Daporinad

Catalog No.S2799 Synonyms: FK866, APO866

For research use only.

Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.

Daporinad  Chemical Structure

CAS No. 658084-64-1

Selleck's Daporinad has been cited by 50 publications

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
Targets
NMPRTase [5]
(Cell-free assay)
0.4 nM(Ki)
In vitro

APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia [AML], acute lymphoblastic leukemia [ALL], mantle cell lymphoma [MCL], chronic lymphocytic leukemia [CLL], and T-cell lymphoma. APO866 at low concentrations ranging from 0-10 nM induces cell death, this effect is independent of caspase activation but is associated with depolarization of mitochondrial membrane. APO866 at concentrations ranging from 0-10 nM dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. [1] APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y NEPsdmREgXSxdH;4bYNqfHliYYPzZZk> MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kB1d3SjbDDj[YxtfWyjcjDORWQpWClibHX2[YwtKEmFNUCgQUAxNjByMEWg{txONg>? M3PrVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OU[xNVg{Lz5zOUm2NVE5OzxxYU6=
SH-SY5Y MmTsR5l1d3SxeHnjbZR6KGG|c3H5 M2Ph[lQ5KGi{cx?= M1TZT2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNJNVO\NWmgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwMECxO{DPxE1w Ml7oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7NkGxPFMoRjF7OU[xNVg{RC:jPh?=
HT1080 NES1XFZEgXSxdH;4bYNqfHliYYPzZZk> M3HTS|Yh\GG7cx?= MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWFExQDBiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=> M{HXT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
A549 M{jn[WN6fG:2b4jpZ4l1gSCjc4PhfS=> M3TUcVYh\GG7cx?= NH64RWZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjF4IN88UU4> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
HCT116 MlT6R5l1d3SxeHnjbZR6KGG|c3H5 MmjIOkBl[Xm| NXfoSFRES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkG2JO69VS5? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
SNU638 Mn7nR5l1d3SxeHnjbZR6KGG|c3H5 NEXDbXc3KGSjeYO= M2HIdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNPXTZ|ODDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5zNjFOwG0v M3G4fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
MCF7 MXHBcpRqfHWvb4KgZZN{[Xl? NXLi[oE{OTBidV2= M4fSOlYh\GG7cx?= NHTOenhCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF1KDFyIIXNJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlY5KM7:TT6= NIjJTpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOzNFAyPSd-MkGzN|AxOTV:L3G+
K562 NXz6T|NTS3m2b4TvfIlkcXS7IHHzd4F6 MV[2JIRigXN? MoniR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNlAh|ryPLh?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
A2780 MlS0R5l1d3SxeHnjbZR6KGG|c3H5 NWLsfnFNPzJiaILz NYDWbXNUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwMECxJO69VS5? M2PzSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG3O|g1Lz5{M{[xO|c5PDxxYU6=
NYH Mo\5R5l1d3SxeHnjbZR6KGG|c3H5 MVKzJJdm\Wu| MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZYZ1\XJiMzD3[YVseyCkeTDjcI9vd2enbnnjJJN2en[rdnHsJIF{e2G7LDDMSFUxKD1iMD6wNFE2KM7:TT6= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5OUmxOUc,OjN4N{m5NVU9N2F-
K562 NGLndmFEgXSxdH;4bYNqfHliYYPzZZk> NWfZZphLQTZiaILz Mn\FR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4xODd{IN88UU4> M{i3cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke5PVE2Lz5{M{[3PVkyPTxxYU6=
A2780 NEm1fGhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NHfKN|k4OiCqcoO= M{HlfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JHNTSi2kYYPl[EBucWO{b4DsZZRmKHKnYXTldkBidmGueYPpd{whUUN3MDC9JFAvODBzIN88UU4> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3OUGxPEc,OjN6NUmxNVg9N2F-
