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33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 MlixR5l1d3SxeHnjbZR6KGG|c3H5 M2[3WWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNJNVO\NWmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKHSxdHHsJINmdGy3bHHyJG5CTCiSKTDs[ZZmdCxiSVO1NEA:KDBwMECwOUDPxE1w NX3iPZhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OlEyQDNpPkG5PVYyOTh|PD;hQi=>
SH-SY5Y MlTlR5l1d3SxeHnjbZR6KGG|c3H5 NX23bIRIPDhiaILz NGqz[5FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkCwNVch|ryPLh?= NVjJNnFXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OlEyQDNpPkG5PVYyOTh|PD;hQi=>
HT1080 M1r0ZmN6fG:2b4jpZ4l1gSCjc4PhfS=> M{j2NVYh\GG7cx?= NFrBclREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXDFyOECgZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwMU[g{txONg>? NInmUWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzNFAyPSd-MkGzN|AxOTV:L3G+
A549 NUTJUXpKS3m2b4TvfIlkcXS7IHHzd4F6 MlnFOkBl[Xm| M{\GUGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=> MmTOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
HCT116 MkHiR5l1d3SxeHnjbZR6KGG|c3H5 M{nSelYh\GG7cx?= Ml[yR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjF4IN88UU4> M{DsOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
SNU638 MVLDfZRwfG:6aXPpeJkh[XO|YYm= MXy2JIRigXN? MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUnU3OzhiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
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NYH MVzDfZRwfG:6aXPpeJkh[XO|YYm= M3PrVmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5[UCClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwJF0hOC5yMEG1JO69VS5? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A2780 NHXkfnBEgXSxdH;4bYNqfHliYYPzZZk> MkHsO|IhcHK| MnfTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD6wNFE3KM7:TT6= M4nBeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HepG2 NYXwVINLTnWwY4Tpc44h[XO|YYm= NV3PWGZZOSCqch?= NELzUVJKdmirYnn0bY9vKG:oIF7BUXBVKGmwIHj1cYFvKEincFeyJINmdGy|IIXzbY5oKFtzNFPdMY5q[2:2aX7hcYll\S:SUmDQJIF{KHO3YoP0doF1\SCjc4Pld5Nm\CCjczDmc5Ju[XSrb36gc4YhYzF2Q22tcolkd3SrbnHtbYRmKG2xbn;ueYNt\W:2aXTlJIFnfGW{IEGgbJIh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYOsJGlEPTBiPTCwMlAxOjJizszNMi=> NVvDRZlmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
PC3 M1rQT2N6fG:2b4jpZ4l1gSCjc4PhfS=> M3TJNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwJF0hOC5yMEO4JO69VS5? MlP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780 NXvqSllTS3m2b4TvfIlkcXS7IHHzd4F6 NUXNTpFvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OCB;IECuNFA2PyEQvF2u NVvlW3B7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
A431 MorNR5l1d3SxeHnjbZR6KGG|c3H5 NIrjd2pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkCwOlEh|ryPLh?= NITYTIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
MCF-7 NELoZY5EgXSxdH;4bYNqfHliYYPzZZk> MYK3NkBpenN? M{nL[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETi15IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OCB;IECuNFA4PCEQvF2u MoTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
MCF7 Ml3OR5l1d3SxeHnjbZR6KGG|c3H5 M2CxfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NEA:KDBwMEC4OEDPxE1w NGLPc4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
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SKOV3 M1rnc2N6fG:2b4jpZ4l1gSCjc4PhfS=> NYS4dFkyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OCB;IECuNlEyKM7:TT6= M3;VUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
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SH-SY5Y Ml;DR5l1d3SxeHnjbZR6KGG|c3H5 Mm\kOVYhcHK| MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB3NjDodpMh[nliTWTUJIF{e2G7LDDFR|UxKD1iMD6wNFM1KM7:TT6= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF4NUe0Nkc,OjhzNkW3OFI9N2F-
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PC3 NUDFVlVvSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3e3UlUh\GG7cx?= NHjBPWRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC1JIRigXNiYomgR4VtdC22aYTldkBIdG9icnXh[4VvfCCkYYPl[EBie3OjeTygTWM2OCB;IECuNFA2PyEQvF2u MmPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4MUC5PFQoRjJ6NkGwPVg1RC:jPh?=
HepG2 NXv4NmFjS3m2b4TvfIlkcXS7IHHzd4F6 MluyO|IhcHK| Mof1R5l1d3SxeHnjbZR6KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE45QSEQvF2u MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh6NUizOEc,Ojh6OEW4N|Q9N2F-
MDA-MB-231 NVraZoxQS3m2b4TvfIlkcXS7IHHzd4F6 M1LkbFczKGi{cx?= M3foSGN6fG:2b4jpZ4l1gSCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT6zJO69VS5? NX;GTWk6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4PFU5OzRpPkK4PFg2QDN2PD;hQi=>
HCT116 NHK5OVFEgXSxdH;4bYNqfHliYYPzZZk> M{DkV|czKGi{cx?= MlXhR5l1d3SxeHnjbZR6KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEvPiEQvF2u NIT1ZVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi4OVg{PCd-Mki4PFU5OzR:L3G+
HepG2 NHH1b4FEgXSxdH;4bYNqfHliYYPzZZk> NW\3V3NlPzJiaILz M4rkOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwOEmg{txONg>? M2TuOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{S4PFA5Lz5{OUO0PFgxQDxxYU6=
HCT116 NFXLT4REgXSxdH;4bYNqfHliYYPzZZk> NF71VZY4OiCqcoO= NIr1WZlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT62JO69VS5? NFT3R2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUO0PFgxQCd-MkmzOFg5ODh:L3G+
A549 NVvLe2ExS3m2b4TvfIlkcXS7IHHzd4F6 M1:x[FczKGi{cx?= NV3uUVNqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB|Lkeg{txONg>? M1fPW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{S4PFA5Lz5{OUO0PFgxQDxxYU6=
SH-SY5Y MXLBeZRweGijZ4mgZZN{[Xl? NUnEWZRYPDBiaILz NHTSNZpKdmS3Y4Tpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[XO|ZYPz[YQh[XNiTFOzM5Bpd3OyaH;0bYR6dGW2aHHuc4xidWmwZTDjc5VxdGmwZzDh[pRmeiB2MDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl4MUG4N{c,OTl7NkGxPFM9N2F-
MCF7 Mn\hRY51cXS3bX;yJIF{e2G7 M1n6eFYh\GG7cx?= NYHQNFdESW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5 MljTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
MDCK MV3GeY5kfGmxbjDhd5NigQ>? MWGxNEB2VQ>? M2XRbGFxeGG{ZX70JJBmem2nYXLpcIl1gSCjY4Lvd5Mh[XCrY3HsJJRwKGKjc3;sZZRmemGuIIPp[IUhcW5iZH;nJG1FS0tiY3XscJMh[XRiMUCgeW0h[nliTFOtUXMwVVNiYX7hcJl{cXN? NVLvU3p4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVkyOThpPkKzPFU6OTF6PD;hQi=>
DU145 NUH1SGhwS3m2b4TvfIlkcXS7IHHzd4F6 NHTJNJREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7 M{HtelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
MCF7 MoC5R5l1d3SxeHnjbZR6KGG|c3H5 NFjodHI6PiCqcoO= M{fSNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JINtd26xZ3XubYMh[XO|YYm= M13tVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HCT116 MVPGeY5kfGmxbjDhd5NigQ>? NXfzUIRYWmW|aYP0ZY5k\SCoYXP0c5ItKHKjdHnvJI9nKEmFNUCg[o9zKEGST{i2Ok1z\XOrc4ThcpQhcHWvYX6gTGNVOTF4IHPlcIx{KHSxIFnDOVAh\m:{IHj1cYFvKEiFVEGxOkBk\Wyucx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A2780 NHK5S4hCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFrZUlc4OiCqcoO= MnThRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUBqdiCycnXz[Y5k\SCxZjDubYNwfGmwYX3p[IUhdW:wb371Z4xmd3SrZHW= NX7JR5M1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU1OTlpPkK0OFA2PDF7PD;hQi=>
Sf9 M1;MXWZ2dmO2aX;uJIF{e2G7 MnezN|AhdWmwcx?= MoTuTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDmeYxtKGynbnf0bEBpfW2jbjDDMZRmem2rbnHsJGhqey:obHHnMZRi\2enZDDISGFEOSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{Bi\nSncjCzNEBucW6|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfS=> NVrRdJlSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg5ODhpPkK5N|Q5QDB6PD;hQi=>

... 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

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

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
Tags: 购买Daporinad (FK866, APO866) | Daporinad (FK866, APO866)供应商 | 采购Daporinad (FK866, APO866) | Daporinad (FK866, APO866)价格 | Daporinad (FK866, APO866)生产 | 订购Daporinad (FK866, APO866) | Daporinad (FK866, APO866)代理商
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID