Ricolinostat (ACY-1215)

For research use only. Not for use in humans.

目录号:S8001 别名: Rocilinostat

Ricolinostat (ACY-1215)  Chemical Structure

CAS No. 1316214-52-4

Ricolinostat (ACY-1215, Rocilinostat) 是一种选择性HDAC6抑制剂,无细胞试验中IC50为5 nM,作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上,对HDAC8具有微弱的作用活性,对HDAC4/5/7/9/11, Sirtuin1和Sirtuin2具有最小的作用活性。Ricolinostat (ACY-1215) 可抑制细胞增殖并促进凋亡。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1566.47 现货
RMB 900.21 现货
RMB 1419.09 现货
RMB 4664.38 现货
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客户使用Selleck生产的Ricolinostat (ACY-1215) 发表文献44篇:

产品安全说明书

HDAC抑制剂选择性比较

生物活性

产品描述 Ricolinostat (ACY-1215, Rocilinostat) 是一种选择性HDAC6抑制剂,无细胞试验中IC50为5 nM,作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上,对HDAC8具有微弱的作用活性,对HDAC4/5/7/9/11, Sirtuin1和Sirtuin2具有最小的作用活性。Ricolinostat (ACY-1215) 可抑制细胞增殖并促进凋亡。Phase 2。
特性 ACY-1215作用于4名健康捐献者的PHA刺激的PBMCs,与pan-HDAC抑制剂SAHA相比,具有更低的细胞毒性。
靶点
HDAC6 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC8 [1]
(Cell-free assay)
4.7 nM 48 nM 51 nM 58 nM 100 nM
体外研究

