Tipifarnib

Catalog No.S1453 Synonyms: R115777

Tipifarnib  Chemical Structure

Molecular Weight(MW): 489.4

Tipifarnib (R115777) is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3.

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In DMSO USD 620 In stock
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Cited by 21 Publications

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description Tipifarnib (R115777) is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3.
Features A potent and selective farnesyl protein transferase inhibitor with significant antitumor effects.
Targets
FTase [1]
0.6 nM
In vitro

Using Tipifarnib 5 μM for 72 hours, the percentage of apoptotic cells is significantly higher in drug-treated compared to DMSO-treated LGL T-cells. Using T-cells from healthy donors, Tipifarnib reduces the percentage of IFNγ-positive cells in a time-dependent manner. Tipifarnib reduces the amount of activated Ras in precipitates compared to DMSO. [2] Tipifarnib exerts selective in vitro toxicity against clonal MDS hematopoiesis at concentrations less than 10 nM the effect being more prominent in white cell progenitors. This action is not due to apoptosis induction as both normal and MDS progenitors displays equivalent DiOC3 and annexin V expression up to 72 hours after exposure to Tipifarnib. [3] Combining Tipifarnib with 10 nM 4-OH-tamoxifen in the presence of E2 reduces the IC50 8-fold from 400 to 50 nM. [4] Tipifarnib induces apoptosis in U937 cells. [5] In addition, Tipifarnib inhibits isolated human farnesyltransferase for a lamin B peptide and for the K-RasB peptide with IC50 of 0.86 nM and 7.9 nM, respectively. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells NV\Sd|JoTnWwY4Tpc44h[XO|YYm= NYTte48zUW6qaXLpeIlwdiCxZjDyZZQhemWlb33ibY5idnRiUF\UJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGK7IIPjbY51cWyuYYTpc44heHKxeHntbZR6KGG|c3H5MEBKSzVyPUCuO{BvVQ>? NYLpUW9xOjB2Mkm1NVE>
NIH3T3 cells MX3GeY5kfGmxbjDhd5NigQ>? NYXEfmtiUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? NFP3c3cyPTlzMUK4NS=>
human RPMI-6666 cell NEPXZXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3rsfGlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=> Mn3xV2FPT0WU
human ML-2 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3jNdGlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlY1KG6P NH72RplUSU6JRWK=
human SIG-M5 cell M2rLNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmXQTY5pcWKrdHnvckBw\iCqdX3hckBUUUdvTUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PyCwTR?= NHnubVZUSU6JRWK=
human QIMR-WIL cell MojES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHLw[FBKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwM{Ggcm0> MVXTRW5ITVJ?
human A4-Fuk cell NELBOGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDIbHBuUW6qaXLpeIlwdiCxZjDoeY1idiCDND3GeYsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOC53OTDuUS=> MoDUV2FPT0WU
human ETK-1 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfQ[XdKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTJibl2= MnG5V2FPT0WU
human MEL-JUSO cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEiycolKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3KWXNQKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwNESgcm0> Mlq4V2FPT0WU
human NALM-6 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkKwTY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk4zOSCwTR?= M1:2cnNCVkeHUh?=
human IA-LM cell M4ToTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX3QRoNxUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjV{IH7N M1O1SHNCVkeHUh?=
human Daoy cell Mn[wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWXW[WI6UW6qaXLpeIlwdiCxZjDoeY1idiCGYX;5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVcvPTNibl2= NX\QeIEzW0GQR1XS
human REH cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1;yW2lvcGmkaYTpc44hd2ZiaIXtZY4hWkWKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUmuNkBvVQ>? MofGV2FPT0WU
human KU812 cell MnTTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY\3WotrUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk4NjB4IH7N NVfFUGFvW0GQR1XS
human KM12 cell NH3YN4FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFG4OmFKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=> NGPxcY5USU6JRWK=
human LCLC-103H cell NFT4bWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO MVTTRW5ITVJ?
human BC-1 cell M1jLNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXLLbY81UW6qaXLpeIlwdiCxZjDoeY1idiCEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOjl7NjFOwG0> MonkV2FPT0WU
human CMK cell Mnn1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXy0VFVuUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=> NH\ObI1USU6JRWK=
human MCF7 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEX6eHRKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE3PjNizszN MlHSV2FPT0WU
human Calu-1 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGH1N3FKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOThzM{Sg{txO MmjUV2FPT0WU
human SK-LMS-1 cell NIPTco5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHLi[plKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOESwPUDPxE1? NEflUYFUSU6JRWK=
human HH cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljxTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUmwPFkh|ryP NWDCbZdoW0GQR1XS
human NCI-H2122 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVPXWm1KUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= NXfFcY1EW0GQR1XS
human SNG-M cell NHy3O2ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnvUTY5pcWKrdHnvckBw\iCqdX3hckBUVkdvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlA{PTRizszN NX7IU3FDW0GQR1XS
human IGROV-1 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKGi3bXHuJGlIWk:YLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxQDJ|IN88US=> NWXST4VXW0GQR1XS
human KYSE-270 cell M1TNe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIewbnpKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1? NWraRYhTW0GQR1XS
human NTERA-S-cl-D1 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGTTN4FKdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{PzRizszN M2\PXXNCVkeHUh?=
human LoVo cell NYDY[2NkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3z2OWlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQxQTFizszN MnLCV2FPT0WU
human MOLT-16 cell NVP5OFNST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{nZTmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO MkGxV2FPT0WU
human P30-OHK cell MmrQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJHA{OC2RSFugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3Ozh6IN88US=> Mn;JV2FPT0WU
human HUTU-80 cell MoS3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmHTTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQDVyMjFOwG0> Mmm0V2FPT0WU
human MIA-PaCa-2 cell MlHXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUi0T|l6UW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlA1KM7:TR?= MVLTRW5ITVJ?
human HCC2157 cell NH7SUYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOzF4IN88US=> MnvFV2FPT0WU
human HCT-15 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLYTY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=> MWLTRW5ITVJ?
human 786-0 cell NHe4[41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHrKTnNKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjF5MzFOwG0> NXr1N|FxW0GQR1XS
human GDM-1 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOVI{QSEQvF2= NFvVR5VUSU6JRWK=
human NCI-H2009 cell NH3DR3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXrDXG5lUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxODliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2N|M3KM7:TR?= M2WzeHNCVkeHUh?=
human TE-15 cell NYKwb5djT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\6UnFmUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO M1LlWXNCVkeHUh?=
human NCI-H2342 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{fSdWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|N{m4N{DPxE1? M2e2[nNCVkeHUh?=
human RT-112 cell MnnuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|gyPzZizqzt MYnTRW5ITVJ?
human HCC2998 cell Ml\VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XKUmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzh2M{[g{txO NXXkNmtqW0GQR1XS
human HEL cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYDJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m0OFkh|ryP NYDZVZBtW0GQR1XS
human NMC-G1 cell M{LMSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3H2cGlvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjVyNTFOwG0> NGDPSoNUSU6JRWK=
human 8505C cell NIHtZVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEjqNHJKdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0> NWHWNFVqW0GQR1XS
human HLE cell M3:2RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3XLcmlvcGmkaYTpc44hd2ZiaIXtZY4hUEyHIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OFgyOSEQvF2= MX3TRW5ITVJ?
human KGN cell M17nUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2OzT2lvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= Mn7aV2FPT0WU
human EW-18 cell NH75bo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3HkUGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2PzlzIN88US=> NF;4PGpUSU6JRWK=
human OCUB-M cell M4PiT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTOO5dTUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2XCMW0h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR5MU[0JO69VQ>? Mn;5V2FPT0WU
human SW620 cell NVHZOnVUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1vKWGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> NX;YXId7W0GQR1XS
human SK-MEL-2 cell Mk\vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWTFNVFLUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEizO|Mh|ryP NXz3cG06W0GQR1XS
human G-401 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1S5cmlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> M2[wOXNCVkeHUh?=
human HT-29 cell NFzQbnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61OFY4KM7:TR?= NEXHZYtUSU6JRWK=
human A427 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVX5NnNvUW6qaXLpeIlwdiCxZjDoeY1idiCDNEK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42PzlzNzFOwG0> NH\ZbYZUSU6JRWK=
human A375 cell Ml30S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;oRVdKdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=> NXf6cWhrW0GQR1XS
SNU-449 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTmTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNES5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OjJ7NDFOwG0> NVfnc4ppW0GQR1XS
human A431 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mon2TY5pcWKrdHnvckBw\iCqdX3hckBCPDNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62OVU{PiEQvF2= MY\TRW5ITVJ?
human NCI-H1299 cell M{jnbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEnt[3JKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVI6QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkmzNFgh|ryP NU\aZlc3W0GQR1XS
human SNU-423 cell NI\OXVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmHOTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0> NFTlVGtUSU6JRWK=
human SW1710 cell NETtSnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|I2PSEQvF2= M3XhNXNCVkeHUh?=
human KYSE-450 cell Mk[wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLOTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ6OEWg{txO MlTSV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Caspase-12 / PARP1; 

PubMed: 21378206     


Western blot analysis of protein extracts from U937 cells incubated in normal media (Control) or media containing tipifarnib at the indicated concentrations. Extracts were probed using antibodies directed against cleaved caspase-12, PARP1 (full-length and cleaved), and β-actin, with the latter used as a lane loading reference. 

Rheb / p-mTOR / mTOR / p-P70S6K / P70 S6K / p-S6 / S6 ; 

PubMed: 23996484     


After U937 cells were treated for 24 h with the indicated tipifarnib concentration, whole cell lysates were subjected to immunoblotting with antibodies that recognize the indicated antigens. GAPDH served as a loading control. In this and subsequent figures, gray arrow indicates farnesylated antigen and black arrow indicates unfarnesylated antigen. 

Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Puma / Noxa / Bim / Lamin B; 

PubMed: 23996484     


After U937 cells were treated for 6 days with the indicated tipifarnib concentration, whole cell lysates were subjected to immunoblotting with antibodies that recognize the indicated polypeptides.

HDJ-2 / N-Ras / FKBP51 / p-AKT / AKT; 

PubMed: 23996484     


Whole cell lysates prepared from parental U937 cells treated for 48 h with diluent or 800 nM tipifarnib (lanes 2 and 3, respectively) or from tipifarnib-resistant cells growing in 800 nM tipifarnib (lane 1) were subjected to SDS-PAGE followed by immunoblotting with antibodies that recognize the indicated antigen.

p-c-Raf / c-Raf / p-MEK / MEK / p-ERK / ERK; 

PubMed: 21673341     


After Jurkat cells were treated for 72 hours with the indicated tipifarnib concentration in the presence of 5μM Q-VD-OPh, whole cell lysates were subjected to immunoblotting with antibodies that recognize the indicate polypeptides. Ribosomal protein S6 and Hsp90 served as loading controls. 

21378206 23996484 21673341
Growth inhibition assay
Cell viability; 

PubMed: 26630652     


NCI-H929, INA6, MM.1S, and RPMI-8226 MM cell lines were cultured with tipifarnib (0–20 μM), dabrafenib (0–20 μM), or AZD6244 (0–20 μM) for 72 h. In each case, cell viability was assessed with the MTT assay of triplicate cultures and expressed as the percentage of the untreated control. Data are the mean ± SD.

26630652
In vivo Ki-67 is lower in the tumors treated with E2 withdrawal plus R115777 compared with E2 withdrawal alone. The combination of tamoxifen and R115777 results in significantly lower Ki-67 compared with either tamoxifen or R115777 alone (mean of 5% versus 16.9% and 67.3%, respectively). [4] In contrast, no significant difference in apoptotic scores is seen between the treatment groups. R115777 alone also reduces the CTI compared with control. The combination of tamoxifen and R115777 or R115777 coupled with E2 withdrawal is most effective at lowering the CTI (0.8 and 0.7, respectively), which may account for the decrease in tumor volume. [4]

Protocol

Cell Research:[4]
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  • Cell lines: MACS-selected CD34+ cells
  • Concentrations: 2.5 nM, 10 nM, 25 nM and 50 nM
  • Incubation Time: 48 hours
  • Method: MACS-selected CD34+ cells are seeded in Methocult 4435 'complete' 1% bovine serum albumin, 3 U/mL recombinant human (rh) erythropoietin, 0.1 mM 2-mercaptoethanol, 2 mM L-glutamine and the following cytokines: 50 ng/mL rh stem cell factor, 20 ng/mL rh GM-CSF, 20 ng/mL rh IL-3, 20 ng/mL rh IL-6 and 20 ng/mL h G-CSF. DMSO or Tipifarnib is added at the concentrations of 2.5, 10, 25 and 50 nM at day 1. All cultures are performed in duplicates and the numbers of colonies are scored after 14 days of incubation at 37 °C in a humidified incubator containing 5% CO2(Only for Reference)
Animal Research:[4]
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  • Animal Models: Female ovariectomized Ncr foxhead nude mice
  • Formulation: 20% w/v β-cyclodextrin (pH 2.5)
  • Dosages: 50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 14 mg/mL (28.6 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
15% Captisol+citrate vehicle
For best results, use promptly after mixing.
5 mg/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 489.4
Formula

C27H22Cl2N4O

CAS No. 192185-72-1
Storage powder
in solvent
Synonyms R115777

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03496766 Recruiting Drug: Tipifarnib Non Small Cell Lung Cancer Spanish Lung Cancer Group May 7 2018 Phase 2
NCT02779777 Recruiting Drug: Tipifarnib Myelodysplastic Syndromes Kura Oncology Inc. May 2016 Phase 2
NCT00510939 Unknown status Drug: Tipifarnib plus Bortezomib Acute Myeloid Leukemia University of Bologna|Janssen-Cilag Ltd. March 2007 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

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID