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 12 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 MnLoSpVv[3Srb36gZZN{[Xl? NWHrRYZvPSCvaX7z NFvo[3hKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIH\1cIwhdGWwZ4ToJGhFSUNzIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KHW|aX7nJIJqd3SrbonsZZRm\CCueYPpcoUhQSCjY3X0fYxifGWmIHjpd5RwdmViSEOgLFEhfG9iMkGgdoV{cWS3ZYOpJIF{KHO3YoP0doF1\SCrbnP1ZoF1\WRiZn;yJFUhdWmwczDmc4xtd3enZDDifUB{fWK|dILheIUh[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgOlAhdWluIFnDOVAhRSByLkGxNkDPxE1w NGK0XlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEizOVc6Pyd-Mki4N|U4QTd:L3G+
EBC1 MnLlRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NV3H[INuPzJiaILz MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWEQ{GgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDJwOTFOwG0v MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh|NUe5O{c,Ojh6M{W3PVc9N2F-
HCT116 NGjqb5BCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVq3NkBpenN? NGHyUVFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gO{45KM7:TT6= NWTPO2dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4N|U4QTdpPkK4PFM2Pzl5PD;hQi=>
HL60 NHjIeoRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYXQWm1yPDhiaILz M{\Hd2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhNPjBiY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRUKG2ndHjv[EwhT0l3MDC9JFAvPCEQvF2u MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOlIyQTh6Lze+R4hGVUKOPD;hQi=>
Jurkat NGXQ[|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3LsNlQ5KGi{cx?= Mo[1S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTpVzc2G2IHPlcIx{KGmwY4XiZZRm\CCob4KgOFghcHK|IHL5JG1VWyCvZYToc4QtKEeLNUCgQUAyNjVizszNMi=> M1zBbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
hematopoietic malignant cells NHzTVoVEgXSxdH;4bYNqfHliYYPzZZk> NVyzbnR4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hcGWvYYTvdI9q\XSrYzDtZYxq\26jboSgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36sJGdKPTBiPTCxMlg3KM7:TT6= M{DUeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
U2OS M2q2RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mk\wOFghcHK| Mn;xS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gWVJQWyClZXzsd{BqdmO3YnH0[YQh\m:{IES4JIhzeyCkeTDNWHMhdWW2aH;kMEBIUTVyIE2gNkDPxE1w MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOlIyQTh6Lze+R4hGVUKOPD;hQi=>
HepG2 NFvaV4ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojHOFghcHK| MmT0S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTIVxTzJiY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRUKG2ndHjv[EwhT0l3MDC9JFQh|ryPLh?= NXnCTG5bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
LNCAP MofuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmXqOFghcHK| NGPNR2NIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBNVkODUDDj[YxteyCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBOXFNibXX0bI9lNCCJSUWwJF0hPCEQvF2u NEDqOos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
Raji MnG0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXjGclFtPDhiaILz MVPHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDSZYpqKGOnbHzzJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IF3UV{Bu\XSqb3SsJGdKPTBiPTC0JO69VS5? NHvMU2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
MCF7 MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH\kVWI1QCCqcoO= NXvUdWJIT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxteyCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBOXFNibXX0bI9lNCCJSUWwJF0hPSEQvF2u NWXxXJN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
28SC M4LRWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUjKWW1LPDhiaILz MlH3S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gNlhUSyClZXzsd{BqdmO3YnH0[YQh\m:{IES4JIhzeyCkeTDNWHMhdWW2aH;kMEBIUTVyIE2gOU45KM7:TT6= NFfMWlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
PANC1 NHjTWGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFvtOpA1QCCqcoO= M1PPNmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHBCVkNzIHPlcIx{KGmwY4XiZZRm\CCob4KgOFghcHK|IHL5JG1VWyCvZYToc4QtKEeLNUCgQUA3NjNizszNMi=> Mk\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
human solid tumor cells NXezdW5PS3m2b4TvfIlkcXS7IHHzd4F6 NGnr[lVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckB{d2yrZDD0eY1weiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdixiR1m1NEA:KDZwNkWg{txONg>? MnHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
HeLa MYjGeY5kfGmxbjDhd5NigQ>? MX6xNEBucW6| Mn;1TY5pcWKrdHnvckBw\iCKRFHDJIVvgnmvYYTpZ{Bi[3Srdnn0fUBqdiCqdX3hckBJ\UyjIHPlcIx{KGmwY4XiZZRm\CCob4KgNVAhdWmwczDpckBxemW|ZX7j[UBw\iC|dXLzeJJifGViYomgZ49td3KrbXX0dolkKGGldHn2bZR6KGG|c3H5MEBKSzVyIE2gO{4zKM7:TT6= MoDyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