ACY-1215是一种异羟肟酸类衍生物。ACY-1215作用于HDAC1, HDAC2, 和 HDAC3 (I型 HDACs)效果分别低12,10, 和 11倍。ACY-1215最低活性作用于(IC50>1μM) HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1,和 Sirtuin2,对HDAC8(IC50=0.1μM)具有轻微的作用活性。ACY-1215作用于T细胞毒性的IC50值为2.5μM。ACY-1215作用于骨髓(BM)环境,克服BMSCs和细胞因子赋予的肿瘤细胞生长和存活。ACY-1215与Bortezomib联用,诱导协同抗MM活性。ACY-1215在非常低的剂量时,诱导强有力的α-tubulin乙酰化,只有在较高剂量时,触发组蛋白H3和H4组蛋白赖氨酸的乙酰化,证实其对HDAC6活性的特定抑制效果。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A-172 NXHQUlZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPZNVDDqG6P MkjONlQwPDhiaB?= NVvNbnpMcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NUj1bW8{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOVA{PDBpPkK2NVUxOzRyPD;hQi=>
U87MG NFn4SJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HrUVExyqCwTR?= Mn35NlQwPDhiaB?= NIXlc4pqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NVqxTFFYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOVA{PDBpPkK2NVUxOzRyPD;hQi=>
Hbl-1 NVPKdYtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYW0PEBp MWHJR|UxRTFwNjFOwG0> NV[5NmF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
OCI-Ly10 NHvhbIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrhOIE1QCCq NWfwRVA{UUN3ME2wMlkh|ryP NH60SY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Riva MnnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTPcGRjPDhiaB?= M{LNS2lEPTB;Mj6yJO69VQ>? Ml[yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
Su-DHL2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHle2o1QCCq M3z3[WlEPTB;Mz6zJO69VQ>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
OCI-Ly1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLQSo4{PDhiaB?= MnjtTWM2OD1{LkSg{txO NYC5WHBlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
OCI-Ly7 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\BPWc5PDhiaB?= M1jCPGlEPTB;MT6yJO69VQ>? NF[yVGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Su-DHL4 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVO0PEBp M1jy[WlEPTB;ND63JO69VQ>? M{D2clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Su-DHL6 M1jUfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXm0PEBp NUj1OmRtUUN3ME2zMlIh|ryP MorUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
Hbl-2 NYTQc4Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DqPVQ5KGh? MUDJR|UxRTFwOTFOwG0> M1LSSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Jeko-1 M4PGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\XUVQ5KGh? NHy2VXBKSzVyPUGuOUDPxE1? Mmr2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
Jvm-2 NEjONoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LGPFQ5KGh? NY\0S|h7UUN3ME20MlAh|ryP MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Rec-1  MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLnOFghcA>? NXL1bGZtUUN3ME2yMlMh|ryP M{j5VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
CCL-119 NW\KOHZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWG0PEBp MnjnTWM2OD1zLkeg{txO NF\UO3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
H9 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnrOFghcA>? MYXJR|UxRTFwMjFOwG0> NGfMcG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
HH MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T1XlQ5KGh? NYKzXGdZUUN3ME2yMlUh|ryP MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Sup-T1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\RW|Q5KGh? M2HzWWlEPTB;MT62JO69VQ>? M4XsRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
MM.1S M1zubWZ2dmO2aX;uJGF{e2G7 MWewMVXPxE1? MUS2JIg> NYfkT5F2cW6lcnXhd4V{KGGlZYT5cIF1\WRizsGteJVjfWyrbh?= NHvlc|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
MM.1S NXnJ[mltTnWwY4Tpc44hSXO|YYm= NIfxfnQxNjJ3L{JOwG0> NH3FOW8yQCCq MXvpcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv MmfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
MM.1R M4nvTmZ2dmO2aX;uJGF{e2G7 MUmwMlI2NzIQvF2= NUHnTXpVOThiaB?= NFv5UlFqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw NYnKNJVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
RPMI8226  NXjGdYc1TnWwY4Tpc44hSXO|YYm= MnnGNE4zPS9zzszN MXSxPEBp MlrwbY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? NUTZeWVSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
MM.1S NXTETJdrS2WubDDWbYFjcWyrdImgRZN{[Xl? M1rnfVAuQM7:TR?= NIL3No41QCCq MYDk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
