Daporinad (FK866, APO866)

Catalog No.S2799

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 (FK866, APO866) Chemical Structure

CAS No. 658084-64-1

Selleck's Daporinad (FK866, APO866) has been cited by 46 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 NYWxT2JbS3m2b4TvfIlkcXS7IHHzd4F6 MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kB1d3SjbDDj[YxtfWyjcjDORWQpWClibHX2[YwtKEmFNUCgQUAxNjByMEWg{txONg>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl4MUG4N{c,OTl7NkGxPFM9N2F-
SH-SY5Y NFPPcGxEgXSxdH;4bYNqfHliYYPzZZk> Mn3zOFghcHK| MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjByMUeg{txONg>? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl4MUG4N{c,OTl7NkGxPFM9N2F-
HT1080 M3H6XmN6fG:2b4jpZ4l1gSCjc4PhfS=> NW\X[XN5PiCmYYnz NWjpdIdFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRzMEiwJINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkG2JO69VS5? NVL2b|dlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|AxOTVpPkKxN|MxODF3PD;hQi=>
A549 MXHDfZRwfG:6aXPpeJkh[XO|YYm= NWflTZNTPiCmYYnz MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlE3KM7:TT6= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
HCT116 M4K5UWN6fG:2b4jpZ4l1gSCjc4PhfS=> MnvHOkBl[Xm| M1rSbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5zNjFOwG0v MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
SNU638 NGrHfmhEgXSxdH;4bYNqfHliYYPzZZk> MXq2JIRigXN? NVfVbpJZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06XNkO4JINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkG2JO69VS5? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
MCF7 M4\TWmFvfGm2dX3vdkBie3OjeR?= MljrNVAhfU1? M2q1TFYh\GG7cx?= NETUc2JCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF1KDFyIIXNJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlY5KM7:TT6= NYTwXFRbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|AxOTVpPkKxN|MxODF3PD;hQi=>
K562 M1fOT2N6fG:2b4jpZ4l1gSCjc4PhfS=> NH:5[WI3KGSjeYO= NXjTVWZWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOjBizszNMi=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
A2780 M1\wUmN6fG:2b4jpZ4l1gSCjc4PhfS=> NH3MV3g4OiCqcoO= Mo\4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvODBzIN88UU4> NIHpU|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xO|c5PCd-MkO2NVc4QDR:L3G+
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K562 MULDfZRwfG:6aXPpeJkh[XO|YYm= NIrROHQ6PiCqcoO= NUG1dlNpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5yMEeyJO69VS5? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5OUmxOUc,OjN4N{m5NVU9N2F-
A2780 M3fTdGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MmjBO|IhcHK| M4PwXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JHNTSi2kYYPl[EBucWO{b4DsZZRmKHKnYXTldkBidmGueYPpd{whUUN3MDC9JFAvODBzIN88UU4> MnrEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUmxNVgoRjJ|OEW5NVE5RC:jPh?=
NYH NGLqd5ZEgXSxdH;4bYNqfHliYYPzZZk> MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3MDC9JFAvODBzNTFOwG0v MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A2780 NWCxWZdES3m2b4TvfIlkcXS7IHHzd4F6 MWO3NkBpenN? M37ScGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OCB;IECuNFAyPiEQvF2u MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
HepG2 M17rdGZ2dmO2aX;uJIF{e2G7 M{fLVFEhcHJ? M4PkdmlvcGmkaYTpc44hd2ZiTlHNVHQhcW5iaIXtZY4hUGWyR{KgZ4VtdHNidYPpcochYzF2Q22tcolkd3SrbnHtbYRmN1CUUGCgZZMhe3Wkc4TyZZRmKGG|c3Xzd4VlKGG|IH\vdo1ifGmxbjDv[kBcOTSFXT3ubYNwfGmwYX3p[IUhdW:wb371Z4xmd3SrZHWgZYZ1\XJiMTDodkBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OCB;IECuNFAzOiEQvF2u M{PjdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
PC3 MULDfZRwfG:6aXPpeJkh[XO|YYm= NEnWZWJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NEA:KDBwMECzPEDPxE1w NIjWRZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
A2780 NX;aVop3S3m2b4TvfIlkcXS7IHHzd4F6 M3zJSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkCwOVch|ryPLh?= NFH4[G89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
A431 M{foRWN6fG:2b4jpZ4l1gSCjc4PhfS=> MnzNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwJF0hOC5yME[xJO69VS5? NGLZcYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
MCF-7 MWfDfZRwfG:6aXPpeJkh[XO|YYm= NGi1fGU4OiCqcoO= NIfBflhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0ZvNzDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTBiPTCwMlAxPzRizszNMi=> NUjlNJBmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
MCF7 M4r3eWN6fG:2b4jpZ4l1gSCjc4PhfS=> NXzhU4hzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7LDDJR|UxKD1iMD6wNFg1KM7:TT6= MlnzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
HCT116 MXLDfZRwfG:6aXPpeJkh[XO|YYm= NYL6dIN5PzJiaILz MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxKD1iMD6wNVA6KM7:TT6= NEjoVow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
SKOV3 MYXDfZRwfG:6aXPpeJkh[XO|YYm= MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwJF0hOC5{MUGg{txONg>? NFvxeJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
HCT116 Mn3pR5l1d3SxeHnjbZR6KGG|c3H5 NHzQc4U4OiCqcoO= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBCWE96Nk[tdoV{cXO2YX70JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVAhRSByLkm0OkDPxE1w MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
A2780 NFLteZpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NW\KfWZPPzJiaILz NEPFO4JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOC5yMEGg{txONg>? MlS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MEW0NVkoRjJ2NEC1OFE6RC:jPh?=
A2780 NEfSRXBHfW6ldHnvckBie3OjeR?= M1fUPVczKGi{cx?= NVX6Ook6UW6qaXLpeIlwdiCxZjDORW1RXCCrbjDoeY1idiCDMke4NEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE4xODFizszNMi=> MmXBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGyO|EoRjJ5NUSxNlcyRC:jPh?=
DE3 MljRSpVv[3Srb36gZZN{[Xl? MYmxOUBucW6| NFe3RYxKdmirYnn0bY9vKG:oIHj1cYFvKG[3bHygcIVv\3SqIFOteIVzdWmwYXygTIl{Pi22YXfn[YQhVkGPUGSg[ZhxemW|c3XkJIlvKEW|Y3jldolkcGmjIHPvcIkhWm:|ZYT0ZUApTEV|KTDj[YxteyC3c3nu[{BvcWOxdHnuZY1q\GViYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiMUWgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BqdiCycnXz[Y5k\SCxZjDQVnBRNCCLQ{WwJF0hOC5yMEOg{txONg>? MlvGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGyO|EoRjJ5NUSxNlcyRC:jPh?=
SH-SY5Y MV3DfZRwfG:6aXPpeJkh[XO|YYm= M3OyZVU3KGi{cx?= NFzxU|lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC1OkBpenNiYomgUXRVKGG|c3H5MEBGSzVyIE2gNE4xODN2IN88UU4> NXvqZ5g1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOlU4PDJpPkK4NVY2PzR{PD;hQi=>
A2780 NIeyT4xEgXSxdH;4bYNqfHliYYPzZZk> NF\GbVBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImsJGlEPTBiPTCwMlAxPDJizszNMi=> Mom4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNkW3OFIoRjJ6MU[1O|QzRC:jPh?=
PC3 NUfDcIR3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MlLtOUBl[Xm| MofjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiNTDkZZl{KGK7IFPlcIwufGm2ZYKgS4xwKHKnYXflcpQh[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwOVch|ryPLh?= M4rLVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkGwPVg1Lz5{OE[xNFk5PDxxYU6=
HepG2 MYTDfZRwfG:6aXPpeJkh[XO|YYm= NXHGdINMPzJiaILz NEPIe2VEgXSxdH;4bYNqfHliaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjh7IN88UU4> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh6NUizOEc,Ojh6OEW4N|Q9N2F-
MDA-MB-231 MYLDfZRwfG:6aXPpeJkh[XO|YYm= M1TONVczKGi{cx?= NXjObXBFS3m2b4TvfIlkcXS7IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxMlMh|ryPLh?= NFjEdpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi4OVg{PCd-Mki4PFU5OzR:L3G+
HCT116 NEjvTohEgXSxdH;4bYNqfHliYYPzZZk> M1:4dlczKGi{cx?= MVXDfZRwfG:6aXPpeJkhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNU43KM7:TT6= M2LofVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEi1PFM1Lz5{OEi4OVg{PDxxYU6=
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HCT116 M2LW[2N6fG:2b4jpZ4l1gSCjc4PhfS=> M1vEfFczKGi{cx?= NUXGVIVwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuOkDPxE1w NUW3WnFvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg5ODhpPkK5N|Q5QDB6PD;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

Ethanol 78 mg/mL
(199.22 mM)
DMSO Insoluble
Water Insoluble

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 2022-01-17)

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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