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 361 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 M2\MNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwME[xJO69VQ>? M1KwWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ALL-PO NH3KNY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rZXWlEPTB;MD6wOlM2PSEQvF2= NETMPFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
697 M1q0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjXTWM2OD1yLkC5PVc3KM7:TR?= MmnSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NCI-H748 MlW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYC3e2dVUUN3ME2wMlExOzN2IN88US=> M1Tq[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NKM-1 M4DRUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nSRWlEPTB;MD6xNFkyOiEQvF2= MmPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
ES1 NHjIWI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\M[WlEPTB;MD6xNVI2PSEQvF2= NYfi[ocyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NCI-H1963 MlrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGL5OWNKSzVyPUCuNVE2PzlizszN MmD2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NCI-H1417 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX5TWM2OD1yLkGyPVc1KM7:TR?= M4X6XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NEC8 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkSwTWM2OD1yLkGzOVI4KM7:TR?= M3i3b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
CRO-AP2 NXXkbJZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjTZXdmUUN3ME2wMlE3QDh7IN88US=> NIS5S289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
A3-KAW M1G3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnNTWM2OD1yLkG3OlI4KM7:TR?= NUPYTFNuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
SF539 NUfHPJJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIj0c4lKSzVyPUCuNVk2QTNizszN NWm0SpJGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NOS-1 Mn7uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nZ[mlEPTB;MD6xPVYyQSEQvF2= NVXSTFl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NTERA-S-cl-D1 Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETkVJhKSzVyPUCuNlAyOTNizszN MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
COR-L88 M2\RV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUT0fZk4UUN3ME2wMlIzQTV7IN88US=> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
EM-2 Mn;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\mbmlEPTB;MD6yOFA4QSEQvF2= M1PVWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
KARPAS-45 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nvOWlEPTB;MD6yO|g{OyEQvF2= MoHoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
DSH1 MlfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwMki3NFgh|ryP MlLUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
HT-144 MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwM{CyOVYh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
ATN-1 MnzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELaTpVKSzVyPUCuN|A2PzZizszN NEO4VGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
HEL NIDjXYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITRU2RKSzVyPUCuN|E{PDhizszN M4DFOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NB12 NXPqOop7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\nTYZKSzVyPUCuN|E4PTZizszN M1jhZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
LU-139 NYTsUlJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HQdGlEPTB;MD6zN|UyKM7:TR?= Mnr6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
J-RT3-T3-5 NUm3dXlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;GTWM2OD1yLkOzO|E3KM7:TR?= MkDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
MOLT-13 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnNOHQyUUN3ME2wMlM{QDFizszN NXn6UWRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
SR NWPSeY5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XMRmlEPTB;MD6zOFI3OSEQvF2= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
CMK MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwM{W3Nlch|ryP M17YOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ES8 NXv4[2wzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwM{[wNlIh|ryP M2rzc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
LB647-SCLC NYPxTpU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLiTWM2OD1yLkO2O|Mh|ryP Mm\5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
TE-8 MojCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvTe2s{UUN3ME2wMlM3QTN3IN88US=> MlLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
BV-173 MonaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX2xfI5sUUN3ME2wMlM4OTJzIN88US=> NXnXTld[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
DEL MnTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHIcWNqUUN3ME2wMlM4PDh5IN88US=> NGLaSGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
ARH-77 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zXUmlEPTB;MD6zPFE6OyEQvF2= MlHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NCCIT M2rGeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwM{i2OFkh|ryP MlrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
RPMI-8402 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknyTWM2OD1yLkO4O|AyKM7:TR?= NYjWUYtTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
MONO-MAC-6 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Tsd2lEPTB;MD6zPFc4PiEQvF2= NEjKTHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
SK-MM-2 NFP1R5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljVTWM2OD1yLkO5PFY5KM7:TR?= M4rGOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
CHP-126 Mle4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHtbIxKSzVyPUCuOFAzOzFizszN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
A101D Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M163d2lEPTB;MD60NFMh|ryP NIqySoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
SCH MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUmydVhDUUN3ME2wMlQxOzR{IN88US=> M4T4SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NMC-G1 NXTaV3hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjydHJKSzVyPUCuOFA{PjdizszN Mn3iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NCI-H209 NWfIUWh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vH[2lEPTB;MD60NFYyOyEQvF2= NG\6eoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
MOLT-16 M2rJWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwNEGwNVch|ryP NGHI[lE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
RPMI-6666 MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\CeGlEPTB;MD60NVEzKM7:TR?= NEPHXok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
OPM-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC1T45KUUN3ME2wMlQyPTF|IN88US=> M3nic|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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MV4-11 M2XXdGZ2dmO2aX;uJIF{e2G7 NXy4S2tDOjByIH7N NGO4RXYzPCCqcoO= M{K5O2lvcGmkaYTpc44hd2ZiY3zhd5MhOSCKRFHDJIlvKGi3bXHuJG1XPC1zMTDj[YxteyCjc4Pld5Nm\CCjczDofZBmemGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFMh[XRiMkCwJI5OKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNw NVPjR2JFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3N|g6PTNpPkK5O|M5QTV|PD;hQi=>
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HL60 MWDBdI9xfG:|aYOgZZN{[Xl? NGTwUFA2KHWP MljZOFghcHK| NF\wTmlKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iY3zlZZZm\CCSQWLQJIxmfmWuIHH0JFUhfU1iYX\0[ZIhPDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcz6= M{Ds[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEG1NFA6Lz5{OESxOVAxQTxxYU6=
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HEL Moj1R4VtdCCleXPs[UBienKnc4SgZZN{[Xl? MV:1JJVO M2H5blI1KGi{cx?= M1XVRWNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGhGVCClZXzsd{BifCB3IIXNJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[ub4egZ5l1d22ndILpZ{Bu\XSqb3Su M{HwWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUi5OFQyLz5{OUW4PVQ1OTxxYU6=
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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
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 2022-08-01)

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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