Entinostat (MS-275)

For research use only. Not for use in humans.

目录号:S1053 别名: SNDX-275 中文名称:恩替诺特

Entinostat (MS-275) Chemical Structure

CAS No. 209783-80-2

Entinostat (MS-275, SNDX-275)强烈抑制HDAC1HDAC3,无细胞试验中IC50分别为0.51 μM和1.7 μM,抑制作用强于HDACs 4, 6, 8,和10。Entinostat可诱导自噬和凋亡。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 746.45 现货
RMB 794.43 现货
RMB 1233.32 现货
RMB 2234.07 现货
RMB 6301.79 现货
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客户使用Selleck生产的Entinostat (MS-275)发表文献312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 Entinostat (MS-275, SNDX-275)强烈抑制HDAC1HDAC3,无细胞试验中IC50分别为0.51 μM和1.7 μM,抑制作用强于HDACs 4, 6, 8,和10。Entinostat可诱导自噬和凋亡。Phase 3。
靶点
HDAC1 [2]
(Cell-free assay)
HDAC3 [2]
(Cell-free assay)
0.51 μM 1.7 μM
体外研究

MS-275通过作用于2′-氨基而抑制HDACs。MS-275作用于 K562细胞,诱导 p21WAF1/CIP1和凝溶胶蛋白的累积。MS-275作用于A2780细胞,可以降低S期细胞,提高G1期细胞。 MS-275通过抑制HAD而抑制人类肿瘤细胞系,包括 A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St和 HCT-15细胞增殖, IC50 为41.5 nM到4.71 μM。[1]MS-275抑制HDACs,作用于HDAC1和 HDAC3时IC50 分别为0.51 μM和1.7 μM。而对其他的HDACs没有抑制效果,如HDAC4, 6, 8和10。[2]MS-275有效抑制人类白血病和淋巴癌细胞,包括U937, HL-60, K562, 和Jurkat。MS-275可以诱导U937细胞p21CIP1/WAF1 调节的生长和变异Marker (CD11b)的表达。MS-275降低cyclin D1和抗凋亡蛋白Mcl-1与XIAP的表达。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SCC-3 Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV65XWFIUUN3ME2wMlA3OSEQvF2= M{j3OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ALL-PO M1HwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe3UWxKSzVyPUCuNFY{PTVizszN NIny[HM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
697 M1X1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\QToVKSzVyPUCuNFk6PzZizszN NEDSeG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NCI-H748 MlPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{WwdWlEPTB;MD6xNFM{PCEQvF2= M2T1R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NKM-1 MnrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwMUC5NVIh|ryP NHXtUoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
ES1 M3TqXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXGcm9uUUN3ME2wMlEyOjV3IN88US=> M1LXV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NCI-H1963 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLCTWM2OD1yLkGxOVc6KM7:TR?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NCI-H1417 M{[zWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHqwbmlKSzVyPUCuNVI6PzRizszN NIG0N249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NEC8 M1fubWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX5TWM2OD1yLkGzOVI4KM7:TR?= M{n4TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
CRO-AP2 NV[wTGVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjBTWM2OD1yLkG2PFg6KM7:TR?= NF;TdZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
A3-KAW MlrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrPeWpKSzVyPUCuNVc3OjdizszN MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
SF539 M4fafGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLhSlBnUUN3ME2wMlE6PTl|IN88US=> MkTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NOS-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\LNFhKSzVyPUCuNVk3OTlizszN NXXwPJlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NTERA-S-cl-D1 M{L0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXWTWM2OD1yLkKwNVE{KM7:TR?= NHnVW3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
COR-L88 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMkK5OVkh|ryP NGf2dJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
EM-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XHOWlEPTB;MD6yOFA4QSEQvF2= Ml73QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
KARPAS-45 NEPieY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vqVGlEPTB;MD6yO|g{OyEQvF2= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
DSH1 M{XsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\a[3VvUUN3ME2wMlI5PzB6IN88US=> M{nG[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
HT-144 NHOw[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrIUJNKSzVyPUCuN|AzPTZizszN M3:5NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ATN-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUT5XYlmUUN3ME2wMlMxPTd4IN88US=> Mn3YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
HEL MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDLeFI2UUN3ME2wMlMyOzR6IN88US=> M2XIdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NB12 NUnrZohNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjtTWM2OD1yLkOxO|U3KM7:TR?= NU[yOlRNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
LU-139 NWXlV|FmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHvN5hKSzVyPUCuN|M2OSEQvF2= NXHifnkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
J-RT3-T3-5 M3v5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:3Z2lEPTB;MD6zN|cyPiEQvF2= M1z4UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
MOLT-13 MkDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwM{O4NUDPxE1? NUGyfYFxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
SR NVPTXJB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX0PHpKSzVyPUCuN|QzPjFizszN MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
CMK NF21V2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;jVGlEPTB;MD6zOVczPyEQvF2= NHPCdpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
ES8 NWLZU5p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHETWM2OD1yLkO2NFIzKM7:TR?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
LB647-SCLC NIHmRZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq4coxKSzVyPUCuN|Y4OyEQvF2= M1nhWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
TE-8 M{f2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzuTWM2OD1yLkO2PVM2KM7:TR?= M{DXT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
BV-173 NH23eYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHXS2hKSzVyPUCuN|cyOjFizszN M2fLb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
DEL MlXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrKVWJKSzVyPUCuN|c1QDdizszN M1LwdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ARH-77 NVn1fXFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4L1bmlEPTB;MD6zPFE6OyEQvF2= NUP1R2hnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NCCIT NYL1R3BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILoSGhKSzVyPUCuN|g3PDlizszN NGTIXno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
RPMI-8402 M{XyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1WwT2lEPTB;MD6zPFcxOSEQvF2= M3HWPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
MONO-MAC-6 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwM{i3O|Yh|ryP NHLuPIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
SK-MM-2 M3vYWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPGOpFtUUN3ME2wMlM6QDZ6IN88US=> NXPGelBwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
CHP-126 M33Lemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkf2TWM2OD1yLkSwNlMyKM7:TR?= M1vtWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
A101D M1P2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjxTWM2OD1yLkSwN{DPxE1? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
SCH MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M133XmlEPTB;MD60NFM1OiEQvF2= M1zoU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NMC-G1 MkLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PURWlEPTB;MD60NFM3PyEQvF2= M4nkblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NCI-H209 Mo\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnnVHVKSzVyPUCuOFA3OTNizszN MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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HL60 M3Twc2Fxd3C2b4Ppd{Bie3OjeR?= NWKzeY5CPSC3TR?= NVz0dHNKPDhiaILz MofNTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKHC{b3Phd5Bie2VvMzDs[ZZmdCCjdDC1JJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNw M2S3XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEG1NFA6Lz5{OESxOVAxQTxxYU6=
HL60 MWHBdI9xfG:|aYOgZZN{[Xl? MmHNOUB2VQ>? NFLYdWo1QCCqcoO= NFPiPYFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iY3zlZZZm\CClYYPwZZNmNTNibHX2[Ywh[XRiNTD1UUBi\nSncjC0PEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{Ng>? MoLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MUWwNFkoRjJ6NEG1NFA6RC:jPh?=
HL60 MnH4RZBweHSxc3nzJIF{e2G7 NV3RO5BCPSC3TR?= NIntcJA1QCCqcoO= M4LPbmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiClbHXheoVlKFCDUmCgcIV3\WxiYYSgOUB2VSCjZoTldkA1QCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|Lh?= MkXuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MUWwNFkoRjJ6NEG1NFA6RC:jPh?=
MV4-11 M3;WOmNmdGxiY4njcIUh[XK{ZYP0JIF{e2G7 M2HWfVUhfU1? MnPBNlQhcHK| NGG3XGtE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IIP1Zk1IOSCyaHHz[UBifCB3IIXNJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[ub4egZ5l1d22ndILpZ{Bu\XSqb3Su NFHaNYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW4PVQ1OSd-Mkm1PFk1PDF:L3G+
HEL NULpOnVpS2WubDDjfYNt\SCjcoLld5Qh[XO|YYm= Mmi3OUB2VQ>? NH7OeYYzPCCqcoO= Mn:zR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTGVNKGOnbHzzJIF1KDVidV2gZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\myxdzDjfZRwdWW2cnnjJI1mfGixZD6= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-
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MV4-11 MlfuSpVv[3Srb36gZZN{[Xl? NU[4VpYxPSC3TR?= NHPLVIczPCCqcoO= Mn\OTY5pcWKrdHnvckBw\iClbHHzd{AyKEiGQVOgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IHnu[JVkfGmxbjDv[kBpcXO2b37lJIh6eGW{YXPleJlt[XSrb36gZZQhPSC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZD6= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-
LNCAP NHnybFVHfW6ldHnvckBie3OjeR?= MnjXNVAhfU1? MoP3NlQhcHK| MUXJcohq[mm2aX;uJI9nKEiGQVO2JIlvKGi3bXHuJGxPS0GSIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTEiWLXnu[JVk\WRiYXzwbIEufHWkdXzpckBl\WGlZYT5cIF1cW:wIHL5JI1m[XO3cnnu[{BqdmO{ZXHz[UBqdiCjbIDoZU11fWK3bHnuJIFk\XS7bHH0bY9vKGG2IEGwJJVOKG2nYYP1doVlKGGodHXyJFI1KGi{czDy[YxifGm4ZTD0c{Bkd262cn;sMi=> MlfDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd5MUe1OFQoRjJ5N{G3OVQ1RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3; 

