Daporinad (FK866, APO866)

For research use only.

Catalog No.S2799

33 publications

Daporinad (FK866, APO866) Chemical Structure

CAS No. 658084-64-1

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.

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Selleck's Daporinad (FK866, APO866) has been cited by 33 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 NIf3U5NEgXSxdH;4bYNqfHliYYPzZZk> MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kB1d3SjbDDj[YxtfWyjcjDORWQpWClibHX2[YwtKEmFNUCgQUAxNjByMEWg{txONg>? NEDPUnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm2NVE5Oyd-MUm5OlEyQDN:L3G+
SH-SY5Y NF3lVHpEgXSxdH;4bYNqfHliYYPzZZk> M1TVb|Q5KGi{cx?= Mn3iR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5yMEG3JO69VS5? M2DGU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OU[xNVg{Lz5zOUm2NVE5OzxxYU6=
HT1080 MkLrR5l1d3SxeHnjbZR6KGG|c3H5 NIn3NXU3KGSjeYO= NU\hNnJNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRzMEiwJINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkG2JO69VS5? M3vKWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
A549 NY[xcndFS3m2b4TvfIlkcXS7IHHzd4F6 NYPjeJNNPiCmYYnz M4HJZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
HCT116 M1PFcWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1j5WVYh\GG7cx?= MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=> MmmzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
SNU638 M{TIZWN6fG:2b4jpZ4l1gSCjc4PhfS=> NHLi[pk3KGSjeYO= Ml36R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25WPjN6IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjF4IN88UU4> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN|MECxOUc,OjF|M{CwNVU9N2F-
MCF7 M4LjfWFvfGm2dX3vdkBie3OjeR?= NITBTJUyOCC3TR?= MX[2JIRigXN? NYe5fHlGSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BifCBzMDD1UUBi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE43QCEQvF2u Mm\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
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A2780 NXTwOZcxSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NEjUNXU4OiCqcoO= M2H4RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JHNTSi2kYYPl[EBucWO{b4DsZZRmKHKnYXTldkBidmGueYPpd{whUUN3MDC9JFAvODBzIN88UU4> NUX3SpZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVkyOThpPkKzPFU6OTF6PD;hQi=>
NYH NHfjS3dEgXSxdH;4bYNqfHliYYPzZZk> MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3MDC9JFAvODBzNTFOwG0v Mnv6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780 M{HVW2N6fG:2b4jpZ4l1gSCjc4PhfS=> NVrWcHFvPzJiaILz NFXyU41EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTBiPTCwMlAxOTZizszNMi=> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
HepG2 NXTyWm9WTnWwY4Tpc44h[XO|YYm= MmraNUBpeg>? NWe1ZWdqUW6qaXLpeIlwdiCxZjDORW1RXCCrbjDoeY1idiCKZYDHNkBk\WyuczD1d4lv\yCdMUTDYU1vcWOxdHnuZY1q\GVxUGLQVEBieyC|dXLzeJJifGViYYPz[ZN{\WRiYYOg[o9zdWG2aX;uJI9nKFtzNFPdMY5q[2:2aX7hcYll\SCvb37vcpVkdGWxdHnk[UBi\nSncjCxJIhzKGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nzMEBKSzVyIE2gNE4xODJ{IN88UU4> NVS2NY9zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
PC3 M2nVU2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3MDC9JFAvODB|ODFOwG0v Mn;6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780 MWHDfZRwfG:6aXPpeJkh[XO|YYm= M2\RXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkCwOVch|ryPLh?= M3f2dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
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MCF-7 MnLqR5l1d3SxeHnjbZR6KGG|c3H5 M1e1cVczKGi{cx?= MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2YuPyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVAhRSByLkCwO|Qh|ryPLh?= M1PkOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
MCF7 NWrreHE1S3m2b4TvfIlkcXS7IHHzd4F6 NIWyUm9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkCwPFQh|ryPLh?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
HCT116 NXX5S21JS3m2b4TvfIlkcXS7IHHzd4F6 NGjnVIo4OiCqcoO= NYm3PZZNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3MDC9JFAvODFyOTFOwG0v MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
SKOV3 M3PwSmN6fG:2b4jpZ4l1gSCjc4PhfS=> NWOydFI5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OCB;IECuNlEyKM7:TT6= M3\vclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HCT116 NYrBNVJJS3m2b4TvfIlkcXS7IHHzd4F6 MWq3NkBpenN? M2rMdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEGST{i2Ok1z\XOrc4ThcpQhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OCB;IECuPVQ3KM7:TT6= NI[w[GE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
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SH-SY5Y Mm\wR5l1d3SxeHnjbZR6KGG|c3H5 M2\x[VU3KGi{cx?= NEDjR5dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC1OkBpenNiYomgUXRVKGG|c3H5MEBGSzVyIE2gNE4xODN2IN88UU4> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF4NUe0Nkc,OjhzNkW3OFI9N2F-
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PC3 NIH3XVhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEK2dnk2KGSjeYO= M2HGOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBqdmO3YnH0[YQh\m:{IEWg[IF6eyCkeTDD[YxtNXSrdHXyJGdtdyC{ZXHn[Y51KGKjc3XkJIF{e2G7LDDJR|UxKD1iMD6wNFU4KM7:TT6= NXf2SGdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2NVA6QDRpPkK4OlExQTh2PD;hQi=>
HepG2 MnXNR5l1d3SxeHnjbZR6KGG|c3H5 MU[3NkBpenN? MVfDfZRwfG:6aXPpeJkhcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCwMlg6KM7:TT6= NVO3SJF1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4PFU5OzRpPkK4PFg2QDN2PD;hQi=>
MDA-MB-231 MlHsR5l1d3SxeHnjbZR6KGG|c3H5 NHjIXVQ4OiCqcoO= NXj2eooxS3m2b4TvfIlkcXS7IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxMlMh|ryPLh?= NHe1Oo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi4OVg{PCd-Mki4PFU5OzR:L3G+
HCT116 NGXpeI1EgXSxdH;4bYNqfHliYYPzZZk> NHrpVWM4OiCqcoO= Ml\rR5l1d3SxeHnjbZR6KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEvPiEQvF2u NEPsUoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi4OVg{PCd-Mki4PFU5OzR:L3G+
HepG2 M3nqUmN6fG:2b4jpZ4l1gSCjc4PhfS=> MXK3NkBpenN? MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjh7IN88UU4> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN2OEiwPEc,Ojl|NEi4NFg9N2F-
HCT116 NUfJN|ZlS3m2b4TvfIlkcXS7IHHzd4F6 NGf3NWM4OiCqcoO= M{CycWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLk[g{txONg>? NYDHWIxRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg5ODhpPkK5N|Q5QDB6PD;hQi=>
A549 NIPuN4JEgXSxdH;4bYNqfHliYYPzZZk> MnLSO|IhcHK| Mmq5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA{NjdizszNMi=> NWrMXY41RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg5ODhpPkK5N|Q5QDB6PD;hQi=>
SH-SY5Y MorMRZV1d3CqYXf5JIF{e2G7 NHP3dos1OCCqcoO= NH7LV5ZKdmS3Y4Tpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[XO|ZYPz[YQh[XNiTFOzM5Bpd3OyaH;0bYR6dGW2aHHuc4xidWmwZTDjc5VxdGmwZzDh[pRmeiB2MDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M1TB[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OU[xNVg{Lz5zOUm2NVE5OzxxYU6=
MCF7 NXr1OHVnSW62aYT1cY9zKGG|c3H5 NFz2NYI3KGSjeYO= NF60bmZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO|YYm= NVfTdHZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN|AxOTVpPkKxN|MxODF3PD;hQi=>
MDCK M13sSmZ2dmO2aX;uJIF{e2G7 M2\jelExKHWP M{exd2FxeGG{ZX70JJBmem2nYXLpcIl1gSCjY4Lvd5Mh[XCrY3HsJJRwKGKjc3;sZZRmemGuIIPp[IUhcW5iZH;nJG1FS0tiY3XscJMh[XRiMUCgeW0h[nliTFOtUXMwVVNiYX7hcJl{cXN? M{m4UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEW5NVE5Lz5{M{i1PVEyQDxxYU6=
DU145 NHPEb3hEgXSxdH;4bYNqfHliYYPzZZk> NG\UZ2REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7 M{HmbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
MCF7 NX\J[GVmS3m2b4TvfIlkcXS7IHHzd4F6 NYnneplUQTZiaILz M37CU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JINtd26xZ3XubYMh[XO|YYm= NWnoT3lVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
HCT116 NYrvRYM3TnWwY4Tpc44h[XO|YYm= MVfS[ZNqe3SjbnPlJIZi[3SxcjygdoF1cW9ib3[gTWM2OCCob4KgRXBQQDZ4LYLld4l{fGGwdDDoeY1idiCKQ2SxNVYh[2WubIOgeI8hUUN3MDDmc5IhcHWvYX6gTGNVOTF4IHPlcIx{ Ml7xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780 NYTBTI95SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NFrBb3M4OiCqcoO= M1rrUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZkhcW5icILld4Vv[2Vib3[gcolkd3SrbnHtbYRmKG2xbn;ueYNt\W:2aXTl M332WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1OFE6Lz5{NESwOVQyQTxxYU6=
Sf9 MlPjSpVv[3Srb36gZZN{[Xl? NELNb3A{OCCvaX7z NHnGUIxKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKGi3bXHuJGMufGW{bXnuZYwhUGm|L3\sZYcufGGpZ3XkJGhFSUNzIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6 NYHkWnh7RGFidHHy[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
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

Cell Research:

[1]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • 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
    (Only for Reference)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 391.51
Formula

C24H29N3O2

CAS No. 658084-64-1
Storage powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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.

Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID