Belinostat (PXD101)

目录号:S1085 别名: PXD101,NSC726630, PX-105684 中文名称:贝利司他

仅限科研使用

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。

Belinostat (PXD101) Chemical Structure

CAS: 414864-00-9

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 7950.07 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Belinostat (PXD101)发表文献88篇:

产品安全说明书

HDAC抑制剂选择性比较

相关HDAC产品

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 NWnmNY11TnWwY4Tpc44hSXO|YYm= NG\VW5MxNjoEoN88UeKh NFPsN4ozPCCq NHfuOldld3ewLYLl[5Vt[XS|IGTTJJBzd3SnaX6gcIV3\Wy|IHHmeIVzKDcEoHigbY5kfWKjdHnvci=> M1zibVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MUK0OVk1Lz5zN{GyOFU6PDxxYU6=
HCT116 MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2K4WlQ5KGh? M4\0[WVEPTB;MD6yPEDPxE1? NGnNfGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyOFU6PCd-MUexNlQ2QTR:L3G+
Granta-519 NI\yZXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVqyOEBp MW\JR|UxRTV4LkOg{txO MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODB4OEC4NEc,OjByNkiwPFA9N2F-
Jeko-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUeyOEBp MoXTTWM2OD1yLkKg{txO MmjmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNkiwPFAoRjJyME[4NFgxRC:jPh?=
HBL-2 NWLGWnkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfjNlQhcA>? M{jYO2lEPTB;MD60JO69VQ>? Mk[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNkiwPFAoRjJyME[4NFgxRC:jPh?=
Panc-1  MoTXRZBweHSxc3nzJGF{e2G7 NX3IbYh7OTByL{WwNE8yODByIH7N MX20PEBp Mm\KbY5lfWOnczDkc5NmKGSncHXu[IVvfCCjcH;weI9{cXN? NFTXNGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[4NVY6QCd-MkK2PFE3QTh:L3G+
AsPC-1 NFnjbFBCeG:ydH;zbZMhSXO|YYm= NUSwVpVFOTByL{WwNE8yODByIH7N NUXDW5N4PDhiaB?= Mn;XbY5lfWOnczDkc5NmKGSncHXu[IVvfCCjcH;weI9{cXN? NXLvNIZvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
T3M4 NVS1bmE5SXCxcITvd4l{KEG|c3H5 NV7wcnJwOTByL{WwNE8yODByIH7N NEnWT3o1QCCq M{\4dIlv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| MoP2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
Panc-1  NX;Dd2dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HVdFAuQDByIH7N NXTtTZR1PDhiaB?= MWDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= Ml\2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
AsPC-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rwOVAuQDByIH7N NFXjXYo1QCCq MWLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NWHBT2NqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
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MiaPaCa2 MmSwSpVv[3Srb36gRZN{[Xl? Moe0NU8yOCEQvF2= MU[yOEBp Ml3hbY5lfWOnczCg[5Jwf3SqIHHydoV{fGWmIHnuJGczN01? MlT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ|NEe1Olk2RC:jPh?=
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Panc1005 MV\BdI9xfG:|aYOgRZN{[Xl? NHHDZ2oyKM7:TR?= MV:yOEBp NHzHVXJqdmS3Y3XzJIFxd3C2b4Ppdy=> NXvrU3NNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc0327 NVzTXm1vSXCxcITvd4l{KEG|c3H5 MU[xJO69VQ>? NHnFO3EzPCCq NFrkV4VqdmS3Y3XzJIFxd3C2b4Ppdy=> NVO1[nFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc0203 M2LSS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvxOFghcA>? MYnFR|UxRTJ{LkKg{txO MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
PL45 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmOzOFghcA>? Ml;JSWM2OD1{MD64JO69VQ>? NEDH[ok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
Panc1005 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[xXoEzPDhiaB?= M4\rXmVEPTB;MT6xJO69VQ>? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc0403 NHjpUnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLXOFghcA>? NGfMZ2dGSzVyPUGuNUDPxE1? NFrqOYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O|U3QTV:L3G+
BxPc3 M3rsPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[0PEBp NFXw[nVGSzVyPUGuNEDPxE1? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
MiaPaCa2 M4TYVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnxOFghcA>? NYLIT5J7TUN3ME2wMlch|ryP NULJXYVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc0327 M{PKSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:wR3NkPDhiaB?= M1frb2VEPTB;MD61JO69VQ>? M33QWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
AsPc1 M3HnN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWG0PEBp MVXFR|UxRTBwMzFOwG0> NUfqNmI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O|U3QTVpPkKzOFc2Pjl3PD;hQi=>
PC9 M1jvXGZ2dmO2aX;uJGF{e2G7 NI[2N4YxNjVxMT:yJO69VQ>? M{HwZlQhcA>? NYn5UoZSTE2VTx?= M4DyOYlvcGmkaYTzJJRp\SCuZY\lcJMhd2ZiQXv0JEhxNUGtdDmgZY5lKEWJRmK= NVK0enlXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
H1650 MUjGeY5kfGmxbjDBd5NigQ>? NI\l[4YxNjVxMT:yJO69VQ>? NUTs[45nPCCq NGXq[Y9FVVOR MnjmbY5pcWKrdIOgeIhmKGyndnXsd{Bw\iCDa4SgLJAuSWu2KTDhcoQhTUeIUh?= NGXpdJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H460 MWPGeY5kfGmxbjDBd5NigQ>? M1;UelAvPS9zL{Kg{txO M1S0UVQhcA>? NWrifXZ{TE2VTx?= M4fsR4lvcGmkaYTzJJRp\SCuZY\lcJMhd2ZiQXv0JEhxNUGtdDmgZY5lKEWJRmK= NYDEbWpIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NVU4PTJpPkKzOVE2PzV{PD;hQi=>
PC9 MXXGeY5kfGmxbjDBd5NigQ>? NULqSGJ4PTBywrDuUS=> MYWyOOKhcA>? MXLEUXNQ MmC3[IVkemWjc3XzJGVITlJiZYjwdoV{e2mxbh?= MoH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
H1650 NGfrenRHfW6ldHnvckBCe3OjeR?= MUK1NFDDqG6P NV\mOoFXOjUEoHi= NI\mU2RFVVOR NXnXXpQ5\GWlcnXhd4V{KEWJRmKg[ZhxemW|c3nvci=> NInKTWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
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HCC4006 Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HRS|czyqCq NGHxfY9FVVOR M1\O[WlEPTB;MD60OkDPxE1? MoruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ|NUG1O|UzRC:jPh?=
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HL60 Ml3FRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4TmSFQ5KGi{cx?= NUnP[5lvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTBiPTCxMlA6KM7:TT6= M{[4WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{S0OFg4Lz5{N{O0OFQ5PzxxYU6=
K562 NHjKTo9CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M13xWVQ5KGi{cx?= M1XtbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT6xJO69VS5? M{LoVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUOzPFc{Lz5{OUWzN|g4OzxxYU6=
PC3 NYHDPYZ7SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M{XN[|Q5KGi{cx?= NUezOHpkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuN{DPxE1w M2PUPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUOzPFc{Lz5{OUWzN|g4OzxxYU6=
NFF MYnDfZRwfG:6aXPpeJkh[XO|YYm= NF3yZVM4OiCqcoO= MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOSmYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IEGuOEDPxE1w NYXOZWhQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyOFEyOTJpPkK4NlQyOTF{PD;hQi=>
HEK293 MULDfZRwfG:6aXPpeJkh[XO|YYm= MXS0PEBpenN? MoXyR5l1d3SxeHnjbZR6KGGpYXnud5QhUEWNMkmzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSC{ZYPhfpVzcW5iYYPzZZktKEmFNUCgQUAyNjRizszNMi=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ2MUGxNkc,Ojh{NEGxNVI9N2F-
NFF Mo\3R5l1d3SxeHnjbZR6KGG|c3H5 Mlv4O|IhcHK| Ml3LR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmZHKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOS52MjFOwG0v MlX6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NEW0NFIoRjNyMkS1OFAzRC:jPh?=
HEK293 MWLDfZRwfG:6aXPpeJkh[XO|YYm= NX;Gd5g{PDhiaILz MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHKnc3H6eZJqdiCmeXWgZoF{\WRiYYPzZZktKEmFNUCgQUAyNjR{IN88UU4> M4Lm[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkS1OFAzLz5|MEK0OVQxOjxxYU6=
RAW264.7 MlLtRY51cS2rbn\sZY1u[XSxcomgZZN{[Xl? NYPkT2ZKOSCqch?= NEXvPWpCdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCwaYTybYMhd3irZHWgdJJw\HWldHnvckBxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCOUGOgd5RqdXWuYYTpc44h\m:{IEK0JIhzeyCkeTDHdolme3NicnXh[4VvfCCkYYPl[EBie3OjeTygTWM2OCB;IEKuNkDPxE1w MmDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUO4O|UoRjJ3MUGzPFc2RC:jPh?=
RAW264.7 MVTBcpRqNWmwZnzhcY1ifG:{eTDhd5NigQ>? M4W1e|EhcHJ? NEnOOG9CdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh[mWob4LlJGxRWyC|dHnteYxifGmxbjDmc5IhOjRiaILzJIJ6KEWOSWPBJI1mfGixZDygTWM2OCB;IESuO{DPxE1w NV7Y[XV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNVM5PzVpPkK1NVE{QDd3PD;hQi=>
RAW264.7 MUTBcpRqNWmwZnzhcY1ifG:{eTDhd5NigQ>? MVuxJIhz NEHkVndCdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCSR1WyJJBzd2S3Y4Tpc44heHKnLXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViTGDTJJN1cW23bHH0bY9vKG[xcjCyOEBpenNiYomg[Y57gW2nIHntcZVvd2G|c3H5JI1mfGixZDygTWM2OCB;IEiuNlgh|ryPLh?= NYjIboZlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNVM5PzVpPkK1NVE{QDd3PD;hQi=>
Huh-luc/neo7 NVTOXZJITnWwY4Tpc44h[XO|YYm= MYWxJJVO MVqxJJRwKDNiaILz NEDEeGlKdmirYnn0bY9vKG:oIFjERWMh[2yjc4OgNUBqdiCqdX3hckBJfWhvbIXjM45mdzdiY3XscJMh[XO|ZYPz[YQh[XNiaHnzeI9v\SCKMzDhZ4V1gWyjdHnvckBifCBzIIXNJIFnfGW{IEGgeI8hOyCqcoOgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> MkjsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{ewNVcoRjJ3OUO3NFE4RC:jPh?=
PC3 MVLGeY5kfGmxbjDhd5NigQ>? NVrwfWVNOC5|IIXN M3XVU|Q5KGi{cx?= MlzMTY5pcWKrdHnvckBw\iCKRFHDJIlvKGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDhcY92dnRib3[gZYNmfHmuYYTl[EBpcXO2b37lJGg{KGG2IECuN{B2VSCjZoTldkA1QCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| M1zuW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{S0OFg4Lz5{N{O0OFQ5PzxxYU6=
HCT116 MmnuSpVv[3Srb36gZZN{[Xl? M172VlAvOyC3TR?= MX[0PEBpenN? M1;CW2lvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[W2xdX70JI9nKGGlZYT5cIF1\WRiaHnzeI9v\SCKMzDheEAxNjNidV2gZYZ1\XJiNEigbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> M1;MVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{S0OFg4Lz5{N{O0OFQ5PzxxYU6=
Assay
Methods Test Index PMID
Western blot p-H2AX(Ser139) / KU70 / KU80 / RAD51 / RAD52 / ERCC1 Acetyl Histone H3 / Acetyl Histone H4 / Acetyl tubulin p21 / p27 SOS1 / SOS2 PARP / p-ERK / p-p38 / p38 / p-BRAF / p-MEK / MEK 24155971 23982416 28397399
Growth inhibition assay Cell viability IC50 24155971 28397399
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]
  • 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]
  • 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。
动物实验:[1]
  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

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)

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操作手册

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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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