Belinostat (PXD101)

For research use only. Not for use in humans.

目录号:S1085 别名: NSC726630, PX-105684 中文名称:贝利司他

Belinostat (PXD101) Chemical Structure

CAS No. 414864-00-9

Belinostat (PXD101, NSC726630, PX-105684)是一种新型HDAC抑制剂,无细胞试验中IC50为27 nM,对耐Cisplatin的肿瘤具有活性。Belinostat (PXD101) 可诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1317.13 现货
RMB 981.69 现货
RMB 3030.32 现货
RMB 4653.78 现货
RMB 7950.07 现货
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客户使用Selleck生产的Belinostat (PXD101)发表文献74篇:

产品安全说明书

HDAC抑制剂选择性比较

生物活性

产品描述 Belinostat (PXD101, NSC726630, PX-105684)是一种新型HDAC抑制剂,无细胞试验中IC50为27 nM,对耐Cisplatin的肿瘤具有活性。Belinostat (PXD101) 可诱导自噬。
特性 Belinostat是Topotarget的领先药物,已经进行过多次临床试验。
靶点
HDAC [1]
(Cell-free assay)
27 nM
体外研究

Belinostat抑制肿瘤细胞生长(包括A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3,及HS852),IC50为0.2到0.66 μM。Belinostat 作用于A2780/cp70 和2780AD细胞时活性很低, 这两个细胞是抗cisplatin和doxorubicin的A2780细胞衍生的。Belinostat通过PARP分裂和组蛋白H3/H4的乙酰化而诱导细胞凋亡。[1] Belinostat抑制膀胱癌细胞生长,尤其是5637细胞,细胞在G0-G1期积累, 在S期下降,在 G2-M期上升。[2] Belinostat抑制细胞生长的活性不受多重耐药表现型的影响, 但是docetaxel的活性明显受影响。Belinostat 可以增强docetaxel或carboplatin 抑制OVCAR-3和A2780细胞的活性。Belinostat作用于卵巢癌细胞系也增强微管乙酰化作用。[3] 最新研究显示 Belinostat在TGF-β信号依赖机制中激活蛋白激酶A 和降低survivin mRNA。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 MkC3SpVv[3Srb36gRZN{[Xl? MYOwMlnDqM7:TdMg NXTTTo9zOjRiaB?= NGLqdWFld3ewLYLl[5Vt[XS|IGTTJJBzd3SnaX6gcIV3\Wy|IHHmeIVzKDcEoHigbY5kfWKjdHnvci=> M1fUTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MUK0OVk1Lz5zN{GyOFU6PDxxYU6=
HCT116 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGX2TZc1QCCq M2rmOWVEPTB;MD6yPEDPxE1? NGLxe2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyOFU6PCd-MUexNlQ2QTR:L3G+
Granta-519 M1W5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\SRlI1KGh? NGe5bVhKSzVyPUW2MlMh|ryP MmfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNkiwPFAoRjJyME[4NFgxRC:jPh?=
Jeko-1 NXLFdmV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLmZ5MzPCCq MoX4TWM2OD1yLkKg{txO NHnt[HY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEC2PFA5OCd-MkCwOlgxQDB:L3G+
HBL-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HqRVI1KGh? M2[3dWlEPTB;MD60JO69VQ>? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB4OEC4NEc,OjByNkiwPFA9N2F-
Panc-1  NX7Nbo9OSXCxcITvd4l{KEG|c3H5 M1LnfVExOC93MECvNVAxOCCwTR?= NH\aO3U1QCCq M1L2folv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| M1zqUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
AsPC-1 MVrBdI9xfG:|aYOgRZN{[Xl? NYWzW3JFOTByL{WwNE8yODByIH7N NWG3flZ5PDhiaB?= M1;W[Ylv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| NIjYclk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[4NVY6QCd-MkK2PFE3QTh:L3G+
T3M4 NFPsbnJCeG:ydH;zbZMhSXO|YYm= NIXacVIyODBxNUCwM|ExODBibl2= NYPyR5lZPDhiaB?= M{O5dolv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| NGnxSpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[4NVY6QCd-MkK2PFE3QTh:L3G+
Panc-1  NW\4dXo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\IfVAuQDByIH7N NX3YS|NtPDhiaB?= MlP5bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MljDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
AsPC-1 M1rnOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEm5VHMxNThyMDDuUS=> MXe0PEBp MlnSbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy M3rKZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
T3M4 NUS0VGVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P5bVAuQDByIH7N MYC0PEBp NHjmOXlqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M37QelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkixOlk5Lz5{Mk[4NVY6QDxxYU6=
MiaPaCa2 M3LsWGZ2dmO2aX;uJGF{e2G7 NFHwTWkyNzFyIN88US=> NWezVYdDOjRiaB?= NUDTcmVqcW6mdXPld{Ah\3Kxd4ToJIFzemW|dHXkJIlvKEd{L12= Ml3xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
AsPc1 NWm5O216TnWwY4Tpc44hSXO|YYm= NH3UT4IyNzFyIN88US=> M1r2fFI1KGh? MYTpcoR2[2W|IDDndo94fGhiYYLy[ZN1\WRiaX6gS|IwVQ>? Mk\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc0403 MnnRRZBweHSxc3nzJGF{e2G7 MUCxJO69VQ>? MlXPNlQhcA>? NVTsS4ZIcW6mdXPld{BieG:ydH;zbZM> NELhOVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc1005 M3fXSmFxd3C2b4Ppd{BCe3OjeR?= M1\6cFEh|ryP NVjETHFDOjRiaB?= MYXpcoR2[2W|IHHwc5B1d3Orcx?= NGrvS5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0327 Mn3ZRZBweHSxc3nzJGF{e2G7 MYKxJO69VQ>? NX3ZXnFGOjRiaB?= M4T6[olv\HWlZYOgZZBweHSxc3nz NIe4dZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc0203 M1XOS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zwXFQ5KGh? MoHnSWM2OD1{Mj6yJO69VQ>? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
PL45 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH4ZWVVPDhiaB?= M{PTZWVEPTB;MkCuPEDPxE1? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc1005 M{L2TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVO0PEBp M2PyPWVEPTB;MT6xJO69VQ>? MnLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc0403 NFTOfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLiOFghcA>? M3\VSWVEPTB;MT6xJO69VQ>? NIX6cIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
BxPc3 M4fjWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXkWWRRPDhiaB?= Mn3iSWM2OD1zLkCg{txO MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
MiaPaCa2 NF\UXnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzGOFghcA>? NHfiW5lGSzVyPUCuO{DPxE1? MnzxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
Panc0327 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXUUnU1QCCq NEPRPItGSzVyPUCuOUDPxE1? Mk\HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
AsPc1 M{njVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoGxOFghcA>? NUHBbIpbTUN3ME2wMlMh|ryP MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
PC9 MY\GeY5kfGmxbjDBd5NigQ>? MmLyNE42NzFxMjFOwG0> NHnJNHc1KGh? NH:1WY9FVVOR M1\BdolvcGmkaYTzJJRp\SCuZY\lcJMhd2ZiQXv0JEhxNUGtdDmgZY5lKEWJRmK= M1TNWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H1650 MUXGeY5kfGmxbjDBd5NigQ>? NVrKeHVtOC53L{GvNkDPxE1? NGq1d4c1KGh? M37M[mROW09? NIXQeolqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S M3LWTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H460 NXHlWnZsTnWwY4Tpc44hSXO|YYm= NVTIcpVOOC53L{GvNkDPxE1? NYfoXmZGPCCq MX7EUXNQ NEn4N5dqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S M4K4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
PC9 NXPmSI1bTnWwY4Tpc44hSXO|YYm= M{e4SlUxOMLibl2= MWmyOOKhcA>? MUPEUXNQ NFnRWXNl\WO{ZXHz[ZMhTUeIUjDlfJBz\XO|aX;u M4DFcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
H1650 M1rsPGZ2dmO2aX;uJGF{e2G7 MXq1NFDDqG6P NIXjfmszPMLiaB?= NGLjUHJFVVOR MX;k[YNz\WG|ZYOgSWdHWiCneIDy[ZN{cW:w MnrTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H460 NVLZVo1PTnWwY4Tpc44hSXO|YYm= M2P2dFUxOMLibl2= M3O2PVI1yqCq NHy2U29FVVOR NV;Gc415\GWlcnXhd4V{KEWJRmKg[ZhxemW|c3nvci=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
HCC4006 M1Ox[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWG3NuKhcA>? MWHEUXNQ NVLiTo1bUUN3ME2wMlQ3KM7:TR?= NH\MW3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
HCC2935 NWrTNm1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEWybFU4OsLiaB?= NV:wOG5rTE2VTx?= MnraTWM2OD1yLkm3JO69VQ>? NUnGOY1QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
HCC827 M1\sWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TIRVczyqCq NIjM[JZFVVOR NX3ZNIs1UUN3ME2wMlI6KM7:TR?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
HCC2279 M4\6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYq3NuKhcA>? NYLUdFF3TE2VTx?= MlXGTWM2OD1yLkSg{txO MkfEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
PC9 NX;nNmFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjMO|LDqGh? M{PXXmROW09? NFvETWhKSzVyPUCuNlkh|ryP NV7MdlN3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H820 M17UTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXu3NuKhcA>? M{fmU2ROW09? M{G5dWlEPTB;MD60JO69VQ>? M1TvNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
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H1975 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHO1UYU4OsLiaB?= M{jxWGROW09? NHXiWZVKSzVyPUCuOlgh|ryP M3zpV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUG1O|UzLz5{M{WxOVc2OjxxYU6=
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H460 Mn7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1X6TFczyqCq MV3EUXNQ NUPyRoEzUUN3ME2wMlg3KM7:TR?= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
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PC3 NGniXoVHfW6ldHnvckBie3OjeR?= NEnzOXQxNjNidV2= M1LWXVQ5KGi{cx?= MWPJcohq[mm2aX;uJI9nKEiGQVOgbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHHtc5VvfCCxZjDhZ4V1gWyjdHXkJIhqe3SxbnWgTFMh[XRiMD6zJJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NInF[5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O0OFQ5Pyd-MkezOFQ1QDd:L3G+
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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. 

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. 

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). 

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.

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.

28397399 23982416 24155971
Growth inhibition assay
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).

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. 

28397399 24155971
体内研究 Belinostat按10mg/kg剂量处理A2780和A2780/cp70 移植瘤,明显延迟肿瘤生长,但是对动物体重没有影响。[1] 在鼠膀胱细胞中,Belinostat也诱导p21WAF1, HDAC 核心和细胞通讯基因。[2] Belinostat按100mg/kg剂量单独处理A2780移植瘤,产生抗癌功效,肿瘤抑制率(TGI)达47% ,这种抑制存在剂量依赖性。100 mg/kg Belinostat和40 mg/kg Carboplatin联用可以延迟肿瘤生长,从18.6 天到22.5 天。 [3] Bortezomib和Belinostat联用,明显抑制肿瘤,此外,作用于携带抗Bortezomib UMSCC-11A移植瘤的鼠显示肠胃毒性 。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

组蛋白脱乙酰基酶活性实验:

汇合培养,用冷PBS中冲洗2遍,按200×g 转速离心5分钟。 细胞悬浮在2体积的溶解 buffer 中,60 mm Tris buffer (pH 为7.4)包含30%甘油和450 mm NaCl,用干冰冻结,然后30oC水浴溶解,循环3次。细胞碎片按1.2×104g转速离心5分钟, 然后上清液储存于−80oC中。使用 [3H]乙酰 CoA,通过p300的重组蛋白包括次黄嘌呤-氨基喋呤-胸腺嘧啶域乙酰化组蛋白H4肽段 (序列为SGRGKGGKGLGKGGAKRHRK)。100 μg H4 肽段与次黄嘌呤-氨基喋呤-胸腺嘧啶buffer(buffer包含50 mM Tris HCl pH为8.0, 5% 甘油, 50 mM KCl, 和0.1 mM EDTA),1 mM DTT, 1 mM 4-(2-氨乙基) ,苯磺酰基氟化物, 1×蛋白酶抑制剂, 50 μL纯化的p300, 及1.85 m [3H]乙酰 CoA (4.50Ci/mmol)混合,最终体积为300 μL,在30oC温育45分钟。p300蛋白 和 20 μL 50% Ni-琼脂糖在4oC下温育1小时,然后离心分离。上清液上样到2 mL Sephadex G15 柱中。加入1毫升蒸馏水,收集三滴样片,重复加入蒸馏水直到体积为4-5 mL,收集40滴样片。用2 mL 闪烁液稀释3微升样片,在闪烁计数板上计数,用于鉴定包含标记肽段的样片。合并样片,测定1 μL组合样本,用于测定每个肽段的放射性。在150 μL buffer,2 μL 细胞抽提物,和2 μL Belinostat的混合液中进行反应。加入2 μL [3H] 标记的底物开始反应。样本在 37oC下温育45分钟,加入HCl 和乙酸(终浓度分别为0.72和0.12 M)终止反应。释放的[3H]乙酸盐加到750 μL of 乙酸乙酯中, 按1.2×104g转速 离心5分钟。上层 (600 μL) 转移到3 mL闪烁液,然后计数。
细胞实验:[1]
- 合并
  • Cell lines: A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3,和HS852细胞
  • Concentrations: 0.016到10 μM
  • Incubation Time: 24小时
  • Method: 肿瘤细胞系(A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3,和HS852) 按8×104个细胞/25 cm2 瓶接种在5 mL 培养基中,温育48小时。用Belinostat (0.016 到 10 μm)处理细胞24小时。1 mL 胰蛋白酶/EDTA加到培养瓶中。细胞分离后,加入1 mL培养基,细胞再次悬浮。稀释细胞,按0.5-2×103个细胞/皿移到6cm Petri皿中。37oC下温育10到15天。用PBS冲洗细胞,溶于甲醇,用结晶紫染色,计数大于50个细胞的群落。通过IC50值计算敏感度。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 右侧腹皮下注射A2780, A2780/cp70和HCT116细胞的CD1 nu/nu鼠
  • Dosages: ≤40 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 64 mg/mL (201.03 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 318.35
化学式

C15H14N2O4S

CAS号 414864-00-9
储存条件 粉状
溶于溶剂
别名 NSC726630, PX-105684

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

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常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

    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