Lonafarnib (SCH66336)

目录号:S2797

仅限科研使用

Lonafarnib (SCH66336) 是一种口服生物有效的FPTase抑制剂,作用于H-rasK-ras-4BN-ras,无细胞试验中IC50分别为1.9 nM, 5.2 nM和2.8 nM。Phase 3。

Lonafarnib (SCH66336) Chemical Structure

CAS: 193275-84-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 3030.3 现货
RMB 1416.91 现货
RMB 4250.61 现货
RMB 10622.43 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Lonafarnib (SCH66336)发表文献17篇:

产品安全说明书

Transferase抑制剂选择性比较

生物活性

产品描述 Lonafarnib (SCH66336) 是一种口服生物有效的FPTase抑制剂,作用于H-rasK-ras-4BN-ras,无细胞试验中IC50分别为1.9 nM, 5.2 nM和2.8 nM。Phase 3。
靶点
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
体外研究

SCH66336在0.1 μM到8 μM浓度范围均可抑制头部和颈部鳞状细胞癌(HNSCC) 生长和诱导凋亡,抑制效果具有剂量和时间依赖性。SCH66336 (8 μM)可在SqCC/Y1细胞中抑制蛋白激酶B/Akt活性和磷酸化 Akt蛋白底物糖原合酶激酶(GSK)- 3β,转录叉因子和BAD[2]。SCH66336 对多细胞系有抗增殖作用,IC 50范围从0.6 μM 到32.3 μM [3] ; Lonafarnib诱导CCAAT /增强子结合蛋白同源蛋白(CHOP)依赖性DR5启动子的转录激活,从而诱导CHOP依赖性的DR5上调。Lonafarnib (< 10 μM) 可激活caspase - 8及其下游的半胱氨酸蛋白酶,从而诱导H1792细胞凋亡。Lonafarnib (5 μM)可增加DR5的细胞表面分布,增强肿瘤坏死因子相关凋亡诱导配体诱导的H1792细胞凋亡[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Cos-1 monkey kidney cells MX7GeY5kfGmxbjDhd5NigQ>? M1zOcWlvcGmkaYTpc44hd2ZiUILveIVqdiCoYYLu[ZN6dHS{YX7z[oVz[XOnIHnuJGNwey1zIH3vcotmgSCtaXTu[Zkh[2WubIOg[ZhxemW|c3nu[{BJNVKjcz32ZYwtKEmFNUC9NE4xODF7IN88US=> NXHPPG1oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUKxPVA{ODlpPkGyNVkxOzB7PD;hQi=>
COS-7 monkey cells MYnGeY5kfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX7nJJRp\SCoYYLu[ZN6dGG2aX;uJI9nKEhvcnHzJJBzd3SnaX7zJIlvKEORUz23JI1wdmuneTDj[YxteyC2cnHud4lmdnSueTDlfJBz\XO|aX7nJGguemG|W2\hcFEzZS2FVlzTJIlvKHSqZTD3bI9t\SClZXzsJIF{e2G7LDDJR|UxRTBwMEGg{txO M33oTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl6MkK1OVgoRjl6MkK1OVg9N2F-
MCF-7 tumor cell line M1;BeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUDDc41xd3WwZDD3ZZMhdWWjc4Xy[YQh\m:{IHnubIljcXSrb36gc4YhVUOILUegeJVud3JiY3XscEBtcW6nIHnuJIJz\WG|dDD1coRmeiC|b3\0JIFo[XJiYYPzZZktKEmFNUC9NE4xPSEQvF2= MmfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTh{MkW1PEc,QTh{MkW1PFww[T5?
HCT116 NF;hNmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXXDc41xd3WwZDD3ZZMhdWWjc4Xy[YQh\m:{IHnubIljcXSrb36gc4YhUEOWMUG2JJR2dW:{IHPlcIwhdGmwZTDpckBkd2yxbjD1coRmeiC|b3\0JIFo[XJiYYPzZZktKEmFNUC9NE4xPyEQvF2= NVyycmNORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUiyNlU2QCd-OUiyNlU2QDxxYU6=
NIH-H tumor cell lines Ml32S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfDc41xd3WwZDDhZoltcXS7IITvJIlvcGmkaYSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bEBw\iCQSVitTEB1fW2xcjDj[YxtKGyrbnXzJIlvKHOxZoSgZYdieixiSVO1NF0xNjB5MjFOwG0> M4Ps[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl6MkK1OVgoRjl6MkK1OVg9N2F-
NIH3T3 cells M3rHUWZ2dmO2aX;uJIF{e2G7 M1rPbmlvcGmkaYTpc44hd2ZiUnHzJIZiem6nc4nsZZRqd25iaX6gTE1T[XNidILhcpNnd3KvZXSgUmlJO1R|IHPlcIx{NCCHQ{WwQVAvOSEQvF2= NUTxdJVQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW0OVQzOjhpPkG1OFU1OjJ6PD;hQi=>
NIH-K tumor cell lines MoXOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1nUWGNwdXCxdX7kJIFjcWyrdImgeI8hcW6qaXLpeEBidmOqb4Lh[4UucW6mZYDlcoRmdnRiZ4Lve5RpKG:oIF7JTE1MKHS3bX;yJINmdGxibHnu[ZMhcW5ic3;meEBi\2G{LDDJR|UxRTBwNTFOwG0> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86QDJ{NUW4K|46QDJ{NUW4QE9iRg>?
Cos-1 NIfH[YVHfW6ldHnvckBie3OjeR?= M1nV[mlvcGmkaYTpc44hd2ZiUILveIVqdiCoYYLu[ZN6dHS{YX7z[oVz[XOnIHnuJGNwey1zIH3vcotmgSCtaXTu[Zkh[2WubIOg[ZhxemW|c3nu[{BJNVKjcz32ZYwtKEmFNUCgQUAxNjByMUmg{txONg>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF7MEOwPUc,OTJzOUCzNFk9N2F-
Cos-1 NEXtTZJHfW6ldHnvckBie3OjeR?= NV\Zb5ZXTW[oZXP0JI9vKFKjczDwdo9k\XO|aX7nJIlvKEOxcz2xJI1wdmuneTDrbYRv\XliY3XscJMh\XiycnXzd4lv\yCnaYTo[ZIhUC2UYYOtWoFtKDF{LVPWUHMhd3JiSD3SZZMuXmGuMUKsJGlEPTBiPTCwMlAyKM7:TT6= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODRzMUS4OUc,OTB2MUG0PFU9N2F-
COS7 MYnGeY5kfGmxbjDhd5NigQ>? MlXtTY5pcWKrdHnvckBw\iCIVHHz[UBqdiCqdX3hckBEV1N5IHPlcIx{NCCLQ{WwJF0hOC5yMTFOwG0v NXjZNlJCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC5NlU1OzNpPkKwPVI2PDN|PD;hQi=>
H-Ras transformed cells MoHISpVv[3Srb36gZZN{[Xl? NVTHR|lMUW6qaXLpeIlwdiCxZjDzc4Z1KGGpYYKgZ49td267IH\vdo1ifGmxbjDpckBJNVKjczD0doFve2[xcn3l[EBk\WyuczygTWM2OCB;IECuNFch|ryPLh?= NGOyWHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUWwNVA3PSd-MUW1NFExPjV:L3G+
NIH3T3 M4Xt[mZ2dmO2aX;uJIF{e2G7 NXfSfmlTTW[oZXP0bZZmKGOxbnPlcpRz[XSrb36gZYdicW6|dDDIZU1TSVNicILvZ4V{e2mwZzDpckBPUUh|VEOgdoF{NXS{YX7z[o9zdWWmIHPlcIx{NCCHQ{WwJF0hOC5zNjFOwG0v MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZ3N{K4OEc,OTJ4NUeyPFQ9N2F-
NIH3T3 M4fhfmZ2dmO2aX;uJIF{e2G7 NGfCWYJVWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCGTmKg[YZndHW6IDjEUnI7KD9idV2pJIlvKE2GUkGt[ZhxemW|c3nu[{BPUUh|VEOgZ4VtdHNuIFnDOVAhRSB{Lkeg{txONg>? M{WzV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzNkC2N|g6Lz5zMU[wOlM5QTxxYU6=
A673 NYLKXGFzeUiWUzDhd5NigQ>? M3zrN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY NUDGZ4w6eUiWUzDhd5NigQ>? NGToVHpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= NImwT3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 MWHxTHRUKGG|c3H5 MnHPdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NHHSfZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 NVPtR5BjeUiWUzDhd5NigQ>? MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD Ml3kdWhVWyCjc4PhfS=> M1nYbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? NIDE[GI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 Mly0dWhVWyCjc4PhfS=> MXrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? NWjqS4ZmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NXrySYJQeUiWUzDhd5NigQ>? NW\DZZV3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NWPQOJZrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M{nwcZFJXFNiYYPzZZk> NVfiSXVTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MXnxTHRUKGG|c3H5 M1PRPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NILjbGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 Mo\xdWhVWyCjc4PhfS=> MnXTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? MnWzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 NIHL[oxyUFSVIHHzd4F6 MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC M4e4d5FJXFNiYYPzZZk> MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= Mo\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 MUDxTHRUKGG|c3H5 Mof3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= NG\LXHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 NVfuflNReUiWUzDhd5NigQ>? NHPaeI1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= Mn\KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Caco-2 NYLsfZRHS3m2b4TvfIlkcXS7IHHzd4F6 M{HNSlQ5KGixdYLz M4SwVGRmfGW{bXnuZZRqd25ib3[gTWM2OCC4YXz1[ZMh\m:{IHnubIljcXSrb36gc4YhW0GUUz3Dc3YuOiCrbnT1Z4VlKGO7dH;0c5hq[2m2eTDv[kBE[WOxLUKgZ4VtdHNiYX\0[ZIhPDhiaH;1dpMh[nliaHnnbEBkd262ZX70JIlu[WerbnesJGlEPTBiPTC1MlY5KM7:TT6= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPVg4OzRxJ{7DbGVOSkx:L3G+
Caco-2 NHnPNWpVd3irY3n0fUBie3OjeR?= Mn2wOFghcG:3coO= NYTkdJRlXG:6aXPpeJkh[WejaX7zeEBE[WOxLUKgZ4VtdHNiZHX0[ZJucW6nZDDheEA1QCCqb4Xyd{BjgSCrboTyZYNmdGy3bHHyJGFVWCClb37j[Y51emG2aX;uJJV{cW6pIITo[UBE\WyuVHn0[ZIuT2yxIFz1cYlv\XOlZX70JGNmdGxiVnnhZoltcXS7IFHzd4F6NCCFQ{WwJF0hOTBwN{Gg{txONg>? NXzNO|kxRGFidHHy[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
体内研究 SCH66336 抑制HTBI77人肺癌裸鼠移植模型中的瘤生长,抑制作用呈剂量依赖性[1]。在NOD/SCID免疫缺陷小鼠皮下注射XEN01, XEN05或XEN08 GBM建立肿瘤移植模型,SCH66336 以 50 mg/kg剂量口服灌胃21天后,可抑制肿瘤生长,抑制率高达69%[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[2]
  • Cell lines: UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, 和UMSCC35, UMSCC38 细胞
  • Concentrations: 0.1 μM - 8 μM
  • Incubation Time: 24 小时
  • Method: 细胞铺板于96孔板中,后续培养5天,据此确定起始密度。24小时后,用不同浓度SCH66336处理细胞。SCH66336溶解于DMSO。对照组细胞用同样量的DMSO处理。5天后用SRB法检测细胞数量。生长抑制的百分比的计算公式为:增长抑制百分比=(1−/At/Ac)×100,At和Ac分别代表实验组和对照组的吸收值。IC 50值由剂量反应曲线确定。
动物实验:[3]
  • Animal Models: 6–12周龄NOD/SCID 小鼠
  • Dosages: 50 mg/kg
  • Administration: 口服

溶解度(25°C)

体外

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 638.82
化学式

C27H31Br2ClN4O2

CAS号 193275-84-2
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

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)

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