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 19 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 M3X2TmZ2dmO2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N Mlv1NlA1Ojl3MUG=
NIH3T3 cells MlT3SpVv[3Srb36gZZN{[Xl? NUjwPZNQUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? NWXWV5lQOTV7MUGyPFE>
human RPMI-6666 cell M4XFZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEP4[GNKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtOlY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdwNEGgcm0> NYLhO445W0GQR1XS
human ML-2 cell NWS5[3RtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3zOS2lvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlY1KG6P M2D0OHNCVkeHUh?=
human SIG-M5 cell MknDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{HFU2lvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTdibl2= NGfNe|RUSU6JRWK=
human QIMR-WIL cell MkXkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zxPWlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5|MTDuUS=> NWrX[G82W0GQR1XS
human A4-Fuk cell NGjwc|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3myUmlvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlAvPTlibl2= MmPGV2FPT0WU
human ETK-1 cell MnTMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFnR[2lKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTJibl2= NYTDZXJUW0GQR1XS
human MEL-JUSO cell NEjXWXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3\VVGlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVrVV28h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOy52NDDuUS=> NFS3UodUSU6JRWK=
human NALM-6 cell MlvhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVnJcohq[mm2aX;uJI9nKGi3bXHuJG5CVE1vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2MlIyKG6P Mne2V2FPT0WU
human IA-LM cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEeuOVIhdk1? MWDTRW5ITVJ?
human Daoy cell M3izNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVHFRnl1UW6qaXLpeIlwdiCxZjDoeY1idiCGYX;5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVcvPTNibl2= MmL5V2FPT0WU
human REH cell NWfDT|dnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJHJGUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV7LkKgcm0> MWXTRW5ITVJ?
human KU812 cell MonWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{mxNmlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{4xPiCwTR?= M1mzOHNCVkeHUh?=
human KM12 cell M3nhZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGO2coxKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=> M3jGT3NCVkeHUh?=
human LCLC-103H cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml;uTY5pcWKrdHnvckBw\iCqdX3hckBNS0yFLUGwN2gh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF{OUCyJO69VQ>? NILuemJUSU6JRWK=
human BC-1 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoDMTY5pcWKrdHnvckBw\iCqdX3hckBDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNlk6PiEQvF2= M1G0W3NCVkeHUh?=
human CMK cell NFjGRmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUWxOFUh|ryP Mn3zV2FPT0WU
human MCF7 cell NEHEPGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlG1TY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlY{KM7:TR?= M3fwSnNCVkeHUh?=
human Calu-1 cell NVnBeoVlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1PNeWlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDF|NDFOwG0> M2SzbXNCVkeHUh?=
human SK-LMS-1 cell NGO2[4VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MofQTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTh2MEmg{txO MWjTRW5ITVJ?
human HH cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUDSOVY3UW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVkxQDlizszN MUTTRW5ITVJ?
human NCI-H2122 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF;0SHpKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUmxOFUh|ryP M{PHdnNCVkeHUh?=
human SNG-M cell NIrlR2hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2fTV2lvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxOzV2IN88US=> MWnTRW5ITVJ?
human IGROV-1 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWjkU2g1UW6qaXLpeIlwdiCxZjDoeY1idiCLR2LPWk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MEiyN{DPxE1? NG\TWHBUSU6JRWK=
human KYSE-270 cell Mn\yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NITGdYFKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1? MVjTRW5ITVJ?
human NTERA-S-cl-D1 cell M3\NXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkL1TY5pcWKrdHnvckBw\iCqdX3hckBPXEWUQT3TMYNtNURzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yN|c1KM7:TR?= NH;W[FRUSU6JRWK=
human LoVo cell Mne1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX3ac3dtUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDB7MTFOwG0> NVPqd|B2W0GQR1XS
human MOLT-16 cell Mo\XS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4j4UWlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO M17ETHNCVkeHUh?=
human P30-OHK cell MmPlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1HOdmlvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjZ|OEig{txO M{LPb3NCVkeHUh?=
human HUTU-80 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1u1VGlvcGmkaYTpc44hd2ZiaIXtZY4hUFWWVT24NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjh3MEKg{txO Ml7MV2FPT0WU
human MIA-PaCa-2 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPtTGhKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh|ryP NFLkSHFUSU6JRWK=
human HCC2157 cell M4PpVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVvJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOzF4IN88US=> MVPTRW5ITVJ?
human HCT-15 cell MlfQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn7kTY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=> M135Z3NCVkeHUh?=
human 786-0 cell NHXBeVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnvYTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN MYXTRW5ITVJ?
human GDM-1 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NITCeYFKdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTJ|OTFOwG0> MVnTRW5ITVJ?
human NCI-H2009 cell NVXnbmJtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1HZS2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|NkOzOkDPxE1? MoTDV2FPT0WU
human TE-15 cell Mnz4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmT5TY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|Y1PjJizszN M33n[HNCVkeHUh?=
human NCI-H2342 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXvFSnZyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO3PVg{KM7:TR?= NYr0SJhkW0GQR1XS
human RT-112 cell NGjFSItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYXldVhwUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6MUe2JO6ddQ>? Mn3nV2FPT0WU
human HCC2998 cell MofTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWjGWldRUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|OESzOkDPxE1? NYSwS4pHW0GQR1XS
human HEL cell M{PtOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4j3[GlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zPVQ1QSEQvF2= MU\TRW5ITVJ?
human NMC-G1 cell M2\hZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzxe2RmUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUC1JO69VQ>? NUj4RXZ4W0GQR1XS
human 8505C cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\YbWlvcGmkaYTpc44hd2ZiaIXtZY4hQDVyNVOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ{OTB7IN88US=> M37aZnNCVkeHUh?=
human HLE cell Mmj5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTXO|hKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ5OTFizszN NFjMRW1USU6JRWK=
human KGN cell Mn;tS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWTEdYRZUW6qaXLpeIlwdiCxZjDoeY1idiCNR16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2OjR7IN88US=> NXy2T|A6W0GQR1XS
human EW-18 cell M3TTeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU[3PFFZUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDV5OUGg{txO MX\TRW5ITVJ?
human OCUB-M cell MojWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXrSGlKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDdzNkSg{txO M3zRVnNCVkeHUh?=
human SW620 cell NUTi[GRYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3zXWGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> NHfCSINUSU6JRWK=
human SK-MEL-2 cell MlHnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{nGOWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR6M{ezJO69VQ>? MkTMV2FPT0WU
human G-401 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHHsSYpKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42ODJ4MTFOwG0> NH;SXnFUSU6JRWK=
human HT-29 cell MknlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkPoTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVQ3PyEQvF2= NU\5do01W0GQR1XS
human A427 cell NXPhRXpIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?= MYTTRW5ITVJ?
human A375 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIDuSINKdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=> Mkj0V2FPT0WU
SNU-449 cell M2i3VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXSXHZPUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkK5OEDPxE1? M1PacXNCVkeHUh?=
human A431 cell NX65PWNLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2XQSmlvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlU2OzZizszN Mnn5V2FPT0WU
human NCI-H1299 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVvETIJPUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFEzQTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[5N|A5KM7:TR?= MYnTRW5ITVJ?
human SNU-423 cell MmGxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoOwTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0> NIrpPJRUSU6JRWK=
human SW1710 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TsVGlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjV3IN88US=> MYnTRW5ITVJ?
human KYSE-450 cell MoHaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFHudIxKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtOFUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55Mki4OUDPxE1? MYnTRW5ITVJ?

... 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]
+ Expand
  • 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]
+ Expand
  • 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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Mass Concentration Volume Molecular Weight

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

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID