Entinostat (MS-275)

目录号:S1053 别名: SNDX-275 中文名称:恩替诺特

仅限科研使用

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。

Entinostat (MS-275) Chemical Structure

CAS: 209783-80-2

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 2234.07 现货
RMB 6301.79 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Entinostat (MS-275)发表文献361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 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 M1nme2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwME[xJO69VQ>? M2\kZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ALL-PO MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1njd2lEPTB;MD6wOlM2PSEQvF2= NHvwTmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
697 NFrNTJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnGwTWM2OD1yLkC5PVc3KM7:TR?= NUX3[5VJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NCI-H748 MoP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFizWFZKSzVyPUCuNVA{OzRizszN MlrKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NKM-1 M3n3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwMUC5NVIh|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
ES1 MlPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMUGyOVUh|ryP M3jrOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NCI-H1963 M{nEXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\3VXB3UUN3ME2wMlEyPTd7IN88US=> NHy3Spg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NCI-H1417 NXXUSpVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnmfVZKSzVyPUCuNVI6PzRizszN NFr4VXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NEC8 MljrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLETWM2OD1yLkGzOVI4KM7:TR?= NWi2VIY4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
CRO-AP2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3tb2dKSzVyPUCuNVY5QDlizszN NHnqXY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
A3-KAW NFPjTYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TTcGlEPTB;MD6xO|YzPyEQvF2= NUTyeIlZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
SF539 NF7rbGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjhVJZlUUN3ME2wMlE6PTl|IN88US=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NOS-1 MlnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjv[YZzUUN3ME2wMlE6PjF7IN88US=> NWC5OpFzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NTERA-S-cl-D1 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljjTWM2OD1yLkKwNVE{KM7:TR?= MmfFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
COR-L88 NEDIU2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq0b|VlUUN3ME2wMlIzQTV7IN88US=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
EM-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwMkSwO|kh|ryP MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
KARPAS-45 M4DGPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwMke4N|Mh|ryP NGe5cFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
DSH1 M{Tzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XvPGlEPTB;MD6yPFcxQCEQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
HT-144 MnPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjKTWM2OD1yLkOwNlU3KM7:TR?= MkT4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
ATN-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLPTWM2OD1yLkOwOVc3KM7:TR?= M4eyNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
HEL NXfDPZJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M322Z2lEPTB;MD6zNVM1QCEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NB12 NUDkZ|NMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwM{G3OVYh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
LU-139 NWXpWZY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXlVZBKSzVyPUCuN|M2OSEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
J-RT3-T3-5 MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDvNpVZUUN3ME2wMlM{PzF4IN88US=> NX22WZFsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
MOLT-13 M2rDc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj2ZWhlUUN3ME2wMlM{QDFizszN MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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CMK MkS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DMUGlEPTB;MD6zOVczPyEQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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LB647-SCLC NWPi[YVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwM{[3N{DPxE1? M3:wXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
TE-8 MmPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HIdGlEPTB;MD6zOlk{PSEQvF2= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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DEL M2\SZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFOwNYdKSzVyPUCuN|c1QDdizszN NIXsT449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
ARH-77 MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwM{ixPVMh|ryP M{jOe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NCCIT Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwM{i2OFkh|ryP MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
RPMI-8402 NXHJVWpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvmSo5KUUN3ME2wMlM5PzBzIN88US=> NIf0SlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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SK-MM-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTBwM{m4Olgh|ryP MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
CHP-126 NWDQOlVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;qdXZKSzVyPUCuOFAzOzFizszN NVT5TXg2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
A101D MojqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfibIlYUUN3ME2wMlQxOyEQvF2= M{LCO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
SCH NWDkbHNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\FS2lEPTB;MD60NFM1OiEQvF2= MnW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NMC-G1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwNECzOlch|ryP M3zM[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NCI-H209 NFfETJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfzfXJ4UUN3ME2wMlQxPjF|IN88US=> NIXQfnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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LP-1 NULWdXVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfQVZI3UUN3ME2xMlI6QTR5IN88US=> M172TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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JiyoyeP-2003 MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzSWYZtUUN3ME2xMlM2OzlizszN NX;4W5hCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NCI-H2107 M33D[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3CTnNKSzVyPUGuN|U5QDNizszN NYr3UmhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
BB30-HNC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTZeWhKSzVyPUGuN|g6PzhizszN NXPReGFwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
K-562 NV3mVnpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{H2emlEPTB;MT6zPVIyQSEQvF2= NEf1fYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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KARPAS-422 MnfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\aOG97UUN3ME2xMlQ2OzV6IN88US=> Mn7JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
LB996-RCC MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H6bGlEPTB;MT60O|ExOyEQvF2= M{TVdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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KG-1 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFwNkG5NFEh|ryP NW[xWZl{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NCI-H82 M2LjU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFwNkO0NFYh|ryP NI\jfWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
LB1047-RCC MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXydFJiUUN3ME2xMlY{PDV7IN88US=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
KM12 MmHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PMbmlEPTB;MT62OFch|ryP MnjuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
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HDLM-2 MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL4cmVqUUN3ME2xMlY5OjhzIN88US=> M1nTTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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DB NHn4[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S1W2lEPTB;MT63NFM2OyEQvF2= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
HD-MY-Z NIrFc5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL4UmhKSzVyPUGuO|UzOzRizszN MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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ETK-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwN{i4O|kh|ryP M1zpVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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ES7 NE\t[VNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjUVYJKSzVyPUGuPFA{ODJizszN NFPIW2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
SW872 Mm\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrGNpVKSzVyPUGuPFE{QTVizszN MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
TK10 NFzrNoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DCV2lEPTB;MT64N|ExQCEQvF2= MkTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
LB831-BLC M4L3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LxRWlEPTB;MT64N|U3OyEQvF2= NEHPN|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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MLMA NIfFd2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnIVWlMUUN3ME2xMlg5OjN2IN88US=> NED6SZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
D-542MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\odoNKSzVyPUGuPFk{PzNizszN NI\scI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
EW-16 MluyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\RfXh2UUN3ME2xMlkzPzJizszN NEXuT4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
LOXIMVI MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFwOUOyPEDPxE1? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
GB-1 MmC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUT2dFgyUUN3ME2xMlk{QDZ4IN88US=> MlHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
IST-SL2 NH3CR|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;tbHE3UUN3ME2yMlAxOjZ{IN88US=> M4Hrb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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MV4-11 M4LyUGFxd3C2b4Ppd{Bie3OjeR?= NIfwXmI2KHWP MWeyOEB1dyB2ODDodpM> NVHaWFlzUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNWlQuOTFiY3XscJMh[XRiNTD1UUBi\nSncjCyOEB1dyB2ODDodpMh[nliQX7u[ZhqdiCYLWDJJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6Ng>? M3fpOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{O4PVU{Lz5{OUezPFk2OzxxYU6=
MV4-11 M{\yfmZ2dmO2aX;uJIF{e2G7 NV7oeWNWOjByIH7N M4\2elI1KGi{cx?= M2nBSmlvcGmkaYTpc44hd2ZiY3zhd5MhOSCKRFHDJIlvKGi3bXHuJG1XPC1zMTDj[YxteyCjc4Pld5Nm\CCjczDofZBmemGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFMh[XRiMkCwJI5OKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNw M1jOR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{O4PVU{Lz5{OUezPFk2OzxxYU6=
HL60 MWfBdI9xfG:|aYOgZZN{[Xl? MkLQOUB2VQ>? NH3NdZA1QCCqcoO= NX7TdldyUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIIDyc4Nie3Cjc3WtN{Bt\X[nbDDheEA2KHWPIHHmeIVzKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOu MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzNUCwPUc,Ojh2MUWwNFk9N2F-
HL60 NFrscIhCeG:ydH;zbZMh[XO|YYm= M2LablUhfU1? NGP2b4E1QCCqcoO= NYr2OYZDUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiY3HzdIF{\S1|IHzleoVtKGG2IEWgeW0h[W[2ZYKgOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqey5? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzNUCwPUc,Ojh2MUWwNFk9N2F-
HL60 M{XQT2Fxd3C2b4Ppd{Bie3OjeR?= MYC1JJVO MlnrOFghcHK| MkDJTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQhWEGUUDDs[ZZmdCCjdDC1JJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNw MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzNUCwPUc,Ojh2MUWwNFk9N2F-
MV4-11 NVfuT49CS2WubDDjfYNt\SCjcoLld5Qh[XO|YYm= MXW1JJVO M{foU|I1KGi{cx?= NF;ZRZZE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IIP1Zk1IOSCyaHHz[UBifCB3IIXNJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[ub4egZ5l1d22ndILpZ{Bu\XSqb3Su M4HtOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUi5OFQyLz5{OUW4PVQ1OTxxYU6=
HEL MVXD[YxtKGO7Y3zlJIFzemW|dDDhd5NigQ>? MVq1JJVO MUWyOEBpenN? MoHIR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTGVNKGOnbHzzJIF1KDVidV2gZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\myxdzDjfZRwdWW2cnnjJI1mfGixZD6= NFThPIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW4PVQ1OSd-Mkm1PFk1PDF:L3G+
Jurkat NFnXVJlE\WyuIHP5Z4xmKGG{cnXzeEBie3OjeR?= NX3kVYhOPSC3TR?= M4POTFI1KGi{cx?= MXvD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDKeZJs[XRiY3XscJMh[XRiNTD1UUBi\nSncjCyOEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobH;3JIN6fG:vZYTybYMhdWW2aH;kMi=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-
MV4-11 Mn7WSpVv[3Srb36gZZN{[Xl? NITRRog2KHWP NIWzWnQzPCCqcoO= NH;XU4JKdmirYnn0bY9vKG:oIHPsZZN{KDFiSFTBR{BqdiCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5lfWO2aX;uJI9nKGirc4TvcoUhcHmyZYLhZ4V1gWyjdHnvckBifCB3IIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;kMi=> NVXWSY1GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1PFk1PDFpPkK5OVg6PDRzPD;hQi=>
LNCAP NWPEXINCTnWwY4Tpc44h[XO|YYm= NXnQeGFbOTBidV2= NHPVWWozPCCqcoO= MmDaTY5pcWKrdHnvckBw\iCKRFHDOkBqdiCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKESKVD3pcoR2[2WmIHHsdIhiNXS3YoXsbY4h\GWjY3X0fYxifGmxbjDifUBu\WG|dYLpcochcW6lcnXhd4UhcW5iYXzwbIEufHWkdXzpckBi[2W2eXzheIlwdiCjdDCxNEB2VSCvZXHzeZJm\CCjZoTldkAzPCCqcoOgdoVt[XSrdnWgeI8h[2:wdILvcE4> NFXTNZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{exO|U1PCd-Mke3NVc2PDR:L3G+
Assay
Methods Test Index PMID
Western blot TopoIIα / TopoIIβ DR4 / DR5 Caspase 8 Cleaved PARP AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3 21254166 19148581 24203492
Immunofluorescence H3K4Me3 / H3K9Me3 DR4 / DR5 phalloidin / snail 22468166 19148581 29855565
Growth inhibition assay Cell viability Cell proliferation 28969017 24203492
ELISA GCP-2 / MCP-2 / MIF 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]
  • 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]
  • 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。
动物实验:[1]
  • 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。

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 376.41
化学式

C21H20N4O3

CAS号 209783-80-2
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
NCT04708470 Recruiting Drug: Bintrafusp Alfa|Drug: NHS-IL12|Drug: Entinostat Cancer|Solid Tumor|Metastatic Checkpoint Refractory HPV Associated Malignancies|Microsatellite Stable Colon Cancer (MSS) National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 5 2021 Phase 1|Phase 2
NCT03829930 Terminated Drug: Entinostat|Drug: Enzalutamide Prostate Adenocarcinoma George Washington University May 1 2019 Phase 1
NCT03765229 Recruiting Drug: Entinostat|Drug: Pembrolizumab Melanoma UNC Lineberger Comprehensive Cancer Center|Syndax Pharmaceuticals Inc. March 22 2019 Phase 2
NCT03473639 Recruiting Drug: Entinostat|Drug: Capecitabine Metastatic Breast Cancer|Breast Cancer University of Virginia|Syndax Pharmaceuticals January 29 2019 Phase 1
NCT03361800 Terminated Drug: Entinostat Breast Cancer|Invasive Breast Cancer|ER-Negative PR-Negative HER2-Negative Breast Cancer UNC Lineberger Comprehensive Cancer Center|Syndax Pharmaceuticals|National Cancer Institute (NCI) November 28 2018 Early 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:
I would like to use Entinostat(Catalog No.S1053) for animal study. What is your recommendation for the solvent? What is the role of PEG 300 in this case? Can I use DMSO only and dilute it with PBS or HBSS?

回答:
2%DMSO/30%PEG/68%Water is recommended. PEG is an important polymer that helps with the solubility of hydrophobic drugs. If you use DMSO only and dilute it with PBS or HBSS, Entinostat will likely to precipitate out since it has very low solubility in water.

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