Lonafarnib (SCH66336)

Catalog No.S2797

For research use only.

Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.

Lonafarnib (SCH66336) Chemical Structure

CAS No. 193275-84-2

Selleck's Lonafarnib (SCH66336) has been cited by 17 publications

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.
Targets
H-ras [1]
(Cell-free assay)
N-ras [1]
(Cell-free assay)
K-ras-4B [1]
(Cell-free assay)
1.9 nM 2.8 nM 5.2 nM
In vitro

SCH66336 at concentration ranging from 0.1 μM to 8 μM suppress growth and induce apoptosis of human head and neck squamous carcinoma cells (HNSCC) in a dose and time dependent manner. SCH66336 (8 μM) suppresses protein kinase B/Akt activity as well as the phosphorylation of the Akt substrates glycogen synthase kinase (GSK)-3β, forkhead transcription factor, and BAD in SqCC/Y1 cells. [2] SCH66336 demonstrate variable antiproliferative effects against the cell lines, with IC50 ranging from 0.6 μM to 32.3 μM. [3] Lonafarnib induces a CCAAT/enhancer-binding protein homologous protein (CHOP)-dependent transactivation of the DR5 promoter, thus induces CHOP-dependent DR5 up-regulation. Lonafarnib (< 10 μM) activates caspase-8 and its downstream caspases, thus induces caspase-8-dependent apoptosis in H1792 cells. Lonafarnib (5 μM) up-regulate DR5 expression, increase cell-surface DR5 distribution, and enhance tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in H1792 cells.[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Cos-1 monkey kidney cells NYHSelRLTnWwY4Tpc44h[XO|YYm= MljGTY5pcWKrdHnvckBw\iCScn;0[YlvKG[jcn7ld5ltfHKjboPm[ZJie2ViaX6gR49{NTFibX;ub4V6KGurZH7lfUBk\WyuczDlfJBz\XO|aX7nJGguWmG|LY\hcEwhUUN3ME2wMlAxOTlizszN M1zrW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUmwN|A6Lz5zMkG5NFMxQTxxYU6=
COS-7 monkey cells NHPWOYNHfW6ldHnvckBie3OjeR?= NHjxRZdKdmirYnn0bY5oKHSqZTDmZZJv\XO7bHH0bY9vKG:oIFitdoF{KHC{b4TlbY5{KGmwIFPPV{04KG2xbnvlfUBk\WyuczD0doFve2mnboTsfUBmgHC{ZYPzbY5oKEhvcnHzX3ZidDF{XT3DWmxUKGmwIITo[UB4cG:uZTDj[YxtKGG|c3H5MEBKSzVyPUCuNFEh|ryP NI\rR3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97OEKyOVU5Lz57OEKyOVU5RC:jPh?=
MCF-7 tumor cell line MlG0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWjDc41xd3WwZDD3ZZMhdWWjc4Xy[YQh\m:{IHnubIljcXSrb36gc4YhVUOILUegeJVud3JiY3XscEBtcW6nIHnuJIJz\WG|dDD1coRmeiC|b3\0JIFo[XJiYYPzZZktKEmFNUC9NE4xPSEQvF2= NWjmd4JiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUiyNlU2QCd-OUiyNlU2QDxxYU6=
HCT116 MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{PTVGNwdXCxdX7kJJdieyCvZXHzeZJm\CCob4KgbY5pcWKrdHnvckBw\iCKQ2SxNVYhfHWvb4KgZ4VtdCCuaX7lJIlvKGOxbH;uJJVv\GW{IIPv[pQh[WejcjDhd5NigSxiSVO1NF0xNjB5IN88US=> NV6yZXFPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUiyNlU2QCd-OUiyNlU2QDxxYU6=
NIH-H tumor cell lines NF\LSnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEDafVREd22yb4Xu[EBi[mmuaYT5JJRwKGmwaHnibZQh[W6laH;yZYdmNWmwZHXw[Y5l\W62IHfyc5d1cCCxZjDOTWguUCC2dX3vdkBk\WyuIHzpcoV{KGmwIIPv[pQh[WejcjygTWM2OD1yLkC3NkDPxE1? M1TCNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl6MkK1OVgoRjl6MkK1OVg9N2F-
NIH3T3 cells M1jTUmZ2dmO2aX;uJIF{e2G7 MXTJcohq[mm2aX;uJI9nKFKjczDmZZJv\XO7bHH0bY9vKGmwIFitVoF{KHS{YX7z[o9zdWWmIF7JTFNVOyClZXzsd{whTUN3ME2wMlEh|ryP NXvKXmdxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW0OVQzOjhpPkG1OFU1OjJ6PD;hQi=>
NIH-K tumor cell lines NFjkVXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTDc41xd3WwZDDhZoltcXS7IITvJIlvcGmkaYSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bEBw\iCQSVitT{B1fW2xcjDj[YxtKGyrbnXzJIlvKHOxZoSgZYdieixiSVO1NF0xNjVizszN MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86QDJ{NUW4K|46QDJ{NUW4QE9iRg>?
Cos-1 NH3ENHhHfW6ldHnvckBie3OjeR?= NWPjUo1OUW6qaXLpeIlwdiCxZjDQdo91\WmwIH\hdo5me3mudILhcpNn\XKjc3WgbY4hS2:|LUGgcY9vc2W7IHvp[I5mgSClZXzsd{BmgHC{ZYPzbY5oKEhvUnHzMZZidCxiSVO1NEA:KDBwMECxPUDPxE1w Mle0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNFkoRjF{MUmwN|A6RC:jPh?=
Cos-1 MmOwSpVv[3Srb36gZZN{[Xl? Mn\zSYZn\WO2IH;uJHJieyCycn;j[ZN{cW6pIHnuJGNwey1zIH3vcotmgSCtaXTu[Zkh[2WubIOg[ZhxemW|c3nu[{BmcXSqZYKgTE1T[XNvVnHsJFEzNUOYTGOgc5IhUC2UYYOtWoFtOTJuIFnDOVAhRSByLkCxJO69VS5? MkHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB2MUG0PFUoRjFyNEGxOFg2RC:jPh?=