MDA-MB-231 NWPK[XhNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\EV|Q5KGi{cx?= M2H2e2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgbY5kfWKjdHXkJIZweiB2ODDodpMh[nliTWTTJI1mfGixZDygS2k2OCB;IEeuPUDPxE1w M4G5dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
SMMC7721 M4fPTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4[yUVQ5KGi{cx?= NFfPO5hIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUVU2FN{eyNUBk\WyuczDpcoN2[mG2ZXSg[o9zKDR6IHjyd{BjgSCPVGOgcYV1cG:mLDDHTVUxKD1iMU[g{txONg>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOlIyQTh6Lze+R4hGVUKOPD;hQi=>
DU145 NUTSO|BTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVHIUIhTPDhiaILz NFvLOWlIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBFXTF2NTDj[YxteyCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBOXFNibXX0bI9lNCCJSUWwJF0hOjVizszNMi=> NEDSVoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
HeLa NWHyOYttT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVy0PEBpenN? MnztS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTIVN[SClZXzsd{BqdmO3YnH0[YQh\m:{IES4JIhzeyCkeTDNWHMhdWW2aH;kMEBIUTVyIE2gOFAh|ryPLh?= M1v3VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
U2OS MWXGeY5kfGmxbjDhd5NigQ>? MXyxJJVO NUn1d|RKOjRiaILz NF3He45C[3SrdnH0bY9vKG:oIGDQRXJIKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiYYSgNUB2VSCrbjDwdoV{\W6lZTDv[kAyOCC3TTDyc5Nq\2yrdHH6c45mKGmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigQ>? MnnzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
U2OS NGjVe|VHfW6ldHnvckBie3OjeR?= M1faUFEhfU1? MVGyOEBpenN? NHPSXmdC[3SrdnH0bY9vKG:oIFXSZoV1[SBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDoeY1idiCXMl;TJINmdGy|IHH0JFEhfU1iaX6gdJJme2WwY3Wgc4YhOC5yMTD1UUBGOiCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? M{[4bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM3OjF7OEivK|5EcEWPQly8M4E,
U2OS NH\5Zm9HfW6ldHnvckBie3OjeR?= NVTpV2tYOSC3TR?= M4rYS|I1KGi{cx?= M4HLXmFkfGm4YYTpc44hd2ZiZ3z1cINw[2:{dHnjc4llKHKnY3XweI9zKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiYYSgNUB2VSCrbjDwdoV{\W6lZTDv[kAxNjFidV2g[IV5[W2ndHjhd49v\SCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? NWXtfHd4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzZ{MUm4PE8oRkOqRV3CUFww[T5?
U2OS NYrkbGdNTnWwY4Tpc44h[XO|YYm= NYm1WYlJOSC3TR?= M13VZVI1KGi{cx?= NUnodGZ{SWO2aY\heIlwdiCxZjDFVoFteGijIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIGWyU3Mh[2WubIOgZZQhOSC3TTDpckBxemW|ZX7j[UBw\iByLkCxJJVOKEV{IHnuZ5Vj[XSnZDDmc5IhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= MkDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
U2OS Mn7DSpVv[3Srb36gZZN{[Xl? MWOxJJVO MWiyOEBpenN? M3jTfGFkfGm4YYTpc44hd2ZiZ3z1cINw[2:{dHnjc4llKHKnY3XweI9zKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIHj1cYFvKFV{T2OgZ4VtdHNiYYSgNUB2VSCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? NFHW[WU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PjJzOUi4M{c,S2iHTVLMQE9iRg>?
U2OS NXjKVWZNTnWwY4Tpc44h[XO|YYm= MlTKNUB2VQ>? NEjFOXAzPCCqcoO= MXnBZ5RqfmG2aX;uJI9nKFCSQWLHJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGi3bXHuJHUzV1NiY3XscJMh[XRiMTD1UUBqdmO3YnH0[YQh\m:{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> MlfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
U2OS MXrGeY5kfGmxbjDhd5NigQ>? M{D4eFEhfU1? M3P5c|I1KGi{cx?= NVLVWFhESWO2aY\heIlwdiCxZjDFVoFteGijIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIGWyU3Mh[2WubIOgZZQhOSC3TTDpcoN2[mG2ZXSg[o9zKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MmPJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|YzOTl6OD:nQmNpTU2ETEyvZV4>
U2OS NHy0dmlHfW6ldHnvckBie3OjeR?= NH\2Z|cyKHWP M3PDdFI1KGi{cx?= MXzBZ5RqfmG2aX;uJI9nKEWUYnX0ZUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCqdX3hckBWOk:VIHPlcIx{KGG2IEGgeW0hcW6ldXLheIVlKG[xcjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6 MXy8ZUB1[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).

Animal Research:

[1]

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

Solubility (25°C)

In vitro

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

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 Recruiting Drug: HBI-8000 in combination with pembrolizumab Non Small Cell Lung Cancer HUYABIO International LLC. March 14 2022 Phase 2
NCT04994210 Recruiting Drug: Sintilimab|Drug: Chidamide Safety and Efficacy Sun Yat-sen University October 4 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

(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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