Tipifarnib

For research use only. Not for use in humans.

Catalog No.S1453 Synonyms: R115777

22 publications

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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Selleck's Tipifarnib has been cited by 22 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 NIiwWpFHfW6ldHnvckBie3OjeR?= NXj1W|VpUW6qaXLpeIlwdiCxZjDyZZQhemWlb33ibY5idnRiUF\UJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGK7IIPjbY51cWyuYYTpc44heHKxeHntbZR6KGG|c3H5MEBKSzVyPUCuO{BvVQ>? MlLiNlA1Ojl3MUG=
NIH3T3 cells MXjGeY5kfGmxbjDhd5NigQ>? NVLIe2tYUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? NWD1SVVjOTV7MUGyPFE>
human RPMI-6666 cell MkHMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXXFVoRnUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVY3PjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD15LkSxJI5O M{f4XXNCVkeHUh?=
human ML-2 cell NXezdJYyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>? NEOy[WRUSU6JRWK=
human SIG-M5 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHycXBwUW6qaXLpeIlwdiCxZjDoeY1idiCVSVetUVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53NzDuUS=> MXjTRW5ITVJ?
human QIMR-WIL cell Mn\CS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF\BepFKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwM{Ggcm0> MYHTRW5ITVJ?
human A4-Fuk cell M2PTdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlU6KG6P M3fQdHNCVkeHUh?=
human ETK-1 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2rS[GlvcGmkaYTpc44hd2ZiaIXtZY4hTVSNLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU42OiCwTR?= M37ycnNCVkeHUh?=
human MEL-JUSO cell Mo\SS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPUUXFKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3KWXNQKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwNESgcm0> NVjD[VFVW0GQR1XS
human NALM-6 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXvqeVBCUW6qaXLpeIlwdiCxZjDoeY1idiCQQVzNMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Pi5{MTDuUS=> MXfTRW5ITVJ?
human IA-LM cell MmHNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEeuOVIhdk1? NEPXVotUSU6JRWK=
human Daoy cell NFfQbXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\xdYZyUW6qaXLpeIlwdiCxZjDoeY1idiCGYX;5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVcvPTNibl2= NGfzcpVUSU6JRWK=
human REH cell NWeycJhsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoT4TY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O MmfBV2FPT0WU
human KU812 cell Mn:zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\X[2lvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{4xPiCwTR?= NHrGeVBUSU6JRWK=
human KM12 cell NEjvV2ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLyTY5pcWKrdHnvckBw\iCqdX3hckBMVTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVY5PiEQvF2= Mn;VV2FPT0WU
human LCLC-103H cell M4e1SGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO MnPmV2FPT0WU
human BC-1 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4\ofmlvcGmkaYTpc44hd2ZiaIXtZY4hSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVI6QTZizszN MYTTRW5ITVJ?
human CMK cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUTMW4JGUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=> MW\TRW5ITVJ?
human MCF7 cell M371TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{PnNWlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVY3OyEQvF2= MX3TRW5ITVJ?
human Calu-1 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVgyOzRizszN NG\FephUSU6JRWK=
human SK-LMS-1 cell NHexcWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn;iTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTh2MEmg{txO Mlz1V2FPT0WU
human HH cell NYLIRmZ2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHm5SIJKdmirYnn0bY9vKG:oIHj1cYFvKEiKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xPVA5QSEQvF2= MVPTRW5ITVJ?
human NCI-H2122 cell NVPLOZgyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;ySmpVUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= MVXTRW5ITVJ?
human SNG-M cell M2rwbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1TIXmlvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxOzV2IN88US=> MXvTRW5ITVJ?
human IGROV-1 cell MnP1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIDDXoJKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? MnrzV2FPT0WU
human KYSE-270 cell NEL2UJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NG[xNotKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1? MmfNV2FPT0WU
human NTERA-S-cl-D1 cell NFfUZ4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;1UWlvcGmkaYTpc44hd2ZiaIXtZY4hVlSHUlGtV{1kdC2GMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlM4PCEQvF2= MVLTRW5ITVJ?
human LoVo cell NWDJeWFZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoSzTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFA6OSEQvF2= NVfYSoI2W0GQR1XS
human MOLT-16 cell NVjIWGJDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4D1cmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO NV:1WWF{W0GQR1XS
human P30-OHK cell NYSwWXNiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3zmWWlvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjZ|OEig{txO M3S0XnNCVkeHUh?=
