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 M4G3bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTKTWM2OD1yLkC2NUDPxE1? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
ALL-PO MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXJTWM2OD1yLkC2N|U2KM7:TR?= NIn6Zpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
697 NUTwU5ByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;OTWM2OD1yLkC5PVc3KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NCI-H748 NH7WVYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwMUCzN|Qh|ryP M{TPZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NKM-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMUC5NVIh|ryP NYqyVmFvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
ES1 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwMUGyOVUh|ryP MnrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NCI-H1963 NYPYZ|doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXUTWM2OD1yLkGxOVc6KM7:TR?= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NCI-H1417 NUnpUWRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELNWFNKSzVyPUCuNVI6PzRizszN MoDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NEC8 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TLWGlEPTB;MD6xN|UzPyEQvF2= MmjXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
CRO-AP2 Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\JTWM2OD1yLkG2PFg6KM7:TR?= NFfRTXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
A3-KAW M1\h[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjDTWM2OD1yLkG3OlI4KM7:TR?= M3\a[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
SF539 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\1XoV1UUN3ME2wMlE6PTl|IN88US=> MkPDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NOS-1 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfKTWM2OD1yLkG5OlE6KM7:TR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NTERA-S-cl-D1 NXvteWtOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnHSZZKSzVyPUCuNlAyOTNizszN Mn7sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
COR-L88 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnCTWM2OD1yLkKyPVU6KM7:TR?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
EM-2 Ml20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVmzepBGUUN3ME2wMlI1ODd7IN88US=> NF3WcW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
KARPAS-45 NH;hboNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[wTWM2OD1yLkK3PFM{KM7:TR?= NWLIS5k2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
DSH1 M{e5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwMki3NFgh|ryP NX\YToVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
HT-144 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLZeZJKSzVyPUCuN|AzPTZizszN MnvBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
ATN-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjPT45KSzVyPUCuN|A2PzZizszN NEfCW3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
HEL MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLKTWM2OD1yLkOxN|Q5KM7:TR?= NGfZeYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NB12 NH[1fmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zKOmlEPTB;MD6zNVc2PiEQvF2= NHjOOXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
LU-139 NHSzZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPJSWlKSzVyPUCuN|M2OSEQvF2= NWm5WI5jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
J-RT3-T3-5 MkTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;ncY1PUUN3ME2wMlM{PzF4IN88US=> NGLxOlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
MOLT-13 M{O0Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrZTWM2OD1yLkOzPFEh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
SR NHvDcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLpPVBKSzVyPUCuN|QzPjFizszN NELFSXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
CMK NEmzU2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nDPWlEPTB;MD6zOVczPyEQvF2= NF7YUYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
ES8 MkfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEWyVndKSzVyPUCuN|YxOjJizszN NUD2OXZ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
LB647-SCLC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDtOVNKSzVyPUCuN|Y4OyEQvF2= NWXHPHhFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
TE-8 NYDTT4VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:wT4xKSzVyPUCuN|Y6OzVizszN NITyT|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
BV-173 M4\1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDWPHdpUUN3ME2wMlM4OTJzIN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
DEL NY[1T|drT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M172VWlEPTB;MD6zO|Q5PyEQvF2= NX\kcWhoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
ARH-77 M2fqT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIi3dHRKSzVyPUCuN|gyQTNizszN NV64TFgzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
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RPMI-8402 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\kTWM2OD1yLkO4O|AyKM7:TR?= M3HQbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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SK-MM-2 M{jPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwM{m4Olgh|ryP M2Pm[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
CHP-126 NFLON2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwNECyN|Eh|ryP MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
A101D NGDCZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHYTWM2OD1yLkSwN{DPxE1? MmnsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
SCH MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwNECzOFIh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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NCI-H209 NHq2cm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHZTYRKSzVyPUCuOFA3OTNizszN MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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RPMI-6666 MoTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DveWlEPTB;MD60NVEzKM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
OPM-2 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTZTWM2OD1yLkSxOVE{KM7:TR?= NGXtcXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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NCI-H2171 MmnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDjXVZ{UUN3ME2xMlM1PTB{IN88US=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
JiyoyeP-2003 M4jwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jQW2lEPTB;MT6zOVM6KM7:TR?= M2iwVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NCI-H2107 NUPONm5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTveWo3UUN3ME2xMlM2QDh|IN88US=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
BB30-HNC NH3ZeYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C5VGlEPTB;MT6zPFk4QCEQvF2= NEXoVHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
K-562 NXvqO|NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PjT2lEPTB;MT6zPVIyQSEQvF2= NVvrb|FnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
PSN1 Mn;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoKxTWM2OD1zLkSyNlg4KM7:TR?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
HCC2157 MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnrXXR2UUN3ME2xMlQzPjlzIN88US=> M4W1ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
SBC-1 MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFwNEK3OFEh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
MC116 Mo\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFwNEO2NVUh|ryP Ml:1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
KARPAS-422 MmmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DYfmlEPTB;MT60OVM2QCEQvF2= NYLqW|ZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
LB996-RCC MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHDUGRrUUN3ME2xMlQ4OTB|IN88US=> M3XpWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
MSTO-211H MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HpTGlEPTB;MT60O|k5PyEQvF2= M2DHTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
BT-474 MlLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTFwNUG3OlQh|ryP NIPYTGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
A388 NGjCb|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zaU2lEPTB;MT61NVk1PSEQvF2= NXfrfFZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
SJSA-1 NFLFdGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjyTWM2OD1zLkWyNlYh|ryP NWXwTpp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
COLO-829 MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkSyTWM2OD1zLkWzOVY1KM7:TR?= MkSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
KM-H2 M4e1Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PKWGlEPTB;MT61OlY4KM7:TR?= M2nmZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
GR-ST M3HtdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj3fnBiUUN3ME2xMlU3QDJizszN M{DWT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
RPMI-8866 NFfLUphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwNkCxOFQh|ryP NUPMbmFyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
KG-1 MkT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjrTWM2OD1zLk[xPVAyKM7:TR?= M3zqZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NCI-H82 M2LJVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTzSXMyUUN3ME2xMlY{PDB4IN88US=> NVX6OmRSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
LB1047-RCC NEnS[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrYTWM2OD1zLk[zOFU6KM7:TR?= Ml[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
KM12 NXf6RpFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXLeZJKSzVyPUGuOlQ4KM7:TR?= M1jNN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NB5 M3XQ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXWxN|V1UUN3ME2xMlY2Pjd5IN88US=> NELzdYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
HDLM-2 NGTNSHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7McIlKSzVyPUGuOlgzQDFizszN M3T5dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
KU812 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvIZotKSzVyPUGuOlk3ODVizszN MnfIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
DB M4O2eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwN{CzOVMh|ryP Mk\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
HD-MY-Z M2jMSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYWyVIdrUUN3ME2xMlc2OjN2IN88US=> NYrwRpV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
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HUTU-80 NH;PbZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjMTHZKSzVyPUGuO|k2ODhizszN NHPHU4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
ES7 MlLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTFwOECzNFIh|ryP NFLxPHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
SW872 NYHEc|F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPGbmlFUUN3ME2xMlgyOzl3IN88US=> MlmwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
TK10 NIexcVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\oTWM2OD1zLkizNVA5KM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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MLMA MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFwOEiyN|Qh|ryP M3T1[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
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GB-1 M{fCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHMflNKSzVyPUGuPVM5PjZizszN M3y4cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
IST-SL2 NWq4T|NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknITWM2OD1{LkCwNlYzKM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
LAN-6 MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLGTWM2OD1{LkCxPVY3KM7:TR?= NWPsUo9YRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
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NCI-H1092 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJwMEWxNlQh|ryP Ml\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
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MV4-11 M33D[GZ2dmO2aX;uJIF{e2G7 NGnwXZMzODBibl2= NGH0c|YzPCCqcoO= Mlf3TY5pcWKrdHnvckBw\iClbHHzd{AyKEiGQVOgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IHj5dIVz[WOndInsZZRqd25ib3[gbIl{fG:wZTDIN{BifCB{MECgcm0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqey5? NH[2SWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUezPFk2Oyd-Mkm3N|g6PTN:L3G+
HL60 NX7NN5A5SXCxcITvd4l{KGG|c3H5 NYLScZAzPSC3TR?= MXu0PEBpenN? M37RXmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCycn;jZZNx[XOnLUOgcIV3\WxiYYSgOUB2VSCjZoTldkA1QCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|Lh?= Mn35QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MUWwNFkoRjJ6NEG1NFA6RC:jPh?=
HL60 M2\rOGFxd3C2b4Ppd{Bie3OjeR?= MnnDOUB2VQ>? MmrpOFghcHK| MUDJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2ynYY\l[EBk[XOyYYPlMVMhdGW4ZXygZZQhPSC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMi=> NWT3PWlyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NVUxODlpPkK4OFE2ODB7PD;hQi=>
HL60 NVXT[nFbSXCxcITvd4l{KGG|c3H5 M2D2TlUhfU1? NHniOmg1QCCqcoO= MorDTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQhWEGUUDDs[ZZmdCCjdDC1JJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNw NID2bFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESxOVAxQSd-Mki0NVUxODl:L3G+
MV4-11 NWnKfVB7S2WubDDjfYNt\SCjcoLld5Qh[XO|YYm= NXe4empLPSC3TR?= NGH4RnYzPCCqcoO= MlTmR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCC|dXKtS|EheGijc3WgZZQhPSC3TTDh[pRmeiB{NDDodpMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndG:5IHP5eI9u\XS{aXOgcYV1cG:mLh?= NULzW4JkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1PFk1PDFpPkK5OVg6PDRzPD;hQi=>
HEL NInLV5hE\WyuIHP5Z4xmKGG{cnXzeEBie3OjeR?= NUXNVYVDPSC3TR?= Ml6zNlQhcHK| NXXNOnlFS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUEWOIHPlcIx{KGG2IEWgeW0h[W[2ZYKgNlQhcHK|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnzve{BkgXSxbXX0dolkKG2ndHjv[E4> M1e4[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUi5OFQyLz5{OUW4PVQ1OTxxYU6=
Jurkat M3q0R2NmdGxiY4njcIUh[XK{ZYP0JIF{e2G7 MnPZOUB2VQ>? M1\mWlI1KGi{cx?= MVfD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDKeZJs[XRiY3XscJMh[XRiNTD1UUBi\nSncjCyOEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobH;3JIN6fG:vZYTybYMhdWW2aH;kMi=> NX7GXXVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1PFk1PDFpPkK5OVg6PDRzPD;hQi=>
MV4-11 MlfRSpVv[3Srb36gZZN{[Xl? MX:1JJVO NGHT[2czPCCqcoO= MWTJcohq[mm2aX;uJI9nKGOuYYPzJFEhUESDQzDpckBpfW2jbjDNWlQuOTFiY3XscJMh[XO|ZYPz[YQh[XNiaX7keYN1cW:wIH;mJIhqe3SxbnWgbJlx\XKjY3X0fYxifGmxbjDheEA2KHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:mLh?= NW\3VFNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1PFk1PDFpPkK5OVg6PDRzPD;hQi=>
LNCAP MlfXSpVv[3Srb36gZZN{[Xl? MVexNEB2VQ>? M4fSNFI1KGi{cx?= NFmweZJKdmirYnn0bY9vKG:oIFjERWM3KGmwIHj1cYFvKEyQQ1HQJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRFjUMYlv\HWlZXSgZYxxcGFvdIXieYxqdiCmZXHj[ZR6dGG2aX;uJIJ6KG2nYYP1dolv\yCrbnPy[YF{\SCrbjDhcJBp[S22dXL1cIlvKGGlZYT5cIF1cW:wIHH0JFExKHWPIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{Bz\WyjdHn2[UB1dyClb370do9tNg>? Ml31QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd5MUe1OFQoRjJ5N{G3OVQ1RC:jPh?=
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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