Daporinad (FK866, APO866)

For research use only. Not for use in humans.

目录号：S2799

Daporinad (FK866, APO866) Chemical Structure

CAS No. 658084-64-1

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。

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客户使用Selleck生产的Daporinad (FK866, APO866)发表文献31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 MnfqR5l1d3SxeHnjbZR6KGG|c3H5 MmrCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhfG:2YXygZ4VtdHWuYYKgUmFFMFBrIHzleoVtNCCLQ{WwJF0hOC5yMEC1JO69VS5? NV7xSmxiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OlEyQDNpPkG5PVYyOTh|PD;hQi=>
SH-SY5Y NUTGVGtpS3m2b4TvfIlkcXS7IHHzd4F6 NWK4SHNMPDhiaILz MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjByMUeg{txONg>? NIPENpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm2NVE5Oyd-MUm5OlEyQDN:L3G+
HT1080 M4PXcmN6fG:2b4jpZ4l1gSCjc4PhfS=> MVy2JIRigXN? NGD5c5hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXDFyOECgZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwMU[g{txONg>? NFXVVlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzNFAyPSd-MkGzN|AxOTV:L3G+
A549 NY\RUVYxS3m2b4TvfIlkcXS7IHHzd4F6 M{Dn[|Yh\GG7cx?= MkP2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE4yPiEQvF2u M{PZS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
HCT116 MoXyR5l1d3SxeHnjbZR6KGG|c3H5 M{f4dlYh\GG7cx?= MlzxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjF4IN88UU4> NIe3TFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzNFAyPSd-MkGzN|AxOTV:L3G+
SNU638 NHnNPZlEgXSxdH;4bYNqfHliYYPzZZk> NWTseWhWPiCmYYnz NXHjT5JiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06XNkO4JINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkG2JO69VS5? Mne3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
MCF7 M3n2ZWFvfGm2dX3vdkBie3OjeR?= MmXsNVAhfU1? NWDx[FF3PiCmYYnz MkS0RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDheEAyOCC3TTDh[pRmeiB4IHThfZMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD62PEDPxE1w NYfnUIhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|AxOTVpPkKxN|MxODF3PD;hQi=>
K562 NH36dIdEgXSxdH;4bYNqfHliYYPzZZk> NWHxe3BGPiCmYYnz MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCyNEDPxE1w NHm0RnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzNFAyPSd-MkGzN|AxOTV:L3G+
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NYH NWLuXo54S3m2b4TvfIlkcXS7IHHzd4F6 NXqyOJFFOyC5ZXXrdy=> NUPnXpQ1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVlmKIHPlcIx{KGGodHXyJFMhf2Wna4OgZpkh[2yxbn;n[Y5q[yC|dYL2bZZidCCjc4PhfUwhVER3MDC9JFAvODBzNTFOwG0v MmnoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4N{m5NVUoRjJ|Nke5PVE2RC:jPh?=
K562 M3P4bGN6fG:2b4jpZ4l1gSCjc4PhfS=> MkjjPVYhcHK| MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlAxPzJizszNMi=> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5OUmxOUc,OjN4N{m5NVU9N2F-
A2780 NX7ycowxSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYrJV4hHPzJiaILz M{HKWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JHNTSi2kYYPl[EBucWO{b4DsZZRmKHKnYXTldkBidmGueYPpd{whUUN3MDC9JFAvODBzIN88UU4> NEDqeJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1PVEyQCd-MkO4OVkyOTh:L3G+
NYH M1HZO2N6fG:2b4jpZ4l1gSCjc4PhfS=> MoHzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUnlJKGOnbHzzJIJ6KGOub37v[4VvcWNiYYPzZZktKEmFNUCgQUAxNjByMUWg{txONg>? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A2780 M3TZc2N6fG:2b4jpZ4l1gSCjc4PhfS=> MlyyO|IhcHK| MnrsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD6wNFE3KM7:TT6= MkTjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
HepG2 M2rnO2Z2dmO2aX;uJIF{e2G7 MXmxJIhz NXzUeWgzUW6qaXLpeIlwdiCxZjDORW1RXCCrbjDoeY1idiCKZYDHNkBk\WyuczD1d4lv\yCdMUTDYU1vcWOxdHnuZY1q\GVxUGLQVEBieyC|dXLzeJJifGViYYPz[ZN{\WRiYYOg[o9zdWG2aX;uJI9nKFtzNFPdMY5q[2:2aX7hcYll\SCvb37vcpVkdGWxdHnk[UBi\nSncjCxJIhzKGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nzMEBKSzVyIE2gNE4xODJ{IN88UU4> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
PC3 NHr2TYVEgXSxdH;4bYNqfHliYYPzZZk> M4rDWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwJF0hOC5yMEO4JO69VS5? Ml3QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780 M3jaUWN6fG:2b4jpZ4l1gSCjc4PhfS=> NUn4N4puS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OCB;IECuNFA2PyEQvF2u MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A431 MVLDfZRwfG:6aXPpeJkh[XO|YYm= MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIJ6KGOub37v[4VvcWNiYYPzZZktKEmFNUCgQUAxNjByNkGg{txONg>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
MCF-7 NHj2SWFEgXSxdH;4bYNqfHliYYPzZZk> NG\Y[Ik4OiCqcoO= MlTzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHNTdiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD6wNFc1KM7:TT6= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
MCF7 NXXUboU3S3m2b4TvfIlkcXS7IHHzd4F6 MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KGOub37v[4VvcWNiYYPzZZktKEmFNUCgQUAxNjByOESg{txONg>? NV\jUoJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
HCT116 MmrTR5l1d3SxeHnjbZR6KGG|c3H5 NXrLV5hRPzJiaILz M{GzTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTBiPTCwMlAyODlizszNMi=> NHHoc3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
SKOV3 M{jVeGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{LZcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkKxNUDPxE1w M{TpRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HCT116 MXPDfZRwfG:6aXPpeJkh[XO|YYm= MlLjO|IhcHK| MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBCWE96Nk[tdoV{cXO2YX70JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVAhRSByLkm0OkDPxE1w NVzy[JFIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
A2780 MWLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M3fqbVczKGi{cx?= M33hSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEmFNUCgQUAxNjByMTFOwG0v MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUSxPUc,OjR2MEW0NVk9N2F-
A2780 M4Lw[2Z2dmO2aX;uJIF{e2G7 M{\TdFczKGi{cx?= MoewTY5pcWKrdHnvckBw\iCQQV3QWEBqdiCqdX3hckBCOjd6MDDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD6wNFEh|ryPLh?= NF6yU5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVI4OSd-Mke1OFEzPzF:L3G+
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SH-SY5Y MonsR5l1d3SxeHnjbZR6KGG|c3H5 MoG5OVYhcHK| NGDXW3JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC1OkBpenNiYomgUXRVKGG|c3H5MEBGSzVyIE2gNE4xODN2IN88UU4> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF4NUe0Nkc,OjhzNkW3OFI9N2F-
A2780 MXnDfZRwfG:6aXPpeJkh[XO|YYm= NVHWcHhiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5MEBKSzVyIE2gNE4xODR{IN88UU4> MlTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNkW3OFIoRjJ6MU[1O|QzRC:jPh?=
PC3 NWfOTpFDSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NXrWNmxGPSCmYYnz NG\HfGdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC1JIRigXNiYomgR4VtdC22aYTldkBIdG9icnXh[4VvfCCkYYPl[EBie3OjeTygTWM2OCB;IECuNFA2PyEQvF2u Mni1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4MUC5PFQoRjJ6NkGwPVg1RC:jPh?=
HepG2 M2XXVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NX7jSpJHPzJiaILz MnTxR5l1d3SxeHnjbZR6KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE45QSEQvF2u M1\P[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEi1PFM1Lz5{OEi4OVg{PDxxYU6=
MDA-MB-231 M4K3c2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYK3NkBpenN? MkLuR5l1d3SxeHnjbZR6KGmwIHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkOg{txONg>? M3jyVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEi1PFM1Lz5{OEi4OVg{PDxxYU6=
HCT116 NXXROpJKS3m2b4TvfIlkcXS7IHHzd4F6 MXq3NkBpenN? MVXDfZRwfG:6aXPpeJkhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNU43KM7:TT6= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh6NUizOEc,Ojh6OEW4N|Q9N2F-
HepG2 NEfkTHpEgXSxdH;4bYNqfHliYYPzZZk> NIexW4M4OiCqcoO= MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjh7IN88UU4> NInXcFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUO0PFgxQCd-MkmzOFg5ODh:L3G+
HCT116 NHu4VnhEgXSxdH;4bYNqfHliYYPzZZk> MmfXO|IhcHK| MnH3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFwNjFOwG0v M2WxV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{S4PFA5Lz5{OUO0PFgxQDxxYU6=
A549 MVLDfZRwfG:6aXPpeJkh[XO|YYm= Mkj2O|IhcHK| MoK0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA{NjdizszNMi=> NHX2TWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUO0PFgxQCd-MkmzOFg5ODh:L3G+
SH-SY5Y MorURZV1d3CqYXf5JIF{e2G7 M3r4bVQxKGi{cx?= MWLJcoR2[3Srb36gc4Yh[XW2b4DoZYd6KGmwIHj1cYFvKFOKLWPZOXkh[2WubIOgZZN{\XO|ZXSgZZMhVEN|L4Doc5NxcG:2aXT5cIV1cGGwb3zhcYlv\SClb4XwcIlv\yCjZoTldkA1OCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| Ml\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7NkGxPFMoRjF7OU[xNVg{RC:jPh?=
MCF7 NV:1T25WSW62aYT1cY9zKGG|c3H5 Ml\tOkBl[Xm| NIPTV|dCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO|YYm= MnTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
MDCK M4THfGZ2dmO2aX;uJIF{e2G7 MWexNEB2VQ>? M1nB[WFxeGG{ZX70JJBmem2nYXLpcIl1gSCjY4Lvd5Mh[XCrY3HsJJRwKGKjc3;sZZRmemGuIIPp[IUhcW5iZH;nJG1FS0tiY3XscJMh[XRiMUCgeW0h[nliTFOtUXMwVVNiYX7hcJl{cXN? NFzzZY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1PVEyQCd-MkO4OVkyOTh:L3G+
DU145 MVPDfZRwfG:6aXPpeJkh[XO|YYm= MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6 M2THbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
MCF7 M3fYcmN6fG:2b4jpZ4l1gSCjc4PhfS=> NXLBZZQ4QTZiaILz M{jNU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JINtd26xZ3XubYMh[XO|YYm= NUfyR41vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
HCT116 NGLVbXpHfW6ldHnvckBie3OjeR?= NEO5ZXBT\XOrc4ThcoNmKG[jY4TvdkwhemG2aX:gc4YhUUN3MDDmc5IhSVCROE[2MZJme2m|dHHueEBpfW2jbjDIR3QyOTZiY3XscJMhfG9iSVO1NEBnd3JiaIXtZY4hUEOWMUG2JINmdGy| Mn\sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780 NXXWZ3VCSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MYS3NkBpenN? NGXhbZhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJI5q[2:2aX7hcYll\SCvb37vcpVkdGWxdHnk[S=> NVfRWFRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU1OTlpPkK0OFA2PDF7PD;hQi=>
Sf9 M1\COGZ2dmO2aX;uJIF{e2G7 MnW0N|AhdWmwcx?= MWDJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IH\1cIwhdGWwZ4ToJIh2dWGwIFOteIVzdWmwYXygTIl{N2[uYXeteIFo\2WmIFjERWMyKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJIFnfGW{IEOwJI1qdnNiYomg[ox2d3Knc3PlcoNmKGG|c3H5 NHmwOnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUO0PFgxQCd-MkmzOFg5ODh:L3G+

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
SIRT1; 

PubMed: 29905535     


Human retinal pigment epithelial cells (ARPE-19) were treated with different doses (0.01-10μM) of FK866 and expression of SIRT1 was evaluated by western blotting.

p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1; 

PubMed: 29541451     


CEM PA cells were treated with 5 and 100 nM FK866 for 48 h. Western blot showing expression of AMPK, mTOR, 4EBP1, and EIF2A in CEM PA cells.

AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448); 

PubMed: 26542945     


Jurkat cells were treated for 48 h with or without (Mock) the indicated concentration of FK866. Thereafter, cells were lysed and the levels of total and p-Akt (Ser-473), total and p-MTOR (Ser-2448), total and p-4EBP1 (Ser-65 and Thr-70).

29905535 29541451 26542945
Immunofluorescence
pMLKL; 

PubMed: 29996103     


Immunofluorescence for pMLKL (monoclonal pMLKL antibody, red, phospho S358) and nuclei (DAPI, blue) in THP-1 cells treated with the indicated concentrations of FK866 for 6 hr. Scale bars, 10 μm. 

phGSK3β; 

PubMed: 22207684     


Representative DUOLINK images of phospho-GSK3β (Ser9) protein expression in HL60 cells treated with 10 nM of FK866 for 96 h or 100 nM of AC93253 for 48 h, or with DMSO as a control.

ph-β-catenin ; 

PubMed: 22207684     


Representative images of inactive phospho-β-catenin (Ser33/37) protein expression in HL60 cells treated with 10 nM of FK866, 100 nM of AC93253 or DMSO as a control

29996103 22207684
Growth inhibition assay
Cell viability ; 

PubMed: 27462772     


Twenty-three PDAC-derived PCCs were treated for 72 h with increasing concentrations of FK866 ranging from 0 to 1000 nM. The horizontal dotted line indicates 50% cell viability. PCCs with the highest sensitivity are highlighted by a blue line and those wit䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ

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]
- 合并
  • 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。


    (Only for Reference)
动物实验：

[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 Ethanol 78 mg/mL (199.22 mM)
DMSO Insoluble
Water 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)：
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 粉状
溶于溶剂
别名 N/A

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 只
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：

    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.

Selleck产品目录册

Transferase Signaling Pathway Map
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID