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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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 Mn63SpVv[3Srb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N NIjMdGczODR{OUWxNS=>
NIH3T3 cells NH3MPXVHfW6ldHnvckBie3OjeR?= NV3WPVZrUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? MmHjNVU6OTF{OEG=
human RPMI-6666 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3PjZ2lvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=> M{DvZnNCVkeHUh?=
human ML-2 cell M{C0[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX7aTJJ6UW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvPjRibl2= MoHDV2FPT0WU
human SIG-M5 cell M2TQSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUjhNYVCUW6qaXLpeIlwdiCxZjDoeY1idiCVSVetUVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53NzDuUS=> NWS0NWtQW0GQR1XS
human QIMR-WIL cell NEixNplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkT6TY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjNzIH7N MnjoV2FPT0WU
human A4-Fuk cell NWTs[mx3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVLJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlU6KG6P MVvTRW5ITVJ?
human ETK-1 cell NGXwdmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWDJcohq[mm2aX;uJI9nKGi3bXHuJGVVUy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkGuOVIhdk1? M3vM[XNCVkeHUh?=
human MEL-JUSO cell NUnGc4hCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4ewOGlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVrVV28h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOy52NDDuUS=> M{DHeHNCVkeHUh?=
human NALM-6 cell NGjURmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4njcGlvcGmkaYTpc44hd2ZiaIXtZY4hVkGOTT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|YvOjFibl2= M3XnOHNCVkeHUh?=
human IA-LM cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1THTWlvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20O{42OiCwTR?= Mn3EV2FPT0WU
human Daoy cell Mn7vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{CyZ2lvcGmkaYTpc44hd2ZiaIXtZY4hTGGxeTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUW3MlU{KG6P NEjKT29USU6JRWK=
human REH cell MonBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3PRZWlvcGmkaYTpc44hd2ZiaIXtZY4hWkWKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUmuNkBvVQ>? NH;GOpJUSU6JRWK=
human KU812 cell M1TkVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\pTY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3MlA3KG6P MYrTRW5ITVJ?
human KM12 cell M1LNU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIT3VHlKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=> MlfJV2FPT0WU
human LCLC-103H cell Ml\KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO NWfx[2VpW0GQR1XS
human BC-1 cell NHvIS2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;DeGlvcGmkaYTpc44hd2ZiaIXtZY4hSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVI6QTZizszN NXXXV5VlW0GQR1XS
human CMK cell NVG2UW9ET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUWxOFUh|ryP NW\iXI81W0GQR1XS
human MCF7 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH[3eIVKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE3PjNizszN M2[zNHNCVkeHUh?=
human Calu-1 cell NWnzV2k5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4C1ZmlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDF|NDFOwG0> M2Wwb3NCVkeHUh?=
human SK-LMS-1 cell NEfpfIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDRyOTFOwG0> MUXTRW5ITVJ?
human HH cell NWPkSlFNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOUC4PUDPxE1? M3XiSXNCVkeHUh?=
human NCI-H2122 cell M2DQdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXzOcXpzUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= NYHlW44{W0GQR1XS
human SNG-M cell NHvHXpRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVLhTYw4UW6qaXLpeIlwdiCxZjDoeY1idiCVTletUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB|NUSg{txO NX3yRZQzW0GQR1XS
human IGROV-1 cell NYXEW41MT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGSyO4RKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? NFPKUJdUSU6JRWK=
human KYSE-270 cell NYH4WZZpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWT6RZZvUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVI4OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkG2Olgh|ryP NUfUXoM6W0GQR1XS
human NTERA-S-cl-D1 cell NFj5NYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVq2UHk5UW6qaXLpeIlwdiCxZjDoeY1idiCQVFXSRU1UNWOuLVSxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOzd2IN88US=> M1Wzc3NCVkeHUh?=
human LoVo cell MoPXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHpTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFA6OSEQvF2= M4KzOnNCVkeHUh?=
human MOLT-16 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3m2VGlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO M3ftcXNCVkeHUh?=
human P30-OHK cell NVezPFJGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHA{OC2RSFugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3Ozh6IN88US=> M174XXNCVkeHUh?=
human HUTU-80 cell MlHHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKGi3bXHuJGhWXFVvOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI5PTB{IN88US=> M4n6XnNCVkeHUh?=
human MIA-PaCa-2 cell NGj3NFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mk\oTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkC0JO69VQ>? NWK3cXRJW0GQR1XS
human HCC2157 cell NVrBcJJTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M37xeWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkG1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ|MU[g{txO M4\Gc3NCVkeHUh?=
human HCT-15 cell Mn6yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoT6TY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=> NVTGS4tlW0GQR1XS
human 786-0 cell M{[wVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nSd2lvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> MlrSV2FPT0WU
human GDM-1 cell NUW5fo5ZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1LnT2lvcGmkaYTpc44hd2ZiaIXtZY4hT0SPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2OjN7IN88US=> NHm0[oVUSU6JRWK=
human NCI-H2009 cell Mk\KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2TDfmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|NkOzOkDPxE1? MWLTRW5ITVJ?
human TE-15 cell NWDNWmhvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkHaTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|Y1PjJizszN M4XxSHNCVkeHUh?=
human NCI-H2342 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4P6fWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|N{m4N{DPxE1? MVzTRW5ITVJ?
human RT-112 cell MlfQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVHyUIo1UW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6MUe2JO6ddQ>? MYjTRW5ITVJ?
human HCC2998 cell NIXZfZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlrJTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QDR|NjFOwG0> NFXwZ|ZUSU6JRWK=
human HEL cell MmXOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m0OFkh|ryP MonQV2FPT0WU
human NMC-G1 cell Moq5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1nITGlvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjVyNTFOwG0> M1G4PHNCVkeHUh?=
human 8505C cell M2PuU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzvOmV[UW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO MXPTRW5ITVJ?
human HLE cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNES4NVEh|ryP NFzlRnZUSU6JRWK=
human KGN cell MnTlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHnPcGRKdmirYnn0bY9vKG:oIHj1cYFvKEuJTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFUzPDlizszN NWPoe|cyW0GQR1XS
human EW-18 cell NV;tTFFKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHfLRW1KdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PTd7MTFOwG0> NWiyR457W0GQR1XS
human OCUB-M cell NU\yeHBQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mk\XTY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4OTZ2IN88US=> MX7TRW5ITVJ?
human SW620 cell Mon5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1nMe2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> NYXGfVF[W0GQR1XS
human SK-MEL-2 cell Mn;1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDN5MzFOwG0> NHzPNotUSU6JRWK=
human G-401 cell M3nMXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJGcuPDBzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61NFI3OSEQvF2= MkPJV2FPT0WU
human HT-29 cell M4rqV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3fPWWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU1PjdizszN NUPkW3U5W0GQR1XS
human A427 cell NYL6PJhLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?= MmjMV2FPT0WU
human A375 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlPCTY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62NVY1QCEQvF2= MlrIV2FPT0WU
SNU-449 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYzOjl2IN88US=> M1;uS3NCVkeHUh?=
human A431 cell MnToS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGHBUnlKdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY2PTN4IN88US=> M1TxfXNCVkeHUh?=
human NCI-H1299 cell NIfWVldIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkmzTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGyPVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ7M{C4JO69VQ>? MVfTRW5ITVJ?
human SNU-423 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljhTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0> Moe5V2FPT0WU
human SW1710 cell NH32ZoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEnBT|JKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ3NTFOwG0> MYXTRW5ITVJ?
human KYSE-450 cell NGDqTXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV;rVWFWUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{K4PFUh|ryP NILoVpJUSU6JRWK=

... 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

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