OPM1 NX7ERnVRS2WubDDWbYFjcWyrdImgRZN{[Xl? NXzJ[4NMOC16zszN M325XlQ5KGh? Mn;z[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Mlv5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
RPMI NUjrTmRrS2WubDDWbYFjcWyrdImgRZN{[Xl? MWmwMVjPxE1? MWS0PEBp NV7PRolt\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NITWO2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
MM.1R MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4\sT|AuQM7:TR?= NIjvTVE1QCCq M1TDdoRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1;BXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[yO|YxLz5{MkK2Nlc3ODxxYU6=
LR5 MlHTR4VtdCCYaXHibYxqfHliQYPzZZk> M1i1R|AuQM7:TR?= MkDkOFghcA>? NEXhW2Nl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmLVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
OPM2 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NETzTGUxNTkQvF2= MXK0PEBp MVHk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NUjO[ldYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
Sf9 NEG0eHVHfW6ldHnvckBie3OjeR?= MkC0NVAhdWmwcx?= NWPENnc3UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBpfW2jbjDy[YNwdWKrbnHueEBPNXSncn3pcoFtKEeVVD30ZYdo\WRiSFTBR|Yh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCIVGOgZZMhe3Wkc4TyZZRmKHC{ZXnuZ5Vj[XSnZDDmc5IhOTBibXnud{Bnd2yub4fl[EBjgSC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRib4\ldkA{OCCvaX7zMEBKSzVyIE2gNE4xODR5IN88UU4> NFTqenA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECzPFMzPCd-MkiwN|g{OjR:L3G+
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Sf9 MmHVSpVv[3Srb36gZZN{[Xl? NX;VVGRrOTVibXnudy=> MVTJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIFOteIVzdWmwYXygTIl{NXSjZ3fl[EBJTEGFMz;OMZRmem2rbnHsJGdUXC22YXfn[YQhVkORUkKgLFM6PSC2bzC0PFkhemW|aXT1[ZMqKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EB{\jliY3XscJMhfXOrbnegRo9kNUy7cz2oRYMqNUGPQzDhd{B{fWK|dILheIUheHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIktKEmFNUCgQUAxNjB|NzFOwG0v NVHPcpN5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NFAyOzBpPkK5OVAxOTNyPD;hQi=>
Sf9 M3jPSmZ2dmO2aX;uJIF{e2G7 NHXBbJoyOCCvaX7z MorBTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDoeY1idiC{ZXPvcYJqdmGwdDDDMZRmem2rbnHsJGZNSUdvdHHn[4VlKEiGQVOyJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNidYPpcochTlSVIHHzJJN2[nO2cnH0[UBxemWrbnP1ZoF1\WRiZn;yJFExKG2rboOg[o9tdG:5ZXSgZpkhe3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKG:4ZYKgN|AhdWmwczygTWM2OCB;IECuNFQ5KM7:TT6= M1LBPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4N|I1Lz5{OECzPFMzPDxxYU6=
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BCP-ALL MWPDfZRwfG:6aXPpeJkh[XO|YYm= MWK3NkBpenN? MkCyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmNRNUGOTDDj[YxteyCmZYLpeoVlKG[{b32gdIF1cWWwdDCxJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4zQSEQvF2u MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
BCP-ALL MYXDfZRwfG:6aXPpeJkh[XO|YYm= NH;afoQ4OiCqcoO= M{XCS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJEWC2DTFygZ4VtdHNiZHXybZZm\CCocn;tJJBifGmnboSgOEBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPTRizszNMi=> M1fL[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
BCP-ALL MlH6R5l1d3SxeHnjbZR6KGG|c3H5 NYrhXGRlPzJiaILz M3nTcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJEWC2DTFygZ4VtdHNiZHXybZZm\CCocn;tJJBifGmnboSgNkBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPThizszNMi=> Mlu1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
RPMI8226 MX\DfZRwfG:6aXPpeJkh[XO|YYm= MVG3NkBpenN? NIm5cY5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTWE2LOEKyOkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT60Olgh|ryPLh?= M1HsNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NESzNFc5Lz5{NkS0N|A4QDxxYU6=
SEM MVzDfZRwfG:6aXPpeJkh[XO|YYm= MU[3NkBpenN? NXvTPHNDS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0WPIHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOS54MTFOwG0v MofQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
SUP-B15 MlHoR5l1d3SxeHnjbZR6KGG|c3H5 NGrodlQ4OiCqcoO= MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWXAuSjF3IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOS57MjFOwG0v MnrhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
RPMI18226 NVfISW5nS3m2b4TvfIlkcXS7IHHzd4F6 MXW3NkBpenN? MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSVG1KOTh{Mk[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSBzLkm3JO69VS5? NUnYb2F3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN|Y2QDl{PD;hQi=>
HL60 MUXDfZRwfG:6aXPpeJkh[XO|YYm= MY[3NkBpenN? NFvhdYNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOi5|NjFOwG0v NWf6fo95RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN|Y2QDl{PD;hQi=>
HL60 Mn;yRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M1zxS|Q5KGi{cx?= NWG3bmtCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IES4JIhzeyCrbjDwdoV{\W6lZTDv[kBLSUt{IHnubIljcXSxcjDDXXQuOzh5IHL5JGNEUy16IHHzd4F6NCCLQ{WwJF0hOi53NDFOwG0v MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MEGxOUc,Ojl7NECxNVU9N2F-
K562 NY\OZZRDSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Ml\iOFghcHK| NWPl[2VNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IES4JIhzeyCrbjDwdoV{\W6lZTDv[kBLSUt{IHnubIljcXSxcjDDXXQuOzh5IHL5JGNEUy16IHHzd4F6NCCLQ{WwJF0hOi53NDFOwG0v M1nP[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwNVE2Lz5{OUm0NFEyPTxxYU6=
HEL M{m5[GFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NUDGSXVIPDhiaILz M3TsTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFXMJINmdGy|IHHmeIVzKDR6IHjyd{BqdiCycnXz[Y5k\SCxZjDKRWszKGmwaHnibZRweiCFWWStN|g4KGK7IFPDT{05KGG|c3H5MEBKSzVyIE2gNk42PCEQvF2u NXjoflNiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFAyOTVpPkK5PVQxOTF3PD;hQi=>
KCL22 M4HSNmN6fG:2b4jpZ4l1gSCjc4PhfS=> MWK3NkBpenN? MWHDfZRwfG:6aXPpeJkh[WejaX7zeEBqdWG2aX7pZk1z\XOrc4ThcpQhcHWvYX6gT2NNOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA{NjN6IN88UU4> MliyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
U266 NWfHTHB3S3m2b4TvfIlkcXS7IHHzd4F6 NF7kTmU4OiCqcoO= NU[5T252S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTJ4NjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDNwNUKg{txONg>? M2PtU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
SUP-B15 NIrsTmdEgXSxdH;4bYNqfHliYYPzZZk> M2LPdFczKGi{cx?= M{HTOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGmvYYTpcoljNXKnc3nzeIFvfCCqdX3hckBUXVBvQkG1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMz61OEDPxE1w MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
KCL22 MVTDfZRwfG:6aXPpeJkh[XO|YYm= NWnFUZd{PzJiaILz Ml\1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2NNOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA{Njd3IN88UU4> NHTIN489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
HL60 NYHjNGp6SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MVm0PEBpenN? M3XCV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLMVgh[XO|YYmsJGlEPTBiPTCzMlc2KM7:TT6= NH3TW449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
K562 M3j1OGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVTWUoY2PDhiaILz M4mzSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLMVgh[XO|YYmsJGlEPTBiPTCzMlc2KM7:TT6= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MEGxOUc,Ojl7NECxNVU9N2F-
HEL MlrkRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2f0OVQ5KGi{cx?= M1vHTmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFXMJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OCB;IEOuO|Uh|ryPLh?= NEXvfIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
BCP-ALL MkPIR5l1d3SxeHnjbZR6KGG|c3H5 NGDvc2o4OiCqcoO= M4HC[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJEWC2DTFygZ4VtdHNiZHXybZZm\CCocn;tJJBifGmnboSgN{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQvPDVizszNMi=> NFXBVJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
MV4-11 MUHGeY5kfGmxbjDhd5NigQ>? MWqxNFAxKG6P M4qyNVYhcHK| NY\4N2oyUW6qaXLpeIlwdiCxZjDISGFEOS9{L{OgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IIXwdoVofWyjdHnvckBw\iCqaYP0c45mKEh|IHHj[ZR6dGG2aX;uJIF1KDFyMECgcm0h[W[2ZYKgOkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MmC0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEOwO|goRjJ4NESzNFc5RC:jPh?=
TC32 MYLxTHRUKGG|c3H5 MoPVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY NUjwe2VSeUiWUzDhd5NigQ>? NFTXWoVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= NETWc4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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A673 NWLR[Hh6eUiWUzDhd5NigQ>? NFrGWlRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MlvKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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BT-37 MV\xTHRUKGG|c3H5 MnPLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| NIrM[|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Ac-α-tubulin / Ac-Histone H4 ; 

PubMed: 31015208     


Ricolinostat promotes the accumulation of acetylated (Ac) α-tubulin. MM cells were treated with the indicated concentrations of ricolinostat for 24 hours. Protein expression was measured by immunoblotting. 

Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1; 

PubMed: 30050135     


Western blot analysis of G2/M phase cell cycle regulatory-proteins for 48 h

Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP; 

PubMed: 30050135     


Western blot analysis of apoptosis regulatory-proteins for 48 h

PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK; 

PubMed: 30050135     


ACY-1215 treatment inhibited PI3K/AKT/mTOR and ERK signaling protein levels in ESCC EC109 and TE-1 cell lines for 48 h.

Ac-β-catenin(K49) / p-β-catenin / β-catenin; 

PubMed: 25546293     


Time-course immunoblot analysis of human NPCs treated with an HDAC6 inhibitor. Human NPCs were treated with HDAC6 inhibitor ACY-1215 at 5 μM for the times points indicated and the lysates immunoblotted with antibodies against β-catenin, Ac-Lys49-β-catenin, phos-Ser45 and phos-Ser33, Ser37, and Thr41. β-actin is using shown as loading control.

31015208 30050135 25546293
Immunofluorescence
β-tubulin / β-catenin; 

PubMed: 25546293     


Immunofluorescence staining for β-catenin treated with HDAC6 inhibitor in human NPCs. Cells were treated with 5 μM ACY-1215 or DMSO for 18 h and imaged with anti-β-catenin antibody (green), anti-β-tubulin antibody (red), and Hoechst 33342 (blue). Scale bar, 20 μm.  Quantification of β-catenin levels at the membrane represent two independent experiments with three fields of view each at 20× magnification. Error bars indicate standard deviation. ** and **** denote significance at p < 0.01 and p < 0.0001, respectively (unpaired t test).

25546293
Growth inhibition assay
Cell viability; 

PubMed: 31015208     


Ricolinostat decreases MM cell viability. A panel of MM cell lines was treated with the indicated concentrations of ricolinostat for 72 hours. Cell viability was measured by MTT assay.

31015208
体内研究 ACY-1215与Bortezomib 联用,作用于两个浆细胞瘤模型和弥散性MM模型,抑制肿瘤生长,并延长生存,没有显著的不利影响。比单独使用具有更显著的抗MM 活性。ACY-1215易被肿瘤组织吸收。此外,药物不会在肿瘤组织中累积,处理24小时后,血液细胞和肿瘤组织的乙酰化的α-tubulin平行下降。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

HDAC 酶促实验:

ACY-1215在实验 Buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, 和20 μM三羧甲基磷酸(TCEP)] 中溶解,然后稀释到终浓度的6倍。HDAC酶在实验Buffer中稀释到终浓度的1.5倍,与ACY-1215预温育10分钟,然后加入底物。通过滴定曲线测定,用于每种酶的FTS(HDAC1,HDAC2,HDAC3和HDAC6)和MAZ-1675(HDAC4,HDAC5,HDAC7,HDAC8,和HDAC9)量等于米氏常数(Km)。使用0.3μM 测序等级胰蛋白酶将FTS或MAZ-1675在实验 Buffer中稀释到终浓度的6倍。底物/胰蛋白酶混合物添加到酶/化合物混合物中,实验板震荡60秒,然后置于SpectraMax M5酶标仪上。监测酶促反应中的7-氨基-4-甲氧基香豆素在30分钟内的释放,肽底物中赖氨酸侧链的脱乙酰化,计算反应的线性速率。
细胞实验:

[1]

- 合并
  • Cell lines: MM cell lines, patient MM cells, and PBMCs
  • Concentrations: ~8 μM
  • Incubation Time: 48 hours
  • Method:

    PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of ACY-1215. DNA synthesis is measured by tritiated thymidine uptake. CD4+T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3 × 104cells/well) are incubated in 96-well culture plates with medium and different concentrations of ACY-1215, bortezomib, and/or recombinant IL-6 (10 ng/mL) or insulin-like growth factor-1 (IGF-1; 50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: MM移植瘤SCID小鼠模型
  • Dosages: 50 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 86 mg/mL (198.38 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 433.5
化学式

C24H27N5O3

CAS号 1316214-52-4
储存条件 粉状
溶于溶剂
别名 Rocilinostat

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What would you suggest to obtain a clear solution?

  • 回答:

    S8001 ACY-1215 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 5 mg/ml clearly while it in 1% DMSO/30% polyethylene glycol/1% Tween 80 at 30 mg/ml is a suspension for oral administration. Please note that the precipitation will go out from the clear solution after stayed for about half an hour, So it is recommended to prepare the solution just before use.

HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID