4RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDXNIE1QCCq MUXFR|UxRTFwMTFOwG0> NGLwTWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
BxPc3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO0fHV6PDhiaB?= M{PKXmVEPTB;MT6wJO69VQ>? M2\QblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
MiaPaCa2 M1zxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjLOFghcA>? NV7ySoprTUN3ME2wMlch|ryP M4rwPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
Panc0327 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfzOFghcA>? M{K5O2VEPTB;MD61JO69VQ>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
AsPc1 NYXtPVBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDmXWFSPDhiaB?= MXzFR|UxRTBwMzFOwG0> NGPMOlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
PC9 MVHGeY5kfGmxbjDBd5NigQ>? Mme3NE42NzFxMjFOwG0> MoXrOEBp NWDiW4tJTE2VTx?= NFH2NJdqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S NUjjbmhyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H1650 NIiwW3RHfW6ldHnvckBCe3OjeR?= NWHFW5VwOC53L{GvNkDPxE1? NH;zRoc1KGh? NYPicld3TE2VTx?= M{XhSIlvcGmkaYTzJJRp\SCuZY\lcJMhd2ZiQXv0JEhxNUGtdDmgZY5lKEWJRmK= NVrTN401RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H460 M{[0RWZ2dmO2aX;uJGF{e2G7 M4C5fVAvPS9zL{Kg{txO M1XH[|QhcA>? Mme0SG1UVw>? NVKzfZI4cW6qaXLpeJMhfGinIHzleoVteyCxZjDBb5QhMHBvQXv0LUBidmRiRVfGVi=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
PC9 NXKySVRLTnWwY4Tpc44hSXO|YYm= NXPzNmtiPTBywrDuUS=> MU[yOOKhcA>? NEjpSpBFVVOR M4nLNoRm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= NXe5Um51RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H1650 NFvwenNHfW6ldHnvckBCe3OjeR?= M4rh[lUxOMLibl2= NWPmZ3BNOjUEoHi= MXLEUXNQ M2PtS4Rm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= NHHu[HY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H460 MYnGeY5kfGmxbjDBd5NigQ>? MVy1NFDDqG6P MlXvNlTDqGh? M3;aOGROW09? M4L5XYRm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= NWHTeWtkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
HCC4006 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[3NuKhcA>? MX;EUXNQ NV7mZXJFUUN3ME2wMlQ3KM7:TR?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
HCC2935 M4TRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ztZlczyqCq MWPEUXNQ NVPDfHVFUUN3ME2wMlk4KM7:TR?= MnfTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
HCC827 M3;QVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzzZ49LPzMEoHi= NVmyRZNjTE2VTx?= NYGyOmpoUUN3ME2wMlI6KM7:TR?= MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
HCC2279 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXu3NuKhcA>? NWfnVZd6TE2VTx?= NE[xOppKSzVyPUCuOEDPxE1? NW\NXZo{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
PC9 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPURZY4OsLiaB?= M{SwdGROW09? MnfwTWM2OD1yLkK5JO69VQ>? M4TWbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H820 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnKwO|LDqGh? MkHPSG1UVw>? MYXJR|UxRTBwNDFOwG0> NWjOfJNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H1650 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnqVI5CPzMEoHi= MX7EUXNQ MoX2TWM2OD1yLki4JO69VQ>? MoHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H1975 NY\CZmtnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7EVIVUPzMEoHi= M1HTOGROW09? NVvLWW5[UUN3ME2wMlY5KM7:TR?= NXjkNGVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H520 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV63VpNoPzMEoHi= NILKeJdFVVOR NG\4RXRKSzVyPUCuO|Uh|ryP MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
H1299 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL6O|LDqGh? MnLiSG1UVw>? MljHTWM2OD1zLkKg{txO Ml\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H460 NFG2OVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXe3NuKhcA>? MoTqSG1UVw>? MlvrTWM2OD1yLki2JO69VQ>? M2jBVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H1666 MnHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\uO|LDqGh? NG\IZWdFVVOR MWTJR|UxRjFyIN88US=> M1n2PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
PANC-1 M{\JPWZ2dmO2aX;uJGF{e2G7 NYLEUINxOTEEoN88US=> NInoNIMzNzRiaB?= MluwSG1UVw>? NGLS[lhqdmO{ZXHz[ZMhcW62cnHj[YxtfWyjcjDSU3MhdGW4ZXy= NGDvSlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e0N|E6QCd-MkO3OFMyQTh:L3G+
PANC-1 NVnzdYhrS2WubDDWbYFjcWyrdImgRZN{[Xl? NV61WHVsOS9zMNMg{txO NETXWpo1QCCq NXLRb|d[TE2VTx?= MWTk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd2M{G5PEc,OjN5NEOxPVg9N2F-
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NFF M3LXSGN6fG:2b4jpZ4l1gSCjc4PhfS=> MofBO|IhcHK| MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOSmYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IEGuOEDPxE1w M1nX[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkSxNVEzLz5{OEK0NVEyOjxxYU6=
HEK293 NEPL[GtEgXSxdH;4bYNqfHliYYPzZZk> MV20PEBpenN? M3TD[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEiHS{K5N{Bk\WyuczDh[pRmeiB2ODDodpMh[nlicnXzZZp2emmwIHHzd4F6NCCLQ{WwJF0hOS52IN88UU4> NWfDOW1LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyOFEyOTJpPkK4NlQyOTF{PD;hQi=>
NFF MofnR5l1d3SxeHnjbZR6KGG|c3H5 NUPacoVIPzJiaILz M2PzNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5HTiClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NEA:KDFwNEKg{txONg>? Mn3HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NEW0NFIoRjNyMkS1OFAzRC:jPh?=
HEK293 NVrucGRYS3m2b4TvfIlkcXS7IHHzd4F6 NHXTXoQ1QCCqcoO= NWHqbXZCS3m2b4TvfIlkcXS7IHHnZYlve3RiSFXLNlk{KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDy[ZNignW{aX6g[JlmKGKjc3XkJIF{e2G7LDDJR|UxKD1iMT60NkDPxE1w NUW0XWhXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOFU1ODJpPkOwNlQ2PDB{PD;hQi=>
RAW264.7 NUHydlRISW62aT3pcoZt[W2vYYTvdpkh[XO|YYm= NH3SXmsyKGi{ NXm3d2tFSW62aT3pcoZt[W2vYYTvdpkh[WO2aY\peJkhcW5iTGDTMZN1cW23bHH0[YQhdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2Zibnn0dolkKG:6aXTlJJBzd2S3Y4Tpc44heHKnLXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViTGDTJJN1cW23bHH0bY9vKG[xcjCyOEBpenNiYomgS5Jq\XO|IILlZYdmdnRiYnHz[YQh[XO|YYmsJGlEPTBiPTCyMlIh|ryPLh?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTFzM{i3OUc,OjVzMUO4O|U9N2F-
RAW264.7 M3XVU2FvfGlvaX7mcIFudWG2b4L5JIF{e2G7 NVLpS3JsOSCqch?= NHzCW5FCdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh[mWob4LlJGxRWyC|dHnteYxifGmxbjDmc5IhOjRiaILzJIJ6KEWOSWPBJI1mfGixZDygTWM2OCB;IESuO{DPxE1w NGTUdXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGxN|g4PSd-MkWxNVM5PzV:L3G+
RAW264.7 NULaNZFWSW62aT3pcoZt[W2vYYTvdpkh[XO|YYm= Mlz3NUBpeg>? M2PZdmFvfGlvaX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKEySUz3zeIlufWyjdHXkJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKFCJRUKgdJJw\HWldHnvckBxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCOUGOgd5RqdXWuYYTpc44h\m:{IEK0JIhzeyCkeTDlcpp6dWViaX3teY5w[XO|YYmgcYV1cG:mLDDJR|UxKD1iOD6yPEDPxE1w Mn3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUO4O|UoRjJ3MUGzPFc2RC:jPh?=
Huh-luc/neo7 M3L0emZ2dmO2aX;uJIF{e2G7 M{L2clEhfU1? NYT0UFNDOSC2bzCzJIhzew>? M1voemlvcGmkaYTpc44hd2ZiSFTBR{BkdGG|czCxJIlvKGi3bXHuJGh2cC2udXOvcoVwPyClZXzsd{Bie3Onc4Pl[EBieyCqaYP0c45mKEh|IHHj[ZR6dGG2aX;uJIF1KDFidV2gZYZ1\XJiMTD0c{A{KGi{czDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz NWfVNGZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|cxOTdpPkK1PVM4ODF5PD;hQi=>
PC3 M1XqZ2Z2dmO2aX;uJIF{e2G7 MX[wMlMhfU1? NIjY[lY1QCCqcoO= MX3Jcohq[mm2aX;uJI9nKEiGQVOgbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHHtc5VvfCCxZjDhZ4V1gWyjdHXkJIhqe3SxbnWgTFMh[XRiMD6zJJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NV32fmhvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezOFQ1QDdpPkK3N|Q1PDh5PD;hQi=>
HCT116 MUfGeY5kfGmxbjDhd5NigQ>? M1zDZlAvOyC3TR?= MX:0PEBpenN? Mkf0TY5pcWKrdHnvckBw\iCKRFHDJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBidW:3boSgc4Yh[WOndInsZZRm\CCqaYP0c45mKEh|IHH0JFAvOyC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NXLlWGdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezOFQ1QDdpPkK3N|Q1PDh5PD;hQi=>
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 2022-01-17)

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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