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 NWTaPW5PTnWwY4Tpc44h[XO|YYm= NIe4WYxKdmirYnn0bY9vKG:oIILheEBz\WOxbXLpcoFvfCCSRmSg[ZhxemW|c3XkJIlvKGmwc3XjeEBU\jliY3XscJMh[nlic3PpcpRqdGyjdHnvckBxem:6aX3peJkh[XO|YYmsJGlEPTB;MD63JI5O M3\hflIxPDJ7NUGx
NIH3T3 cells M1PNfmZ2dmO2aX;uJIF{e2G7 MoPZTY5pcWKrdHnvckBw\iCUYYOgdJJw[2W|c3nu[{BqdiCKLYLhd{B1emGwc3\vdo1m\CCQSVizWFMh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiVHnwbYZiem6rYjygSWM2OD1zLk[gcm0> MlzJNVU6OTF{OEG=
human RPMI-6666 cell Mo[5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4LO[mlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=> MXTTRW5ITVJ?
human ML-2 cell M3j5fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWTJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>? MnHRV2FPT0WU
human SIG-M5 cell M4Tmemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNKTy2PNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlU4KG6P NIL3RVhUSU6JRWK=
human QIMR-WIL cell NXvFRmV[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVLIUmVZUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkOxJI5O MoLnV2FPT0WU
human A4-Fuk cell NXLEbZRwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{fuO2lvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlAvPTlibl2= MVjTRW5ITVJ?
human ETK-1 cell NF7xdmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXHlb3I6UW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV{IH7N M363[XNCVkeHUh?=
human MEL-JUSO cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MorqTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSmXTU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjR2IH7N NH73V2xUSU6JRWK=
human NALM-6 cell NXvSNlVST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoW1TY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk4zOSCwTR?= MUXTRW5ITVJ?
human IA-LM cell NFjuN49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXPuXlBUUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjV{IH7N NXH5NIdUW0GQR1XS
human Daoy cell NYHoTlBzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlzOTY5pcWKrdHnvckBw\iCqdX3hckBF[W:7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUeuOVMhdk1? MWrTRW5ITVJ?
human REH cell NX60V5JmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkLDTY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O NYjVV4RrW0GQR1XS
human KU812 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEHZUXlKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVcvODZibl2= MW\TRW5ITVJ?
human KM12 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXLzSZh1UW6qaXLpeIlwdiCxZjDoeY1idiCNTUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTZ6NjFOwG0> M2DoeXNCVkeHUh?=
human LCLC-103H cell M1f2fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUPudXc6UW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVExO0hiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyPVAzKM7:TR?= M{jqOnNCVkeHUh?=
human BC-1 cell Mne5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHfDZYdKdmirYnn0bY9vKG:oIHj1cYFvKEKFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEzQTl4IN88US=> MWrTRW5ITVJ?
human CMK cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUDGRpl2UW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=> M1L0OnNCVkeHUh?=
human MCF7 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml31TY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlY{KM7:TR?= NGC1fXBUSU6JRWK=
human Calu-1 cell NVXtV3FIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NG\adoFKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOThzM{Sg{txO NHjwUZpUSU6JRWK=
human SK-LMS-1 cell M36xXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIHvOoZKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOESwPUDPxE1? MWTTRW5ITVJ?
human HH cell MojPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PTcmlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NFg6KM7:TR?= MnvIV2FPT0WU
human NCI-H2122 cell NFHqTXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnVdHk2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= MVLTRW5ITVJ?
human SNG-M cell MoruS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3W5fWlvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxOzV2IN88US=> MXXTRW5ITVJ?
human IGROV-1 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWGwUIo5UW6qaXLpeIlwdiCxZjDoeY1idiCLR2LPWk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MEiyN{DPxE1? NIjWO3FUSU6JRWK=
human KYSE-270 cell NInpUlJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH7UO4VKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1? NF\DS5NUSU6JRWK=
human NTERA-S-cl-D1 cell NF3JPW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1fPOWlvcGmkaYTpc44hd2ZiaIXtZY4hVlSHUlGtV{1kdC2GMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlM4PCEQvF2= MlW1V2FPT0WU
human LoVo cell MofnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HIdmlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQxQTFizszN NGDnXo5USU6JRWK=
human MOLT-16 cell M13WN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFT0ZZNKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ3OEKzJO69VQ>? MYnTRW5ITVJ?
human P30-OHK cell NHnYdXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlXpTY5pcWKrdHnvckBw\iCqdX3hckBROzBvT1jLJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPjN6ODFOwG0> MVHTRW5ITVJ?
human HUTU-80 cell M1zWOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml\XTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQDVyMjFOwG0> MnrKV2FPT0WU
human MIA-PaCa-2 cell NF7ld5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH;NXmRKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh|ryP Ml7jV2FPT0WU
human HCC2157 cell NEX1dFRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3\1UmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkG1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ|MU[g{txO MWnTRW5ITVJ?
human HCT-15 cell NHjJRZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVnSTpN[UW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{N{C1JO69VQ>? NV[zc3F7W0GQR1XS
human 786-0 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoHiTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN MV3TRW5ITVJ?
human GDM-1 cell NX24WZFiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOVI{QSEQvF2= M2XPcXNCVkeHUh?=
human NCI-H2009 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ|M{[g{txO M1WzRnNCVkeHUh?=
human TE-15 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVrrR5BxUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO NXPsW2EzW0GQR1XS
human NCI-H2342 cell NVHTN4NOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M33MfGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|N{m4N{DPxE1? MkHyV2FPT0WU
human RT-112 cell M4PBfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH;ZVHZKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzhzN{[g{rxu NHmybHRUSU6JRWK=
human HCC2998 cell Mn7KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM5PDN4IN88US=> NWnhem5ZW0GQR1XS
human HEL cell M1yyeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4m1[mlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zPVQ1QSEQvF2= MWfTRW5ITVJ?
human NMC-G1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoT3TY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQzPTB3IN88US=> M2LIVHNCVkeHUh?=
human 8505C cell M1v3OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NESzbVZKdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0> NF:ydphUSU6JRWK=
human HLE cell NV3oWXNLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmnTTY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFEyKM7:TR?= NWH4bYZkW0GQR1XS
human KGN cell NF:yTZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3\FZmlvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= MlHPV2FPT0WU
human EW-18 cell MmnYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{P6RWlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2PzlzIN88US=> NVrVWYw3W0GQR1XS
human OCUB-M cell NVzxPIEyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIfsU5lKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDdzNkSg{txO MorjV2FPT0WU
human SW620 cell Mlm2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{iyN2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> Ml3WV2FPT0WU
human SK-MEL-2 cell M4L4Omdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFTKdm9KdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OEO3N{DPxE1? M4fNW3NCVkeHUh?=
human G-401 cell MoT6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4Dm[mlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> M1\6[XNCVkeHUh?=
human HT-29 cell Mnz1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PoWWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU1PjdizszN NFS1WFlUSU6JRWK=
human A427 cell MnnjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?= NHPiZYRUSU6JRWK=
human A375 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHT2NY1KdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=> MmnhV2FPT0WU
SNU-449 cell NUHifJROT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M37ZOGlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUS0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjJ{OUSg{txO M4[1[nNCVkeHUh?=
human A431 cell NXnpU3BwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M37nW2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlU2OzZizszN NHn6RmRUSU6JRWK=
human NCI-H1299 cell NYjnUJQ3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\Mem0zUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFEzQTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[5N|A5KM7:TR?= MXTTRW5ITVJ?
human SNU-423 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnO5TY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0> NF63ZVdUSU6JRWK=
human SW1710 cell MnPmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVO5bohlUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd{NUWg{txO MY\TRW5ITVJ?
human KYSE-450 cell M3TVb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnPJTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ6OEWg{txO NXznZoNqW0GQR1XS

... 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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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