NYH MoP3R5l1d3SxeHnjbZR6KGG|c3H5 MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3MDC9JFAvODBzNTFOwG0v MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A2780 MojGR5l1d3SxeHnjbZR6KGG|c3H5 NV;afpR7PzJiaILz MofjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD6wNFE3KM7:TT6= NF[1O2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
HepG2 NVXKS4p3TnWwY4Tpc44h[XO|YYm= MljQNUBpeg>? NGP4c41KdmirYnn0bY9vKG:oIF7BUXBVKGmwIHj1cYFvKEincFeyJINmdGy|IIXzbY5oKFtzNFPdMY5q[2:2aX7hcYll\S:SUmDQJIF{KHO3YoP0doF1\SCjc4Pld5Nm\CCjczDmc5Ju[XSrb36gc4YhYzF2Q22tcolkd3SrbnHtbYRmKG2xbn;ueYNt\W:2aXTlJIFnfGW{IEGgbJIh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYOsJGlEPTBiPTCwMlAxOjJizszNMi=> NVvTc2lsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
PC3 NI\pU5ZEgXSxdH;4bYNqfHliYYPzZZk> NEjMeFhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NEA:KDBwMECzPEDPxE1w NEe5cJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
A2780 MVPDfZRwfG:6aXPpeJkh[XO|YYm= MlLQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NEA:KDBwMEC1O{DPxE1w M2noc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
A431 M4TzXWN6fG:2b4jpZ4l1gSCjc4PhfS=> MmXLR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwJF0hOC5yME[xJO69VS5? NFnoSXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
MCF-7 MVfDfZRwfG:6aXPpeJkh[XO|YYm= NGDZems4OiCqcoO= M4LjcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETi15IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OCB;IECuNFA4PCEQvF2u NWPJd3JRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
MCF7 MVnDfZRwfG:6aXPpeJkh[XO|YYm= NXvPdGN6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7LDDJR|UxKD1iMD6wNFg1KM7:TT6= M1fKRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HCT116 Ml;HR5l1d3SxeHnjbZR6KGG|c3H5 MVq3NkBpenN? M17Cb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTBiPTCwMlAyODlizszNMi=> NXvINGhXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
SKOV3 MmXnR5l1d3SxeHnjbZR6KGG|c3H5 M4jEU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkKxNUDPxE1w M1;CZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HCT116 MnHxR5l1d3SxeHnjbZR6KGG|c3H5 NInwU2c4OiCqcoO= Mn;VR5l1d3SxeHnjbZR6KGGpYXnud5QhSVCROE[2MZJme2m|dHHueEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD65OFYh|ryPLh?= M2jPVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
A2780 MkH0RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NFu4ToI4OiCqcoO= NFmxXolCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOC5yMEGg{txONg>? NW\rb5M5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU1OTlpPkK0OFA2PDF7PD;hQi=>
A2780 MkXhSpVv[3Srb36gZZN{[Xl? MX63NkBpenN? M2[yNGlvcGmkaYTpc44hd2ZiTlHNVHQhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IECuNFAyKM7:TT6= NV\LUHFMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFEzPzFpPkK3OVQyOjdzPD;hQi=>
DE3 MV;GeY5kfGmxbjDhd5NigQ>? M{HW[VE2KG2rboO= MoDhTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuIHzlcod1cCCFLYTldo1qdmGuIFjpd|YufGGpZ3XkJG5CVVCWIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJHJwe2W2dHGgLGRGOyliY3XscJMhfXOrbnegcolkd3SrbnHtbYRmKGG|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDF3IH3pcpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiUGLQVEwhUUN3MDC9JFAvODB|IN88UU4> NYftUVdlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFEzPzFpPkK3OVQyOjdzPD;hQi=>
SH-SY5Y MUHDfZRwfG:6aXPpeJkh[XO|YYm= NIH5SIk2PiCqcoO= NYXMXXNJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0hvU2m1XUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOVYhcHK|IHL5JG1VXCCjc4PhfUwhTUN3MDC9JFAvODB|NDFOwG0v MlS5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNkW3OFIoRjJ6MU[1O|QzRC:jPh?=
A2780 M1:2XmN6fG:2b4jpZ4l1gSCjc4PhfS=> NEPve|NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImsJGlEPTBiPTCwMlAxPDJizszNMi=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF4NUe0Nkc,OjhzNkW3OFI9N2F-
