Daporinad

目录号:S2799 别名: FK866, APO866

仅限科研使用

Daporinad (FK866, APO866)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase; Nampt),Daporinad (FK866, APO866) 可引发自噬,无细胞试验中IC50为0.09 nM。Phase 1/2。

Daporinad  Chemical Structure

CAS: 658084-64-1

规格 价格 库存 购买数量
RMB 737.65 现货
RMB 3025.95 现货
RMB 4662.84 现货
大包装 有超大折扣

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Daporinad 发表文献50篇:

产品安全说明书

Transferase抑制剂选择性比较

生物活性

产品描述 Daporinad (FK866, APO866)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase; Nampt),Daporinad (FK866, APO866) 可引发自噬,无细胞试验中IC50为0.09 nM。Phase 1/2。
靶点
NMPRTase [5]
(Cell-free assay)
0.4 nM(Ki)
体外研究

APO866在0.09-27 nM的低浓度范围内会在41血液恶性肿瘤细胞中诱导产生细胞毒性,包括急性髓细胞白血病[AML],急性淋巴细胞白血病 [ALL], 套细胞淋巴瘤[MCL], 慢性淋巴细胞白血病[CLL]和 T细胞淋巴瘤,这种毒性具有剂量依赖特性. APO866在0-10 nM的低浓度范围内会诱导细胞死亡,这一效果与线粒体膜去极化有关而与半胱天冬酶的激活无关。APO866在0-10 nM的浓度范围内会诱导胞内NAD 和 ATP 的损耗和多种血液肿瘤细胞的死亡,这一效果具有剂量依赖特性[1] 。10 nM APO866 会抑制HFFF2细胞内 PBEF诱导的 MMP-3, CCL2和CXCL8 的分泌 [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y MX3DfZRwfG:6aXPpeJkh[XO|YYm= NE[4[5JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iC2b4ThcEBk\WyudXzhdkBPSURqUDmgcIV3\WxuIFnDOVAhRSByLkCwNFUh|ryPLh?= NITXZ5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm2NVE5Oyd-MUm5OlEyQDN:L3G+
SH-SY5Y MVLDfZRwfG:6aXPpeJkh[XO|YYm= MUC0PEBpenN? MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjByMUeg{txONg>? NYrzN3RxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OlEyQDNpPkG5PVYyOTh|PD;hQi=>
HT1080 NYrVZnBJS3m2b4TvfIlkcXS7IHHzd4F6 MXe2JIRigXN? MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWFExQDBiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=> NH75WWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzNFAyPSd-MkGzN|AxOTV:L3G+
A549 NVuzblNFS3m2b4TvfIlkcXS7IHHzd4F6 MmHVOkBl[Xm| MkfXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE4yPiEQvF2u M3jBVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
HCT116 MnG4R5l1d3SxeHnjbZR6KGG|c3H5 M17SclYh\GG7cx?= MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=> NUDhemZ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|AxOTVpPkKxN|MxODF3PD;hQi=>
SNU638 MmLOR5l1d3SxeHnjbZR6KGG|c3H5 MYC2JIRigXN? NXTTdnBQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06XNkO4JINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkG2JO69VS5? M2DXT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
MCF7 NVHwXJN3SW62aYT1cY9zKGG|c3H5 NEfuO4EyOCC3TR?= M17BOVYh\GG7cx?= NUTGT5pbSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BifCBzMDD1UUBi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE43QCEQvF2u M{fEe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
K562 NX[1b3ZmS3m2b4TvfIlkcXS7IHHzd4F6 NXfUbI9PPiCmYYnz NVvuZVlMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOjBizszNMi=> MnPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
A2780 MWLDfZRwfG:6aXPpeJkh[XO|YYm= NVLpOnM2PzJiaILz MnnQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvODBzIN88UU4> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzN{e4OEc,OjN4MUe3PFQ9N2F-
NYH M2XoU2N6fG:2b4jpZ4l1gSCjc4PhfS=> MWKzJJdm\Wu| NWTpPZdiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVlmKIHPlcIx{KGGodHXyJFMhf2Wna4OgZpkh[2yxbn;n[Y5q[yC|dYL2bZZidCCjc4PhfUwhVER3MDC9JFAvODBzNTFOwG0v MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5OUmxOUc,OjN4N{m5NVU9N2F-
K562 M{n3UmN6fG:2b4jpZ4l1gSCjc4PhfS=> MYW5OkBpenN? M2POOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvODB5MjFOwG0v M2PrUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke5PVE2Lz5{M{[3PVkyPTxxYU6=
A2780 NULSUJV3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MWe3NkBpenN? NUXpSWZrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhW1KELXLhd4VlKG2rY4LvdIxifGVicnXh[IVzKGGwYXz5d4l{NCCLQ{WwJF0hOC5yMEGg{txONg>? MmGzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUmxNVgoRjJ|OEW5NVE5RC:jPh?=
NYH NVfienRDS3m2b4TvfIlkcXS7IHHzd4F6 MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3MDC9JFAvODBzNTFOwG0v MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A2780 MUnDfZRwfG:6aXPpeJkh[XO|YYm= MmDGO|IhcHK| MljGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD6wNFE3KM7:TT6= NYDPU3oyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
HepG2 M1q3V2Z2dmO2aX;uJIF{e2G7 NHPVblkyKGi{ NFjpbHZKdmirYnn0bY9vKG:oIF7BUXBVKGmwIHj1cYFvKEincFeyJINmdGy|IIXzbY5oKFtzNFPdMY5q[2:2aX7hcYll\S:SUmDQJIF{KHO3YoP0doF1\SCjc4Pld5Nm\CCjczDmc5Ju[XSrb36gc4YhYzF2Q22tcolkd3SrbnHtbYRmKG2xbn;ueYNt\W:2aXTlJIFnfGW{IEGgbJIh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYOsJGlEPTBiPTCwMlAxOjJizszNMi=> MkL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
PC3 MoLsR5l1d3SxeHnjbZR6KGG|c3H5 NEfHWoVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NEA:KDBwMECzPEDPxE1w NGTMPGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
A2780 NXT1SYk{S3m2b4TvfIlkcXS7IHHzd4F6 NWO5UXNES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OCB;IECuNFA2PyEQvF2u MoDNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A431 NH7FTnpEgXSxdH;4bYNqfHliYYPzZZk> NVSwOplMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR|MTDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7LDDJR|UxKD1iMD6wNFYyKM7:TT6= NF\ycYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
MCF-7 NWHTWlVIS3m2b4TvfIlkcXS7IHHzd4F6 NGjLVnM4OiCqcoO= MkS0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHNTdiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD6wNFc1KM7:TT6= NV;MS5RVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
MCF7 MV;DfZRwfG:6aXPpeJkh[XO|YYm= M1Wy[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NEA:KDBwMEC4OEDPxE1w M3j4dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HCT116 MmT0R5l1d3SxeHnjbZR6KGG|c3H5 MmLGO|IhcHK| MkXPR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OCB;IECuNFExQSEQvF2u NV7sXldnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
SKOV3 M2\HRWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2HaTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkKxNUDPxE1w MlfyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
HCT116 MWTDfZRwfG:6aXPpeJkh[XO|YYm= NUO0fmxGPzJiaILz MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBCWE96Nk[tdoV{cXO2YX70JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVAhRSByLkm0OkDPxE1w NVPtRWVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
A2780 MY\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Ml22O|IhcHK| NX7iXm5kSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NEA:KDBwMECxJO69VS5? NVyzNGVDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU1OTlpPkK0OFA2PDF7PD;hQi=>
A2780 NIXHO3ZHfW6ldHnvckBie3OjeR?= NEnP[lU4OiCqcoO= NGrtSIRKdmirYnn0bY9vKG:oIF7BUXBVKGmwIHj1cYFvKEF{N{iwJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlAxOSEQvF2u MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUK3NUc,Ojd3NEGyO|E9N2F-
DE3 M33U[mZ2dmO2aX;uJIF{e2G7 NFfCfIYyPSCvaX7z M33pU2lvcGmkaYTpc44hd2ZiaIXtZY4h\nWubDDs[Y5ofGhiQz30[ZJucW6jbDDIbZM3NXSjZ3fl[EBPSU2SVDDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBTd3OndIThJEhFTTNrIHPlcIx{KHW|aX7nJI5q[2:2aX7hcYll\SCjczDzeYJ{fHKjdHWgbY5kfWKjdHXkJIZweiBzNTDtbY5{KHC{aX;yJJRwKHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkA{OCCvaX7zJIlvKHC{ZYPlcoNmKG:oIGDSVHAtKEmFNUCgQUAxNjByMzFOwG0v M{D2OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxNlcyLz5{N{W0NVI4OTxxYU6=
SH-SY5Y MmL6R5l1d3SxeHnjbZR6KGG|c3H5 MXO1OkBpenN? Ml[xR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiNU[gbJJ{KGK7IF3UWEBie3OjeTygSWM2OCB;IECuNFA{PCEQvF2u NFP1fIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG2OVc1Oid-MkixOlU4PDJ:L3G+
A2780 MVXDfZRwfG:6aXPpeJkh[XO|YYm= MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHluIFnDOVAhRSByLkCwOFIh|ryPLh?= MmG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNkW3OFIoRjJ6MU[1O|QzRC:jPh?=
PC3 MVTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NXGyTGxvPSCmYYnz M4jlcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBqdmO3YnH0[YQh\m:{IEWg[IF6eyCkeTDD[YxtNXSrdHXyJGdtdyC{ZXHn[Y51KGKjc3XkJIF{e2G7LDDJR|UxKD1iMD6wNFU4KM7:TT6= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZzMEm4OEc,Ojh4MUC5PFQ9N2F-
