Entinostat (MS-275)

Catalog No.S1053 Synonyms: SNDX-275

For research use only.

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.

Entinostat (MS-275) Chemical Structure

CAS No. 209783-80-2

Selleck's Entinostat (MS-275) has been cited by 359 publications

Purity & Quality Control

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Biological Activity

Description Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Targets
HDAC1 [2]
(Cell-free assay)
HDAC3 [2]
(Cell-free assay)
0.51 μM 1.7 μM
In vitro

MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. MS-275 inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. [1] MS-275 is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. [2] MS-275 shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SCC-3 NVrqNXJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LSWGlEPTB;MD6wOlEh|ryP MlPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
ALL-PO NHfNWmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwME[zOVUh|ryP MnX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
697 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\le2lEPTB;MD6wPVk4PiEQvF2= NVvjdWhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NCI-H748 NWfWZ|RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjHWnFKSzVyPUCuNVA{OzRizszN M{PRWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NKM-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;U[mlEPTB;MD6xNFkyOiEQvF2= NXLWO3dqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
ES1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXhTWM2OD1yLkGxNlU2KM7:TR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NCI-H1963 NHiwbllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwMUG1O|kh|ryP MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NCI-H1417 Mof0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf5elBKSzVyPUCuNVI6PzRizszN M4L5PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NEC8 MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC1coRKSzVyPUCuNVM2OjdizszN MlLnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
CRO-AP2 NVXjeW15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETnfotKSzVyPUCuNVY5QDlizszN MoTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
A3-KAW NUXrWGhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nIXmlEPTB;MD6xO|YzPyEQvF2= NUjVUVF6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
SF539 M3L5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;0XXNKSzVyPUCuNVk2QTNizszN NVPvPZUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NOS-1 NIDaWoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fleWlEPTB;MD6xPVYyQSEQvF2= NUniZWt1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NTERA-S-cl-D1 Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnWTWM2OD1yLkKwNVE{KM7:TR?= M3vYb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
COR-L88 MnLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTKe3hKSzVyPUCuNlI6PTlizszN MoXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
EM-2 NHnYN49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwMkSwO|kh|ryP M3WxdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
KARPAS-45 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TMe2lEPTB;MD6yO|g{OyEQvF2= NY\nSplpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
DSH1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nuNWlEPTB;MD6yPFcxQCEQvF2= M2rYd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
HT-144 NYfCNVdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLLTWM2OD1yLkOwNlU3KM7:TR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
ATN-1 M1jYSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjXTWM2OD1yLkOwOVc3KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
HEL NWHWV2doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwM{GzOFgh|ryP NYrqXWRvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NB12 MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\vd45qUUN3ME2wMlMyPzV4IN88US=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
LU-139 NEH1Z2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzKVXFKSzVyPUCuN|M2OSEQvF2= MnXNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
J-RT3-T3-5 NG\J[5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwM{O3NVYh|ryP NFrLXmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
MOLT-13 NF25U|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fPRmlEPTB;MD6zN|gyKM7:TR?= MnL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
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LB647-SCLC M2DaXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPpN206UUN3ME2wMlM3PzNizszN Mn\lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
TE-8 MljJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vvfGlEPTB;MD6zOlk{PSEQvF2= NGH1Soo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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DEL NHXmbldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLSTWM2OD1yLkO3OFg4KM7:TR?= M1zPT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ARH-77 NVu1TG9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LUN2lEPTB;MD6zPFE6OyEQvF2= NHKwO3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NCCIT NGPxZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwM{i2OFkh|ryP Mo\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
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SK-MM-2 NWjLcnVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTBwM{m4Olgh|ryP MnHnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
CHP-126 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwNECyN|Eh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
A101D NEHGSZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwNECzJO69VQ>? NFjhWIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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MOLT-16 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS4NGFjUUN3ME2wMlQyODF5IN88US=> NIT4T3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
RPMI-6666 MlL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwNEGxNkDPxE1? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
OPM-2 M4jrTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\zdm5QUUN3ME2wMlQyPTF|IN88US=> NG\zSnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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HepG2 NH3p[WNHfW6ldHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGhmeEd{IHPlcIx{NCCLQ{WwJF0hOC5yMEC5JO69VS5? NEjzNWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEK0O|U2PCd-MUiyOFc2PTR:L3G+
HCT116 NHyxS3ZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUm0PEBpenN? M2T2fWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlEh|ryPLh?= NUHySJZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3NFUxOjJpPkKyO|A2ODJ{PD;hQi=>
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HEK293 M1K2U2Z2dmO2aX;uJIF{e2G7 NV\CboxIUW6qaXLpeIlwdiCxZjDoeY1idiCFLYTldo1qdmGuIF\MRWcufGGpZ3XkJGhFSUN{IHnuJGhGUzJ7MzDj[YxteyxiSVO1NEA:KDBwMkWg{txONg>? NHHYfGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUS0NVg1Pid-MUm0OFE5PDZ:L3G+
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HEK293 MnnCSpVv[3Srb36gZZN{[Xl? M{fOOGlvcGmkaYTpc44hd2ZiSFTBR|MhcW5iSFXLNlk{KGOnbHzzMEBKSzVyIE2gNE41KM7:TT6= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDNyOEW2N{c,OTh|MEi1OlM9N2F-
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Assay
Methods Test Index PMID
Western blot AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3 ; Cleaved PARP ; Caspase 8 ; DR4 / DR5 ; TopoIIα / TopoIIβ 24203492 19148581 21254166
Immunofluorescence phalloidin / snail ; DR4 / DR5 ; H3K4Me3 / H3K9Me3 29855565 19148581 22468166
Growth inhibition assay Cell proliferation ; Cell viability 24203492 28969017
ELISA GCP-2 / MCP-2 / MIF 24241152
In vivo MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. [1] MS-275 demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. [4] MS-275, combination with IL-2, has great antitumor activity to renal cell carcinoma xenograft model, which due to decreased T regulatory cells and increased splenocytes. [5]

Protocol (from reference)

Kinase Assay:

[6]

  • Standard HDAC Assays:

    Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. Km and Vmax values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme.

Cell Research:

[2]

  • Cell lines: A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells
  • Concentrations: ~ 10 μM
  • Incubation Time: 3 days
  • Method:

    Cancer cells (5 × 103) are seeded into each well of 96-well plates and cultured with graded concentrations of MS-275 for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na2HPO4 is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration.

Animal Research:

[1]

  • Animal Models: A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice.
  • Dosages: 12.3, 24.5 and 49 mg/kg
  • Administration: Administered orally once daily 5 days per week for 4 weeks

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 376.41
Formula

C21H20N4O3

CAS No. 209783-80-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3

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
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 2022-01-17)

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:
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?

Answer:
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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