COS7 MU\GeY5kfGmxbjDhd5NigQ>? MlXhTY5pcWKrdHnvckBw\iCIVHHz[UBqdiCqdX3hckBEV1N5IHPlcIx{NCCLQ{WwJF0hOC5yMTFOwG0v MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODl{NUSzN{c,OjB7MkW0N|M9N2F-
H-Ras transformed cells M163fWZ2dmO2aX;uJIF{e2G7 M{\xTWlvcGmkaYTpc44hd2Zic3;meEBi\2G{IHPvcI9vgSCob4LtZZRqd25iaX6gTE1T[XNidILhcpNnd3KvZXSgZ4VtdHNuIFnDOVAhRSByLkC3JO69VS5? MlXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV3MEGwOlUoRjF3NUCxNFY2RC:jPh?=
NIH3T3 M4fTT2Z2dmO2aX;uJIF{e2G7 NFrtVJdG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDh[4FqdnO2IFjhMXJCWyCycn;j[ZN{cW6pIHnuJG5KUDOWMzDyZZMufHKjboPmc5Ju\WRiY3XscJMtKEWFNUCgQUAxNjF4IN88UU4> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZ3N{K4OEc,OTJ4NUeyPFQ9N2F-
NIH3T3 NXP5U2pmTnWwY4Tpc44h[XO|YYm= NFnJdINVWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCGTmKg[YZndHW6IDjEUnI7KD9idV2pJIlvKE2GUkGt[ZhxemW|c3nu[{BPUUh|VEOgZ4VtdHNuIFnDOVAhRSB{Lkeg{txONg>? M4\RdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzNkC2N|g6Lz5zMU[wOlM5QTxxYU6=
A673 NVnkR5Z2eUiWUzDhd5NigQ>? MmLLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? NFyyZ3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY MV7xTHRUKGG|c3H5 M4PhRZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy| MlTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MlzvdWhVWyCjc4PhfS=> M1PCWpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= NIHBcIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 MnrBdWhVWyCjc4PhfS=> MnnwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| NIXje|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD NFvNdYJyUFSVIHHzd4F6 MorxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ MnfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 NHvo[3FyUFSVIHHzd4F6 NVLnfY9DeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz M3\Kd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) NE[3Vo1yUFSVIHHzd4F6 MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NYPZeHN5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NHj5foZyUFSVIHHzd4F6 M1SwT5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= MnHnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NVXYbWJ[eUiWUzDhd5NigQ>? NUXNdGV1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NHfOXGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 MmXydWhVWyCjc4PhfS=> NWjQfHVMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= NGrZVYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MXHxTHRUKGG|c3H5 NWH3V5ZZeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NGLJTWVyUFSVIHHzd4F6 MmD1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NV\jeZFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 M3;2fZFJXFNiYYPzZZk> NYnZV41keUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> M2LhbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 MkXWdWhVWyCjc4PhfS=> MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NWrT[Vd[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Caco-2 MW\DfZRwfG:6aXPpeJkh[XO|YYm= M4C5V|Q5KGixdYLz MV;E[ZRmem2rbnH0bY9vKG:oIFnDOVAhfmGudXXzJIZweiCrbnjpZol1cW:wIH;mJHNCWlNvQ3;WMVIhcW6mdXPl[EBkgXSxdH;4bYNqfHlib3[gR4Fkdy1{IHPlcIx{KGGodHXyJFQ5KGixdYLzJIJ6KGirZ3igZ49vfGWwdDDpcYFocW6pLDDJR|UxKD1iNT62PEDPxE1w MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPVg4OzRxJ{7DbGVOSkx:L3G+
Caco-2 M3rBfnRwgGmlaYT5JIF{e2G7 MWi0PEBpd3W{cx?= NIrmepFVd3irY3n0fUBi\2GrboP0JGNi[29vMjDj[YxteyCmZYTldo1qdmWmIHH0JFQ5KGixdYLzJIJ6KGmwdILhZ4VtdHWuYYKgRXRRKGOxbnPlcpRz[XSrb36geZNqdmdidHjlJGNmdGyWaYTldk1IdG9iTIXtbY5me2OnboSgR4VtdCCYaXHibYxqfHliQYPzZZktKEOFNUCgQUAyOC55MTFOwG0v NYG3SmhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjl6N{O0M{c,S2iHTVLMQE9iRg>?
Assay
Methods Test Index PMID
Western blot LC3A / LC3B ; Cyclin D / CDK6 / CDK4 / SKP2 ; PARP / cleaved-PARP / pro-caspase3 / cleaved-caspase3 / Bcl-2 ; p-ERK / p-SAPK / p-JNK 29069775 29285232
Growth inhibition assay Cell viability ; Cell number 15860663 29069775
In vivo SCH66336 inhibits HTBI77 human lung carcinoma xenograft growth in nude mice in a dose-dependent fashion. [1] SCH66336 dosed at 50 mg/kg p.o. bid by oral gavage inhibits tumor growth with up to 69% growth inhibition after 21 days of treatment in NOD/SCID mice bearing s.c. flank XEN01, XEN05 or XEN08 GBM xenografts. [3]

Protocol (from reference)

Cell Research:[2]
  • Cell lines: UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, and UMSCC35, UMSCC38 cell lines
  • Concentrations: 0.1 μM - 8 μM
  • Incubation Time: 24 hours
  • Method: The cells are seeded in 96-well cell-culture cluster plates at a density that allowed control cultures to grow exponentially for 5 days. After 24 hours, the cells are treated with different concentrations of SCH66336. SCH66336 is dissolved in DMSO. Control cultures received the same amount of DMSO as the treated cultures do. Cell numbers are estimated after 5 days of treatment by SRB assay. The percentage of growth inhibition is calculated by using the equation: percentage growth inhibition = (1 − At/Ac) × 100, where At and Ac represent the absorbance in treated and control cultures, respectively. The drug concentration causing a 50% cell growth inhibition (IC50), is determined by interpolation from dose-response curves.
Animal Research:[3]
  • Animal Models: NOD/SCID mice between 6–12 weeks of age
  • Dosages: 50 mg/kg
  • Administration: p.o. bid by oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 638.82
Formula

C27H31Br2ClN4O2

CAS No. 193275-84-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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% 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

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02579044 Enrolling by invitation Drug: Everolimus and lonafarnib Progeria Boston Children''s Hospital December 2015 Phase 1|Phase 2
NCT02527707 Completed Drug: lonafarnib|Drug: Ritonavir Chronic Delta Hepatitis Eiger BioPharmaceuticals|Hannover Medical School September 2015 Phase 2
NCT02430194 Completed Drug: lonafarnib|Drug: Ritonavir|Drug: PEG IFN-a Chronic Hepatitis D Infection Eiger BioPharmaceuticals|Ankara University December 2014 Phase 2
NCT02430181 Completed Drug: lonafarnib|Drug: PEG IFN-a|Drug: Ritonavir Chronic Hepatitis D Infection Eiger BioPharmaceuticals November 2014 Phase 2
NCT01495585 Completed Drug: Lonafarnib|Other: Placebo Hepatitis D National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) December 2011 Phase 2
NCT01232881 Terminated Procedure: Tumor Sample|Procedure: Serum Sample Breast Cancer Hoosier Cancer Research Network|United States Department of Defense|Indiana University School of Medicine|Emory University August 2009 --

(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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