Tucidinostat (Chidamide)

Catalog No.S8567 Synonyms: HBI-8000, CS-055

For research use only.

Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.

Tucidinostat (Chidamide) Chemical Structure

CAS No. 1616493-44-7

Selleck's Tucidinostat (Chidamide) has been cited by 9 Publications

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Biological Activity

Description Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
Targets
HDAC3 [1]
(Cell-free)
HDAC10 [1]
(Cell-free)
HDAC1 [1]
(Cell-free)
HDAC2 [1]
(Cell-free)
67 nM 78 nM 95 nM 160 nM
In vitro

Chidamide inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly induces histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC. Cell growth inhibition studies performed with 18 human-derived tumor cell lines demonstrate that chidamide and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, chidamide, and to a lesser extent MS-275, is significantly less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCC-HEL), indicating a differential cytotoxic response of normal cells versus cancerous cells to chidamide[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 MX;GeY5kfGmxbjDhd5NigQ>? M3[2T|UhdWmwcx?= MYjJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIFjERWMyKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBtgXOrbnWgPUBi[2W2eXzheIVlKGirc4TvcoUhUDNiKEGgeI8hOjFicnXzbYR2\XNrIHHzJJN2[nO2cnH0[UBqdmO3YnH0[YQh\m:{IEWgcYlveyCob3zsc5dm\CCkeTDzeYJ{fHKjdHWgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiNkCgcYktKEmFNUCgQUAxNjFzMjFOwG0v M4jURVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEO1O|k4Lz5{OEizOVc6PzxxYU6=
EBC1 NGDUUHdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXG3NkBpenN? MkGwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCHQlOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB{Lkmg{txONg>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh|NUe5O{c,Ojh6M{W3PVc9N2F-
HCT116 MmfGRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUC3NkBpenN? M3TySWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTC3Mlgh|ryPLh?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh|NUe5O{c,Ojh6M{W3PVc9N2F-
HL60 M2f6dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPrZnRXPDhiaILz NFrRXnBIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJVDZyIHPlcIx{KGmwY4XiZZRm\CCob4KgOFghcHK|IHL5JG1VWyCvZYToc4QtKEeLNUCgQUAxNjRizszNMi=> NILCT209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
Jurkat M1\GZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDTOFghcHK| MXzHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDKeZJs[XRiY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRUKG2ndHjv[EwhT0l3MDC9JFEvPSEQvF2u M2PMOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
hematopoietic malignant cells MYLDfZRwfG:6aXPpeJkh[XO|YYm= NHPTXYpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBp\W2jdH;wc4lmfGmlIH3hcIlodmGwdDDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjygS2k2OCB;IEGuPFYh|ryPLh?= NHPqZ4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
U2OS MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVvxR2t2PDhiaILz NXfmWmJIT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hXTKRUzDj[YxteyCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBOXFNibXX0bI9lNCCJSUWwJF0hOiEQvF2u NY\ZWXdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
HepG2 M3rtO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlm4OFghcHK| NEjMXItIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJ\XCJMjDj[YxteyCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBOXFNibXX0bI9lNCCJSUWwJF0hPCEQvF2u NXLwTotXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
LNCAP MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NU\5Z5NzPDhiaILz NX2we3IzT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVE6FQWCgZ4VtdHNiaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhVVSVIH3leIhw\CxiR1m1NEA:KDRizszNMi=> MmLCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
Raji M1vxdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUW0PEBpenN? M4LMbWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHJicmliY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRUKG2ndHjv[EwhT0l3MDC9JFQh|ryPLh?= NVna[pBHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
MCF7 Mm\0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn\MOFghcHK| M2PkN2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRUKG2ndHjv[EwhT0l3MDC9JFUh|ryPLh?= M4roUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
28SC M1iyN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MojDOFghcHK| NVexe2lmT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hOjiVQzDj[YxteyCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBOXFNibXX0bI9lNCCJSUWwJF0hPS56IN88UU4> NFfxU5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
PANC1 NWLOO|MxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWjxfpppPDhiaILz MlW4S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gVGFPSzFiY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRUKG2ndHjv[EwhT0l3MDC9JFYvOyEQvF2u MmTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
human solid tumor cells NEfkRoxEgXSxdH;4bYNqfHliYYPzZZk> M3HJ[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJNwdGmmIIT1cY9zKGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCJSUWwJF0hPi54NTFOwG0v NVnWS4E2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
HeLa MnjZSpVv[3Srb36gZZN{[Xl? MWqxNEBucW6| MWnJcohq[mm2aX;uJI9nKEiGQVOg[Y57gW2jdHnjJIFkfGm4aYT5JIlvKGi3bXHuJGhmVGFiY3XscJMhcW6ldXLheIVlKG[xcjCxNEBucW6|IHnuJJBz\XOnbnPlJI9nKHO3YoP0doF1\SCkeTDjc4xwemmvZYTybYMh[WO2aY\peJkh[XO|YYmsJGlEPTBiPTC3MlIh|ryPLh?= NXGwRpJIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
MDA-MB-231 MlfhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVS0PEBpenN? NWm0N5hxT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BqdmO3YnH0[YQh\m:{IES4JIhzeyCkeTDNWHMhdWW2aH;kMEBIUTVyIE2gO{46KM7:TT6= NHvWfFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
SMMC7721 NYTKOY1sT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTGW5o1QCCqcoO= MnzES5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gV21OSzd5MkGgZ4VtdHNiaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhVVSVIH3leIhw\CxiR1m1NEA:KDF4IN88UU4> M{LwNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
DU145 M{DmcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYi0PEBpenN? Mor1S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gSHUyPDViY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRUKG2ndHjv[EwhT0l3MDC9JFI2KM7:TT6= M33lOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
HeLa NV\VRYJzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX7uXYlLPDhiaILz MX3Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDI[WxiKGOnbHzzJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IF3UV{Bu\XSqb3SsJGdKPTBiPTC0NEDPxE1w NIGxO4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
U2OS NVHrfG1FTnWwY4Tpc44h[XO|YYm= NHPIfJgyKHWP MWGyOEBpenN? MmXlRYN1cX[jdHnvckBw\iCSUFHSS{ApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCqdX3hckBWOk:VIHPlcIx{KGG2IEGgeW0hcW5icILld4Vv[2Vib3[gNVAhfU1icn;zbYdtcXSjen;u[UBqdmO3YnH0[YQh\m:{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> NFvER3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
U2OS Mke2SpVv[3Srb36gZZN{[Xl? NF7Zc|cyKHWP NWTSOZZHOjRiaILz NGDOTFFC[3SrdnH0bY9vKG:oIFXSZoV1[SBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDoeY1idiCXMl;TJINmdGy|IHH0JFEhfU1iaX6gdJJme2WwY3Wgc4YhOC5yMTD1UUBGOiCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? M4nkN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
U2OS NWOw[|E{TnWwY4Tpc44h[XO|YYm= NV;t[pZbOSC3TR?= MmrlNlQhcHK| NVrXO5ZlSWO2aY\heIlwdiCxZjDncJVt[2:lb4L0bYNwcWRicnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbJVu[W5iVULPV{Bk\WyuczDheEAyKHWPIHnuJJBz\XOnbnPlJI9nKDBwMTD1UUBl\XijbXX0bIF{d26nIHnuZ5Vj[XSnZDDmc5IhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= MnzFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
U2OS MYnGeY5kfGmxbjDhd5NigQ>? M4TGfVEhfU1? M{i4W|I1KGi{cx?= MnrVRYN1cX[jdHnvckBw\iCHUnHsdIhiKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiYYSgNUB2VSCrbjDwdoV{\W6lZTDv[kAxNjBzIIXNJGUzKGmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigQ>? NFPiNI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
U2OS NGPwWmFHfW6ldHnvckBie3OjeR?= MUSxJJVO NWL4XnlGOjRiaILz NE\6ZXZC[3SrdnH0bY9vKG:oIHfseYxkd2OxcoTpZ49q\CC{ZXPldJRweiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDoeY1idiCXMl;TJINmdGy|IHH0JFEhfU1iaX7jeYJifGWmIH\vdkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOlIyQTh6Lze+R4hGVUKOPD;hQi=>
U2OS NX\qcolWTnWwY4Tpc44h[XO|YYm= MWCxJJVO NF\sZYIzPCCqcoO= NXLROJF5SWO2aY\heIlwdiCxZjDQVGFTTyBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDoeY1idiCXMl;TJINmdGy|IHH0JFEhfU1iaX7jeYJifGWmIH\vdkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOlIyQTh6Lze+R4hGVUKOPD;hQi=>
U2OS NVrj[WZqTnWwY4Tpc44h[XO|YYm= NFj4eJoyKHWP NELn[FMzPCCqcoO= NFPqV29C[3SrdnH0bY9vKG:oIFXSZYxxcGFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbJVu[W5iVULPV{Bk\WyuczDheEAyKHWPIHnuZ5Vj[XSnZDDmc5IhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= MojoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
U2OS NH;1SodHfW6ldHnvckBie3OjeR?= NIfNcGkyKHWP NIHN[WEzPCCqcoO= MljoRYN1cX[jdHnvckBw\iCHUnLleIEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hXTKRUzDj[YxteyCjdDCxJJVOKGmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigQ>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOlIyQTh6Lze+R4hGVUKOPD;hQi=>
Assay
Methods Test Index PMID
Western blot PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 ; p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK ; Ace-H3K18 / Ace-H3K9 / Ac-H4K8 ; Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 ; HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4 30854137 29773595 31289512
Growth inhibition assay Cell viability 29100410
In vivo In HCT-8 colorectal carcinoma mice xenografts, Chidamide shows in vivo antitumor activity. Chidamide in the dose range of 12.5-50 mg/kg dose-dependently reduces tumor size and tumor weight, and the dose of 50 mg/kg produces similar or greater efficacy compared with the control drugs 5-fluorouracil(5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models). However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: PBMC effector cells
  • Concentrations: 0-400 nM
  • Incubation Time: 0-400 nM
  • Method:

    Isolated PBMC effector cells are seeded into 6-well plates (6 x 106 cells/well) and treated with chidamide at different concentrations (0-400 nM) for different times (24-72 h).

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Athymic nude mice (BALB/c-nu)
  • Dosages: 12.5-50 mg/kg
  • Administration: oral
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 78 mg/mL
(199.78 mM)
Ethanol 2 mg/mL
(5.12 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.

30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 390.41
Formula

C22H19FN4O2

CAS No. 1616493-44-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N

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
NCT05141357 Not yet recruiting Drug: HBI-8000 in combination with pembrolizumab Non Small Cell Lung Cancer HUYABIO International LLC. December 2021 Phase 2
NCT04994210 Not yet recruiting Drug: Sintilimab|Drug: Chidamide Safety and Efficacy Sun Yat-sen University September 1 2021 Phase 2
NCT05140616 Recruiting Drug: Chidamide Safety and Efficacy The First Affiliated Hospital of Soochow University May 31 2021 Phase 1|Phase 2
NCT04651127 Recruiting Drug: Toripalimab + Chidamide Cervical Cancer|Cervix Cancer|Cervix Neoplasm Sun Yat-sen University November 9 2020 Phase 1|Phase 2
NCT03820596 Recruiting Drug: Sintilimab|Drug: Chidamide Safety and Efficacy Huiqiang Huang|Sun Yat-sen University March 29 2019 Phase 1|Phase 2

(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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