human HUTU-80 cell NXXwWoxvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWjoNIRIUW6qaXLpeIlwdiCxZjDoeY1idiCKVWTVMVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{OEWwNkDPxE1? M{XYTXNCVkeHUh?=
human MIA-PaCa-2 cell NIT4XGpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVTvcY9QUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlA1KM7:TR?= MVrTRW5ITVJ?
human HCC2157 cell NUnhbWtUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnrTTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MUW3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjNzNjFOwG0> M2jwfHNCVkeHUh?=
human HCT-15 cell MlvDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoXhTY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=> MUPTRW5ITVJ?
human 786-0 cell NFjJbIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmTITY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN MmToV2FPT0WU
human GDM-1 cell MofZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NULzV29NUW6qaXLpeIlwdiCxZjDoeY1idiCJRF2tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzV{M{mg{txO NETuOG9USU6JRWK=
human NCI-H2009 cell NGr4ZmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ|M{[g{txO MXHTRW5ITVJ?
human TE-15 cell M4npemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3ThRmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM3PDZ{IN88US=> M4TTU3NCVkeHUh?=
human NCI-H2342 cell MnewS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLCTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN5OUizJO69VQ>? M{P6b3NCVkeHUh?=
human RT-112 cell M3vIV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEe2RXBKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzhzN{[g{rxu NXS1PIprW0GQR1XS
human HCC2998 cell NFTvRppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHP5cYxKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6NEO2JO69VQ>? NEPx[Y1USU6JRWK=
human HEL cell NFTxNXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnTDTY5pcWKrdHnvckBw\iCqdX3hckBJTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO5OFQ6KM7:TR?= NWL6O4E4W0GQR1XS
human NMC-G1 cell Mm\wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmDzTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQzPTB3IN88US=> NUfmfFVRW0GQR1XS
human 8505C cell NF23eXVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHT1NmNKdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0> NUfOWlJKW0GQR1XS
human HLE cell MlXxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUDrPHJGUW6qaXLpeIlwdiCxZjDoeY1idiCKTFWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDFzIN88US=> NE\IWXhUSU6JRWK=
human KGN cell NITsbXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M136XGlvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= MlvYV2FPT0WU
human EW-18 cell NHviUZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV7XcGlvUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDV5OUGg{txO MYLTRW5ITVJ?
human OCUB-M cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2S4b2lvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PzF4NDFOwG0> NFX5OWtUSU6JRWK=
human SW620 cell M4O2Rmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HOXGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> MVLTRW5ITVJ?
human SK-MEL-2 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn\1TY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDh|N{Og{txO NYPITVVNW0GQR1XS
human G-401 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUXETpByUW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTB{NkGg{txO NFe2PG5USU6JRWK=
human HT-29 cell MlXZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61OFY4KM7:TR?= MlfXV2FPT0WU
human A427 cell MoDYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHLoSWhKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU4QTF5IN88US=> MVvTRW5ITVJ?
human A375 cell NUG0[pJUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXLjRW9{UW6qaXLpeIlwdiCxZjDoeY1idiCDM{e1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OTZ2ODFOwG0> NYDTSYtUW0GQR1XS
SNU-449 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWDJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYzOjl2IN88US=> MlzFV2FPT0WU
human A431 cell M{LrOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEjNSlRKdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY2PTN4IN88US=> MW\TRW5ITVJ?
human NCI-H1299 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUK5PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjl|MEig{txO NXX4c4hxW0GQR1XS
human SNU-423 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHX3fYxKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjdyNE[2JO69VQ>? M4POb3NCVkeHUh?=
human SW1710 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NE[3[3NKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ3NTFOwG0> M4nBbXNCVkeHUh?=
human KYSE-450 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVHlV3dMUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{K4PFUh|ryP NFTLUlRUSU6JRWK=

... 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
Smiles C[N]1C=NC=C1C(N)(C2=CC=C(Cl)C=C2)C3=CC4=C(C=C3)N(C)C(=O)C=C4C5=CC(=CC=C5)Cl

Bio Calculators

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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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.

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID