Ricolinostat (ACY-1215)

目录号:S8001 别名: Rocilinostat

仅限科研使用

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。

Ricolinostat (ACY-1215)  Chemical Structure

CAS: 1316214-52-4

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 4664.38 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Ricolinostat (ACY-1215) 发表文献57篇:

产品安全说明书

HDAC抑制剂选择性比较

相关HDAC产品

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 NGf3R5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HjbVExyqCwTR?= NG\ON|gzPC92ODDo NV\VTlZPcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF3MEO0NEc,OjZzNUCzOFA9N2F-
U87MG NI\JVW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHsXo9mOTEEoH7N MonZNlQwPDhiaB?= NGnrNnJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NV;Oc5dGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOVA{PDBpPkK2NVUxOzRyPD;hQi=>
Hbl-1 MojFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrI[pQ6PDhiaB?= MYXJR|UxRTFwNjFOwG0> MnrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
OCI-Ly10 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWG0PEBp NFizSm1KSzVyPUCuPUDPxE1? NHTIUmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Riva MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrtPXNLPDhiaB?= M2DWRWlEPTB;Mj6yJO69VQ>? MonNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
Su-DHL2 NVPNVYNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkmwOFghcA>? NGTFN5lKSzVyPUOuN{DPxE1? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
OCI-Ly1 M3vtWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\ROFghcA>? NFrYOXVKSzVyPUKuOEDPxE1? NHnmc3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
OCI-Ly7 NGXSdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvTbIc1QCCq NWG0bFg2UUN3ME2xMlIh|ryP M3\pR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Su-DHL4 Mnz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXm0PEBp MmPCTWM2OD12Lkeg{txO M2PrblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Su-DHL6 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXK0PEBp NVXoWIJxUUN3ME2zMlIh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Hbl-2 Mk\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUSzN2Z[PDhiaB?= MmHUTWM2OD1zLkmg{txO NUXWVXl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Jeko-1 NG[xNo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPEOGtjPDhiaB?= MmTCTWM2OD1zLkWg{txO MojXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
Jvm-2 NYP4UHp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLW[pV[PDhiaB?= M4\JfWlEPTB;ND6wJO69VQ>? NXfpfYNVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Rec-1  NUDKUIJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TuXFQ5KGh? NWjHOIFSUUN3ME2yMlMh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
CCL-119 MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\XOFghcA>? MWXJR|UxRTFwNzFOwG0> M1P5OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
H9 M1j2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLiOFghcA>? NYLGZXVtUUN3ME2xMlIh|ryP NFOzOHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
HH M3rVRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[5c3drPDhiaB?= NGrT[4JKSzVyPUKuOUDPxE1? MlX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
Sup-T1 MlGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\xOFghcA>? MV\JR|UxRTFwNjFOwG0> M3rrdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
MM.1S MXjGeY5kfGmxbjDBd5NigQ>? MWSwMVXPxE1? NV;2PI9zPiCq NXPvbJFYcW6lcnXhd4V{KGGlZYT5cIF1\WRizsGteJVjfWyrbh?= NGjISJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
MM.1S MmfjSpVv[3Srb36gRZN{[Xl? MlHDNE4zPS9zzszN NYrjeVh4OThiaB?= M3HuRolv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
MM.1R M1TVbWZ2dmO2aX;uJGF{e2G7 NVXMVZVXOC5{NT:x{txO Mon4NVghcA>? MUPpcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv MoTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
RPMI8226  MY\GeY5kfGmxbjDBd5NigQ>? NHeweXIxNjJ3L{JOwG0> NW[3XXQyOThiaB?= NUHENJl{cW6lcnXhd4V{KGGlZYT5cIF1\WRizsGteJVjfWyrbh?= NFX5fZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
MM.1S M4\jfmNmdGxiVnnhZoltcXS7IFHzd4F6 MWCwMVjPxE1? NFrpU4c1QCCq M4jQOIRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHHFN4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
OPM1 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmLINE05|ryP NFzTSFc1QCCq Ml\o[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NXzKWJd6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
RPMI Ml;PR4VtdCCYaXHibYxqfHliQYPzZZk> NWq4NW9xOC16zszN NYX2[GFtPDhiaB?= NXTTbIpC\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHjONmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
MM.1R Mn[4R4VtdCCYaXHibYxqfHliQYPzZZk> MVSwMVjPxE1? NX7LWINEPDhiaB?= NYLHdFh4\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NV;pWFNYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
LR5 M3XOfWNmdGxiVnnhZoltcXS7IFHzd4F6 MYqwMVjPxE1? MnzyOFghcA>? NUfP[3o{\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
OPM2 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH\pTGMxNTkQvF2= MnzoOFghcA>? MkjX[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHTzdZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
Sf9 Mm\aSpVv[3Srb36gZZN{[Xl? NH60[o4yOCCvaX7z MonWTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDoeY1idiC{ZXPvcYJqdmGwdDDOMZRmem2rbnHsJGdUXC22YXfn[YQhUESDQ{[g[ZhxemW|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{BHXFNiYYOgd5Vje3S{YYTlJJBz\WmwY4XiZZRm\CCob4KgNVAhdWmwczDmc4xtd3enZDDifUB{fWK|dILheIUh[WSmaYTpc44hdWWjc4Xy[YQhd3[ncjCzNEBucW6|LDDJR|UxKD1iMD6wNFQ4KM7:TT6= NFPhO449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECzPFMzPCd-MkiwN|g{OjR:L3G+
Sf9 M3;GW2Z2dmO2aX;uJIF{e2G7 MYqxOUBucW6| M2njNGlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBIW1RvdHHn[4VlKEiGQVO2JIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDz[lkh[2WubIOgeZNqdmdiQn;jMWx6ey1qQXOpMWFOSyCjczDzeYJ{fHKjdHWgdJJmcW6ldXLheIVlKG[xcjCxOUBucW6|IH\vcIxwf2WmIHL5JJN2[nO2cnH0[UBi\GSrdHnvckBu\WG|dYLl[EBi\nSncjC2NEBucW6|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFAvODB7IN88UU4> NGm0[pY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWwNFE{OCd-Mkm1NFAyOzB:L3G+
Sf9 Mn[4SpVv[3Srb36gZZN{[Xl? NWLZd2dUOTVibXnudy=> M{nqU2lvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gR{11\XKvaX7hcEBJcXNvdHHn[4VlKEiGQVOzM24ufGW{bXnuZYwhT1OWLYTh[4dm\CCQQ1;SNkApOzl3IITvJFQ5QSC{ZYPp[JVmeyliZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKHOoOTDj[YxteyC3c3nu[{BDd2NvTInzMUhC[ylvQV3DJIF{KHO3YoP0doF1\SCycnXpcoN2[mG2ZXSg[o9zKDF3IH3pcpMh\m:ubH;3[YQh[nlic4Xid5Rz[XSnIHHk[Il1cSxiSVO1NEA:KDBwMEO3JO69VS5? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVyMEGzNEc,Ojl3MECxN|A9N2F-
Sf9 MoDiSpVv[3Srb36gZZN{[Xl? MUWxNEBucW6| MYXJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIHj1cYFvKHKnY3;tZolv[W62IFOteIVzdWmwYXygSmxCTy22YXfn[YQhUESDQ{Kg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{BHXFNiYYOgd5Vje3S{YYTlJJBz\WmwY4XiZZRm\CCob4KgNVAhdWmwczDmc4xtd3enZDDifUB{fWK|dILheIUh[WSmaYTpc44hdWWjc4Xy[YQhd3[ncjCzNEBucW6|LDDJR|UxKD1iMD6wOFgh|ryPLh?= MnK0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{izNlQoRjJ6MEO4N|I1RC:jPh?=
Sf9 NXnDdmdWTnWwY4Tpc44h[XO|YYm= MXGxNEBucW6| MnroTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDoeY1idiC{ZXPvcYJqdmGwdDDDMZRmem2rbnHsJGZNSUdvSHnzMZRi\2enZDDISGFEOSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJV{cW6pIF\UV{BieyC|dXLzeJJifGVicILlbY5kfWKjdHXkJIZweiBzMDDtbY5{KG[xbHzve4VlKGK7IIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDveoVzKDNyIH3pcpMtKEmFNUCgQUAxNjB3ODFOwG0v MlKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{izNlQoRjJ6MEO4N|I1RC:jPh?=
Sf9 Mle2SpVv[3Srb36gZZN{[Xl? MX6xOUBucW6| NXi2THNCUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBENXSncn3pcoFtKEircz30ZYdo\WRiSFTBR|Ih\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnQSClZXzsd{B2e2mwZzDCc4MuVHm|LTjBZ{kuSU2FIHHzJJN2[nO2cnH0[UBxemWrbnP1ZoF1\WRiZn;yJFE2KG2rboOg[o9tdG:5ZXSgZpkhe3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFYxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwJF0hOC5yNk[g{txONg>? MkD3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MECxN|AoRjJ7NUCwNVMxRC:jPh?=
Sf9 Ml\NSpVv[3Srb36gZZN{[Xl? NVjzdodMOTVibXnudy=> MUDJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIFOteIVzdWmwYXygSmxCTy:KaYOteIFo\2WmIFjERWMyKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EB{\jliY3XscJMhfXOrbnegRo9kNUy7cz2oRYMqNUGPQzDhd{B{fWK|dILheIUheHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkA3OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDhd5MtKEmFNUCgQUAxNjFizszNMi=> NFLvW3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWwNFE{OCd-Mkm1NFAyOzB:L3G+
BCP-ALL MWfDfZRwfG:6aXPpeJkh[XO|YYm= M3HTdVczKGi{cx?= MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCR3AuSUyOIHPlcIx{KGSncnn2[YQh\nKxbTDwZZRq\W62IEGgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlI6KM7:TT6= NW[yO3hnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN|Y2QDl{PD;hQi=>
BCP-ALL MoXFR5l1d3SxeHnjbZR6KGG|c3H5 NUnI[YtiPzJiaILz MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCR3AuSUyOIHPlcIx{KGSncnn2[YQh\nKxbTDwZZRq\W62IESgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlU1KM7:TT6= NHO1VI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
BCP-ALL M{D3[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MnXGO|IhcHK| NGXHZolEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDS1BvQVzMJINmdGy|IHTldol3\WRiZoLvcUBx[XSrZX70JFIh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjV6IN88UU4> M17JelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
RPMI8226 M2HtOmN6fG:2b4jpZ4l1gSCjc4PhfS=> MX[3NkBpenN? MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS52Nkig{txONg>? NXfremdjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0OFMxPzhpPkK2OFQ{ODd6PD;hQi=>
SEM M3vXbmN6fG:2b4jpZ4l1gSCjc4PhfS=> NXXzUG97PzJiaILz NWfTfpBbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0WPIHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOS54MTFOwG0v M2nBSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
SUP-B15 NEjpUWNEgXSxdH;4bYNqfHliYYPzZZk> Mm\OO|IhcHK| NET4SIxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXVBvQkG1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMT65NkDPxE1w M{jrUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
RPMI18226 NGPBelhEgXSxdH;4bYNqfHliYYPzZZk> MonxO|IhcHK| NGfiR4REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTWE2LMUiyNlYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCxMlk4KM7:TT6= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
HL60 NHG1VW5EgXSxdH;4bYNqfHliYYPzZZk> NW\s[ZRkPzJiaILz NV3TO5BGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDJwM{[g{txONg>? NH;3bpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
HL60 MnLHRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MYS0PEBpenN? M{PnWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB2ODDodpMhcW5icILld4Vv[2Vib3[gTmFMOiCrbnjpZol1d3JiQ2nUMVM5PyCkeTDDR2suQCCjc4PhfUwhUUN3MDC9JFIvPTRizszNMi=> MmDaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NECxNVUoRjJ7OUSwNVE2RC:jPh?=
K562 MX\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVO0PEBpenN? NUnnSndnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IES4JIhzeyCrbjDwdoV{\W6lZTDv[kBLSUt{IHnubIljcXSxcjDDXXQuOzh5IHL5JGNEUy16IHHzd4F6NCCLQ{WwJF0hOi53NDFOwG0v M2DhOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwNVE2Lz5{OUm0NFEyPTxxYU6=
HEL NI\XdpVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3f3XVQ5KGi{cx?= Mmm4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKRVygZ4VtdHNiYX\0[ZIhPDhiaILzJIlvKHC{ZYPlcoNmKG:oIFrBT|IhcW6qaXLpeI9zKEO\VD2zPFch[nliQ1PLMVgh[XO|YYmsJGlEPTBiPTCyMlU1KM7:TT6= Mn7SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NECxNVUoRjJ7OUSwNVE2RC:jPh?=
KCL22 MYLDfZRwfG:6aXPpeJkh[XO|YYm= MlnKO|IhcHK| M4\C[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGmvYYTpcoljNXKnc3nzeIFvfCCqdX3hckBMS0x{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDNwM{ig{txONg>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
U266 MlO0R5l1d3SxeHnjbZR6KGG|c3H5 NF;GdnE4OiCqcoO= M3iwb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHUzPjZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA{NjV{IN88UU4> M3XWc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
SUP-B15 MXTDfZRwfG:6aXPpeJkh[XO|YYm= MnrjO|IhcHK| MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBqdWG2aX7pZk1z\XOrc4ThcpQhcHWvYX6gV3VRNUJzNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDNwNUSg{txONg>? M1f4UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
KCL22 MYnDfZRwfG:6aXPpeJkh[XO|YYm= MlLOO|IhcHK| NVnkT|IzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0OOMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB|Lke1JO69VS5? NH7yTXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
HL60 NFXye3RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MWe0PEBpenN? MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR|UxKD1iMz63OUDPxE1w NYTGW4IzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFAyOTVpPkK5PVQxOTF3PD;hQi=>
K562 M2nPV2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MoTrOFghcHK| NGfm[YVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT{05KGG|c3H5MEBKSzVyIE2gN{44PSEQvF2u NHHFb3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
HEL NV\s[pd2SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Ml3VOFghcHK| MomwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKRVygZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR|UxKD1iMz63OUDPxE1w NG\tPZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
BCP-ALL MlHIR5l1d3SxeHnjbZR6KGG|c3H5 NWH5PZBRPzJiaILz M{HTVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJEWC2DTFygZ4VtdHNiZHXybZZm\CCocn;tJJBifGmnboSgN{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQvPDVizszNMi=> MkPhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
MV4-11 MnXvSpVv[3Srb36gZZN{[Xl? MofFNVAxOCCwTR?= M{i0VlYhcHK| Ml3pTY5pcWKrdHnvckBw\iCKRFHDNU8zNzNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBpcXO2b37lJGg{KGGlZYT5cIF1cW:wIHH0JFExODBibl2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz Mom0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEOwO|goRjJ4NESzNFc5RC:jPh?=
TC32 NIPJPYhyUFSVIHHzd4F6 M2XDRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| M{HafVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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SJ-GBM2 NI\mfm9yUFSVIHHzd4F6 MmLIdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 MoD5dWhVWyCjc4PhfS=> MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NF;NOms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MnfGdWhVWyCjc4PhfS=> M3zoVpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NUO5OXByRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 NH7i[IFyUFSVIHHzd4F6 MnLndWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| MoH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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Assay
Methods Test Index PMID
Western blot Ac-α-tubulin / Ac-Histone H4 Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1 Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK Ac-β-catenin(K49) / p-β-catenin / β-catenin 31015208 30050135 25546293
Immunofluorescence β-tubulin / β-catenin 25546293
Growth inhibition assay Cell viability 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]

  • 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]

  • 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.

动物实验:

[1]

  • Animal Models: MM移植瘤SCID小鼠模型
  • Dosages: 50 mg/kg
  • Administration: 腹腔注射

溶解度(25°C)

体外

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):
5% DMSO+ 40% PEG 300+ 5% Tween 80+ 50% ddH2O

0.62mg/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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02632071 Completed Drug: ACY-1215|Drug: Nab-paclitaxel Metastatic Breast Cancer|Breast Carcinoma Columbia University|Acetylon Pharmaceuticals Incorporated|National Cancer Institute (NCI) March 1 2016 Phase 1
NCT01583283 Active not recruiting Drug: ACY-1215|Drug: lenalidomide|Drug: Dexamethasone Multiple Myeloma Celgene July 12 2012 Phase 1|Phase 2
NCT01323751 Completed Drug: ACY-1215 Multiple Myeloma Celgene|The Leukemia and Lymphoma Society July 2011 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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.