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 NICyfFBHfW6ldHnvckBie3OjeR?= NE\HU2pKdmirYnn0bY9vKG:oIGDyc5RmcW5iZnHycoV{gWy2cnHud4ZmemG|ZTDpckBEd3NvMTDtc45s\Xlia3nkcoV6KGOnbHzzJIV5eHKnc4PpcochUC2UYYOteoFtNCCLQ{WwQVAvODBzOTFOwG0> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOwPUc,OTJzOUCzNFk9N2F-
COS-7 monkey cells NVnuWJlITnWwY4Tpc44h[XO|YYm= M2PPUmlvcGmkaYTpcochfGinIH\hdo5me3muYYTpc44hd2ZiSD3yZZMheHKxdHXpcpMhcW5iQ1;TMVchdW:wa3X5JINmdGy|IITyZY5{cWWwdHz5JIV5eHKnc4PpcochUC2{YYPbWoFtOTKfLVPWUHMhcW5idHjlJJdpd2ynIHPlcIwh[XO|YYmsJGlEPTB;MD6wNUDPxE1? M2XyUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl6MkK1OVgoRjl6MkK1OVg9N2F-
MCF-7 tumor cell line NED0ZmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XzUWNwdXCxdX7kJJdieyCvZXHzeZJm\CCob4KgbY5pcWKrdHnvckBw\iCPQ1[tO{B1fW2xcjDj[YxtKGyrbnWgbY4h[nKnYYP0JJVv\GW{IIPv[pQh[WejcjDhd5NigSxiSVO1NF0xNjB3IN88US=> NV3TWJFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUiyNlU2QCd-OUiyNlU2QDxxYU6=
HCT116 NWW3ZlMzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFe3[4hEd22yb4Xu[EB4[XNibXXhd5Vz\WRiZn;yJIlvcGmkaYTpc44hd2ZiSFPUNVE3KHS3bX;yJINmdGxibHnu[UBqdiClb3zvckB2dmSncjDzc4Z1KGGpYYKgZZN{[XluIFnDOVA:OC5yNzFOwG0> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86QDJ{NUW4K|46QDJ{NUW4QE9iRg>?
NIH-H tumor cell lines Mn;sS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{S3R2NwdXCxdX7kJIFjcWyrdImgeI8hcW6qaXLpeEBidmOqb4Lh[4UucW6mZYDlcoRmdnRiZ4Lve5RpKG:oIF7JTE1JKHS3bX;yJINmdGxibHnu[ZMhcW5ic3;meEBi\2G{LDDJR|UxRTBwMEeyJO69VQ>? M4DCbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl6MkK1OVgoRjl6MkK1OVg9N2F-
NIH3T3 cells MmTJSpVv[3Srb36gZZN{[Xl? NInYeVlKdmirYnn0bY9vKG:oIGLhd{Bn[XKwZYP5cIF1cW:wIHnuJGguWmG|IITyZY5{\m:{bXXkJG5KUDOWMzDj[YxteyxiRVO1NF0xNjFizszN M1u3SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3NEW0NlI5Lz5zNUS1OFIzQDxxYU6=
NIH-K tumor cell lines MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlexR49ueG:3bnSgZYJqdGm2eTD0c{BqdmirYnn0JIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIghd2ZiTlnIMWshfHWvb4KgZ4VtdCCuaX7ld{BqdiC|b3\0JIFo[XJuIFnDOVA:OC53IN88US=> MkjOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTh{MkW1PEc,QTh{MkW1PFww[T5?
Cos-1 MWDGeY5kfGmxbjDhd5NigQ>? NEnqPXNKdmirYnn0bY9vKG:oIGDyc5RmcW5iZnHycoV{gWy2cnHud4ZmemG|ZTDpckBEd3NvMTDtc45s\Xlia3nkcoV6KGOnbHzzJIV5eHKnc4PpcochUC2UYYOteoFtNCCLQ{WwJF0hOC5yMEG5JO69VS5? MkjzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJzOUCzNFkoRjF{MUmwN|A6RC:jPh?=
Cos-1 M4r5XGZ2dmO2aX;uJIF{e2G7 M4DrSGVn\mWldDDvckBT[XNicILvZ4V{e2mwZzDpckBEd3NvMTDtc45s\Xlia3nkcoV6KGOnbHzzJIV5eHKnc4Ppcoch\Wm2aHXyJGguWmG|LW\hcEAyOi2FVlzTJI9zKEhvUnHzMXZidDF{LDDJR|UxKD1iMD6wNUDPxE1w MojZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB2MUG0PFUoRjFyNEGxOFg2RC:jPh?=
COS7 NGfXN3JHfW6ldHnvckBie3OjeR?= MofOTY5pcWKrdHnvckBw\iCIVHHz[UBqdiCqdX3hckBEV1N5IHPlcIx{NCCLQ{WwJF0hOC5yMTFOwG0v M2fLOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOUK1OFM{Lz5{MEmyOVQ{OzxxYU6=
H-Ras transformed cells NEfGZ4RHfW6ldHnvckBie3OjeR?= NYTvVoFzUW6qaXLpeIlwdiCxZjDzc4Z1KGGpYYKgZ49td267IH\vdo1ifGmxbjDpckBJNVKjczD0doFve2[xcn3l[EBk\WyuczygTWM2OCB;IECuNFch|ryPLh?= NUTpWW83RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW1NFExPjVpPkG1OVAyODZ3PD;hQi=>
NIH3T3 MlrySpVv[3Srb36gZZN{[Xl? NXjHS3NuTW[oZXP0bZZmKGOxbnPlcpRz[XSrb36gZYdicW6|dDDIZU1TSVNicILvZ4V{e2mwZzDpckBPUUh|VEOgdoF{NXS{YX7z[o9zdWWmIHPlcIx{NCCHQ{WwJF0hOC5zNjFOwG0v M2rWUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{NkW3Nlg1Lz5zMk[1O|I5PDxxYU6=
NIH3T3 M2DWcWZ2dmO2aX;uJIF{e2G7 Mk[4WHBgXFKDTmPQU3JVTVJ8IHnubIljcXSrb36gc4YhTE6UIHXm[ox2gCBqRF7SPkA0KHWPKTDpckBOTFJzLXX4dJJme3OrbnegUmlJO1R|IHPlcIx{NCCLQ{WwJF0hOi55IN88UU4> NF36S2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMU[wOlM5QSd-MUG2NFY{QDl:L3G+
A673 M2f1SZFJXFNiYYPzZZk> NGrje4RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MoH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
DAOY MofudWhVWyCjc4PhfS=> Ml\RdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? NWfXNYdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NFm4NlhyUFSVIHHzd4F6 NFnjeWlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz M1Xwb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 NHG0NXlyUFSVIHHzd4F6 NWHSZ2xPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz M3nOWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD NIDzO2pyUFSVIHHzd4F6 M{XQO5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? NE\sU449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 NGDMflNyUFSVIHHzd4F6 M{fyPJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) MoHidWhVWyCjc4PhfS=> MnjDdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NV3XW21tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NGLDUXZyUFSVIHHzd4F6 NHnPRoFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz Mnu5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 MoPXdWhVWyCjc4PhfS=> NULIUZo{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> MmLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NH3UR|ByUFSVIHHzd4F6 NVm1cYVZeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 M2PwTJFJXFNiYYPzZZk> M3ryZpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz NYXQUpc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NUDFelZZeUiWUzDhd5NigQ>? MoPKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 NGHyUHhyUFSVIHHzd4F6 NELENVRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NFzmXpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 M1\CbZFJXFNiYYPzZZk> NHzRUY5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= M1TLWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Caco-2 NWPHSG4yS3m2b4TvfIlkcXS7IHHzd4F6 M4nROlQ5KGixdYLz NHPIVoVF\XSncn3pcoF1cW:wIH;mJGlEPTBidnHseYV{KG[xcjDpcohq[mm2aX;uJI9nKFODUmOtR49XNTJiaX7keYNm\CCleYTveI95cWOrdImgc4YhS2Glbz2yJINmdGy|IHHmeIVzKDR6IHjveZJ{KGK7IHjp[4gh[2:wdHXueEBqdWGpaX7nMEBKSzVyIE2gOU43QCEQvF2u MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPVg4OzRxJ{7DbGVOSkx:L3G+
Caco-2 NIH5[otVd3irY3n0fUBie3OjeR?= M{PlSFQ5KGixdYLz MX\Uc5hq[2m2eTDh[4FqdnO2IFPhZ48uOiClZXzsd{Bl\XSncn3pcoVlKGG2IES4JIhwfXK|IHL5JIlvfHKjY3XscJVt[XJiQWTQJINwdmOnboTyZZRqd25idYPpcochfGinIFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO|YYmsJGNEPTBiPTCxNE44OSEQvF2u MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPVg4OzRxJ{7DbGVOSkx:L3G+
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

DMSO 127 mg/mL
(198.8 mM)
Water Insoluble
Ethanol '127 mg/mL

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 %

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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
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 2022-01-17)

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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