PubMed: 24203492     


HCT-15 or fresh primary NK cells were treated with entinostat for 24 h, and AcH3, AcH4, and HDAC1, 2, and 3 were detected by Western blotting. 

Cleaved PARP; 

PubMed: 19148581     


Induction of PARP cleavage in Daoy cells upon exposure to MS-275 was demonstrated by Western blot analyses using antibodies that recognize the cleaved 89 kDa PARP protein. Pan-Actin (45 kDa) was used as a loading control.

Caspase 8 ; 

PubMed: 19148581     


Cleavage of pro-Caspase-8 was demonstrated by Western blotting with extracts prepared from Daoy cells treated with 2.5 µM MS-275 for various time periods. Antibodies specific to human Caspase-8 or the loading control, pan-Actin were used to probe protein expression.

DR4 / DR5; 

PubMed: 19148581     


Western blotting to detect DR4 and DR5 expression upon treatment of Daoy cells with 2.5 µM MS-275 for 4, 8 and 24 h.

TopoIIα / TopoIIβ; 

PubMed: 21254166     


Upper panel, concentration-dependent effects of AR42, MS-275 and vorinostat on the expression of topoIIα versus topoIIβ after 48 h. Lower panel, time-dependent effect of 0.5 μM AR42 and 5 μM MS-275 on topoIIα versus topoIIβ expression in PLC-5 cells.

24203492 19148581 21254166
Immunofluorescence
phalloidin / snail; 

PubMed: 29855565     


(C) Effect of MS-275 treatment on Snail expression and localization. MCs (mesothelial cells) were treated with MS-275 (250 nM), or DMSO for 48 hr and then stimulated with TGFβ1 (2 ng/ml) for 24 h before processing for immunofluorescence with a monoclonal antibody against Snail. Cell nuclei are shown in blue (Hoechst 33342). Confocal images are shown from one representative experiment of three performed.

DR4 / DR5; 

PubMed: 19148581     


Flow Cytometry to measure cell surface expression of FAS, DR4 and DR5 using PE-labeled antibodies. Cells stained with isotype matched anti-human IgG antibodies served as controls.

H3K4Me3 / H3K9Me3; 

PubMed: 22468166     


Immunocytochemical analysis of the effects of AR42, SAHA, and MS-275 at the indicated concentrations on H3K4Me3 (upper panels) and H3K9Me3 (lower panels) after 24 h of treatment in LNCaP cells.

29855565 19148581 22468166
Growth inhibition assay
Cell proliferation; 

PubMed: 24203492     


(A) HCT-15 cells were cultured in indicated concentrations of entinostat for up to 72 h, and proliferation determined by MTT assay as indicated. (B) HCT-15, CCH-OS-D, COL and HOS cells were cultured in indicated concentrations of entinostat for 72 h, and viable cell number was determined using the Vi-cell assay and proliferation index calculated. (C) Freshly-isolated human NK cells were cultured in indicated concentrations of entinostat for up to 72 h, and viability was assessed by flow cytometry for 7-AAD uptake. *, P < 0.05, **; P ≤ 0.01; ***, P ≤ 0.001

Cell viability; 

PubMed: 28969017     


PANC-1, MIA PaCa-2, BxPC3, CFPAC-1, SUIT2 and SUIT2 Clone 1 cells were plated at a density of 3-5×103 per well in 96-well microtiter plates, allowed to adhere overnight and incubated for 72 hours in the presence of variable concentrations of entinostat (0-100μM). Cell viability was determined by XTT assays. The data presented are the mean values from triplicate wells from two independent experiments ±SE.

24203492 28969017
ELISA
GCP-2 / MCP-2 / MIF ; 

PubMed: 24241152     


MS-275 and SAHA suppressed the secretion of GCP-2, MCP-2 and MIF in E11 cells. (A) GCP suppression. (B) MCP-2 suppression. (C) MIF suppression. E11 cells were incubated with HDAC inhibitors at various concentrations for 1 h before they were stimulated by LPS. 24 h later, the secretion of GCP-2, MCP-2 and MIF were quantified by ELISA (n = 8). Bars show the mean and SD in (A–C).

24241152
体内研究 MS-275按49 mg/kg剂量作用于除了HCT-15的人类移植瘤都显示出强抗癌活性。[1]MS-275促进恶性实体瘤和恶性血液病的治疗可能性,及生理和畸变基因表达的调节。[4]MS-275和IL-2联用,作用于肾细胞癌显示出强抗癌活性,因为降低调节性T细胞和增强脾细胞的表达。[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:[6]
- 合并

标准HDAC实验:

用HDAC buffer按1:6稀释鼠肝内的酶。重组人类HDACs按1:4稀释在HDAC buffer中。用于标准HDAC实验,60 μl HDAC buffer和10 μl 稀释的酶溶液在30oC混合。在HDAC buffer中加入30 μl基底液开始HDAC反应,随后在30oC下温育30分钟。加入100 μl胰蛋白酶溶液终止反应,胰蛋白酶溶液由溶于50 mM Tris-HCl(pH 为8.0)的10 mg/ml 胰蛋白酶, 100 mM NaCl,及 2 μM TSA组成。30oC下温育20分钟, 通过测定460纳米(λex = 390 nm)处的荧光监测AMC的释放。使用释放的AMC校准荧光强度 。用于标准时间过程实验,在初始100 μl HDAC 反应中加入20 pmol 基底物。2-50 pmol 基底物的酶法分析产物获得荧光AMC,通过测量这种荧光AMC来测定 Km值和 Vmax值。使用Hanes 图分析实验数据。记录的AMC信号是针对没有酶而有buffer和基底物的空白区。
细胞实验:[2]
- 合并
  • Cell lines: A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St和HCT-15细胞
  • Concentrations: 10 μM 左右
  • Incubation Time: 3天
  • Method: 5×103个肿瘤细胞接种到96孔板上,加入梯度浓度MS-275培养三天。细胞用0.1 mg/mL中性红在CO2反应器中染色1小时,测定中性红与50 μL乙醇和150 μL 0.1 M Na2HPO4溶解后的OD540,测定IC50值。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 侧腹皮下注射A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1和Calu-3细胞的裸鼠
  • Dosages: 12.3, 24.5和49 mg/kg
  • Administration: 每天口服处理一次,每周进行5天,持续4周。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 75 mg/mL (199.25 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 376.41
化学式

C21H20N4O3

CAS号 209783-80-2
储存条件 粉状
溶于溶剂
别名 SNDX-275

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