PC3 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NXntV3l{PSCmYYnz MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB3IHThfZMh[nliQ3XscE11cXSncjDHcI8hemWjZ3XueEBj[XOnZDDhd5NigSxiSVO1NEA:KDBwMEC1O{DPxE1w NH;WdmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[xNFk5PCd-Mki2NVA6QDR:L3G+
HepG2 MlvIR5l1d3SxeHnjbZR6KGG|c3H5 MlvvO|IhcHK| MVLDfZRwfG:6aXPpeJkhcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlg6KM7:TT6= M1rQW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEi1PFM1Lz5{OEi4OVg{PDxxYU6=
MDA-MB-231 NU\Wb4c1S3m2b4TvfIlkcXS7IHHzd4F6 NWTR[ppnPzJiaILz M3HxVWN6fG:2b4jpZ4l1gSCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMT6zJO69VS5? NGX1bos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi4OVg{PCd-Mki4PFU5OzR:L3G+
HCT116 M3zQUmN6fG:2b4jpZ4l1gSCjc4PhfS=> NWXEWldPPzJiaILz NUjGUVQ1S3m2b4TvfIlkcXS7IHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFwNjFOwG0v NXTQWYM{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4PFU5OzRpPkK4PFg2QDN2PD;hQi=>
HepG2 Mo\oR5l1d3SxeHnjbZR6KGG|c3H5 NUfWeHpmPzJiaILz NYryV5lSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD64PUDPxE1w MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN2OEiwPEc,Ojl|NEi4NFg9N2F-
HCT116 M37PPWN6fG:2b4jpZ4l1gSCjc4PhfS=> MU[3NkBpenN? Ml\UR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFwNjFOwG0v M1jSN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{S4PFA5Lz5{OUO0PFgxQDxxYU6=
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MCF7 NW\RU|FWSW62aYT1cY9zKGG|c3H5 MlXpOkBl[Xm| NYnye3k{SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5 MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
MDCK M1O2XmZ2dmO2aX;uJIF{e2G7 MmL3NVAhfU1? MU\BdJBiemWwdDDw[ZJu\WGkaXzpeJkh[WO{b4PzJIFxcWOjbDD0c{Bj[XOxbHH0[ZJidCC|aXTlJIlvKGSxZzDNSGNMKGOnbHzzJIF1KDFyIIXNJIJ6KEyFLV3TM21UKGGwYXz5d4l{ NVmyVJhERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVkyOThpPkKzPFU6OTF6PD;hQi=>
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A2780 M{exVGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXG3NkBpenN? M1[0cGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZkhcW5icILld4Vv[2Vib3[gcolkd3SrbnHtbYRmKG2xbn;ueYNt\W:2aXTl NX;2TG85RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU1OTlpPkK0OFA2PDF7PD;hQi=>
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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
In vivo APO866 administered intraperitoneally at dose of 20 mg/kg twice a day for 4 days, repeat weekly over 3 weeks, prevents and abrogats tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. [1] APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA. [2]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: 41 hematologic malignant cell lines
  • Concentrations: 0 - 10 nM
  • Incubation Time: 72 hours or 96 hours
  • Method:

    For MTT assays, 0.5 × 106 cells/mL is plated in triplicate on 96-well plates. APO866 (0.01 nM-100 nM) is added in 50 μL of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 μL of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 μL/well) is added for 1 hour and the absorbance is read at 570 nm on a spectrophotometer. For trypan blue dye exclusion staining, 0.5 × 105 cells/well is grown in 6-well plates with 1 mL media in the absence or presence of APO866 for 96 hours. Cells from each sample are incubated with 10 μL trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells.

Animal Research:

[1]

  • Animal Models: C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
  • Dosages: 20 mg/kg
  • Administration: administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

4mg/mL

Chemical Information

Molecular Weight 391.51
Formula

C24H29N3O2

CAS No. 658084-64-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

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

Answer:
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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