HepG2 NHjndJJEgXSxdH;4bYNqfHliYYPzZZk> M2fLeVczKGi{cx?= MVTDfZRwfG:6aXPpeJkhcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlg6KM7:TT6= NXTte|lvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4PFU5OzRpPkK4PFg2QDN2PD;hQi=>
MDA-MB-231 MoHBR5l1d3SxeHnjbZR6KGG|c3H5 MX23NkBpenN? NXm2T3BES3m2b4TvfIlkcXS7IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxMlMh|ryPLh?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh6NUizOEc,Ojh6OEW4N|Q9N2F-
HCT116 NYDlUVBnS3m2b4TvfIlkcXS7IHHzd4F6 M2DPUFczKGi{cx?= MmrPR5l1d3SxeHnjbZR6KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEvPiEQvF2u NVLwNVVURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4PFU5OzRpPkK4PFg2QDN2PD;hQi=>
HepG2 M4C3SWN6fG:2b4jpZ4l1gSCjc4PhfS=> NHvlcGE4OiCqcoO= NHywbldEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLki5JO69VS5? Mn\6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl|NEi4NFgoRjJ7M{S4PFA5RC:jPh?=
HCT116 NGXxcJdEgXSxdH;4bYNqfHliYYPzZZk> NUDFRXN2PzJiaILz MlvSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFwNjFOwG0v NIXPcZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUO0PFgxQCd-MkmzOFg5ODh:L3G+
A549 NE\wUmtEgXSxdH;4bYNqfHliYYPzZZk> NVnDNVJ5PzJiaILz MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFMvPyEQvF2u NH\zUVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUO0PFgxQCd-MkmzOFg5ODh:L3G+
SH-SY5Y M3;ke2F2fG:yaHHnfUBie3OjeR?= M33LRlQxKGi{cx?= NEK1VYpKdmS3Y4Tpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[XO|ZYPz[YQh[XNiTFOzM5Bpd3OyaH;0bYR6dGW2aHHuc4xidWmwZTDjc5VxdGmwZzDh[pRmeiB2MDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NYjCZ2IyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OlEyQDNpPkG5PVYyOTh|PD;hQi=>
MCF7 M375bmFvfGm2dX3vdkBie3OjeR?= MkL5OkBl[Xm| M{HKe2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNjDkZZl{KGK7IGPSRkBie3OjeR?= NYLuVnRyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|AxOTVpPkKxN|MxODF3PD;hQi=>
MDCK MV3GeY5kfGmxbjDhd5NigQ>? NHzqS|gyOCC3TR?= MmPlRZBx[XKnboSgdIVzdWWjYnnsbZR6KGGlcn;zd{BieGmlYXygeI8h[mG|b3zheIVz[Wxic3nk[UBqdiCmb3egUWREUyClZXzsd{BifCBzMDD1UUBjgSCOQz3NV{9OWyCjbnHsfZNqew>? NXXxW2RMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVkyOThpPkKzPFU6OTF6PD;hQi=>
DU145 NYrNTXZFS3m2b4TvfIlkcXS7IHHzd4F6 NIfibJpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7 M1v0flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
MCF7 MmewR5l1d3SxeHnjbZR6KGG|c3H5 MVK5OkBpenN? NF65OIlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFk3KGi{czDifUBkdG:wb3flcolkKGG|c3H5 MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
HCT116 M{fTVmZ2dmO2aX;uJIF{e2G7 NIPTd41T\XOrc4ThcoNmKG[jY4TvdkwhemG2aX:gc4YhUUN3MDDmc5IhSVCROE[2MZJme2m|dHHueEBpfW2jbjDIR3QyOTZiY3XscJMhfG9iSVO1NEBnd3JiaIXtZY4hUEOWMUG2JINmdGy| M2XjOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
A2780 NV7hdnRTSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mmm0O|IhcHK| NVLvXFlbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSCrbjDwdoV{\W6lZTDv[kBvcWOxdHnuZY1q\GVibX;uc452[2ynb4Tp[IU> M2PHXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1OFE6Lz5{NESwOVQyQTxxYU6=
Sf9 NGf0Z4FHfW6ldHnvckBie3OjeR?= NUSwTWNLOzBibXnudy=> M{DJcGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSg[pVtdCCuZX7neIghcHWvYX6gR{11\XKvaX7hcEBJcXNxZnzh[{11[WepZXSgTGRCSzFiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKFOoOTDpcpNm[3RiY3XscJMh[W[2ZYKgN|AhdWmwczDifUBndHWxcnXzZ4Vv[2ViYYPzZZk> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN2OEiwPEc,Ojl|NEi4NFg9N2F-
Assay
Methods Test Index PMID
Western blot SIRT1 p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1 AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448) 29905535 29541451 26542945
Immunofluorescence pMLKL phGSK3β ph-β-catenin 29996103 22207684
Growth inhibition assay Cell viability 27462772
体内研究 用C.B.-17 SCID 小鼠建立人急性髓细胞白血病,淋巴母细胞淋巴瘤和白血病的异种移植模型,腹腔注射APO866 ,一天两次,一次20 mg/kg 一周4天, 重复三周以上可以抑制肿瘤生长。 [1]对于携带CIA的小鼠, 0.12 mg/kg/小时剂量的 APO866 可以通过抑制PBEF 来防止关节破坏和白细胞浸润[2]

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)

细胞实验:

[1]

  • Cell lines: 41血液恶性肿瘤细胞系
  • Concentrations: 0 - 10 nM
  • Incubation Time: 72 小时或 96小时
  • Method:

    MTT 分析流程, 细胞按每毫升0.5 &time 106 个的密度接种到96孔板,接种三份。将APO866 (0.01 nM-100 nM) 加到50 μL 培养基中, 空白培养基作为对照。 孵育 72或 96 小时后每孔加入15 μL 染料溶液继续孵育 4 小时。 然后每孔加入100 μL 终止液孵育 1小时,用分光光度计测量570 nm 处吸光度。台盼蓝染色分析流程, 细胞按每孔0.5 &time105 个接种到6孔板,每孔加入1 mL培养基,在含有或缺少 APO866的情况下孵育 96 小时。 每孔取10μL 细胞样品与10 μL 台盼蓝孵育1分钟(体积比1:1)。细胞存活情况通过计算未染色的细胞个数来获得。

动物实验:

[1]

  • Animal Models: 人急性髓细胞白血病,淋巴瘤以及白血病的C.B.-17 SCID 小鼠异种移植模型
  • Dosages: 20 mg/kg
  • Administration: 腹腔注射一天两次,连续四天,重复3周以上

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

4mg/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 391.51
化学式

C24H29N3O2

CAS号 658084-64-1
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
NCT00435084 Completed Drug: APO866 B-cell Chronic Lymphocytic Leukemia Onxeo February 2007 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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常见问题及建议解决方法

问题 1:
We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?

回答:
The vehicle we recommend for S2799 in vivo study is 45% Propylene glycol (dissolve first) +5% Tween 80+ddH2O. You can dissolve the compound in Propylene glycol first and then dilute with water with Tween 80. The solution is clear and can be used for injection.

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