Tipifarnib

For research use only.

Catalog No.S1453 Synonyms: R115777

25 publications

Tipifarnib  Chemical Structure

CAS No. 192185-72-1

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 25 publications

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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 MmLRSpVv[3Srb36gZZN{[Xl? NF34RnNKdmirYnn0bY9vKG:oIILheEBz\WOxbXLpcoFvfCCSRmSg[ZhxemW|c3XkJIlvKGmwc3XjeEBU\jliY3XscJMh[nlic3PpcpRqdGyjdHnvckBxem:6aX3peJkh[XO|YYmsJGlEPTB;MD63JI5O NVK0bHQ2OjB2Mkm1NVE>
NIH3T3 cells MonOSpVv[3Srb36gZZN{[Xl? MoTuTY5pcWKrdHnvckBw\iCUYYOgdJJw[2W|c3nu[{BqdiCKLYLhd{B1emGwc3\vdo1m\CCQSVizWFMh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiVHnwbYZiem6rYjygSWM2OD1zLk[gcm0> MYGxOVkyOTJ6MR?=
human RPMI-6666 cell NUDUd4tbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2r6SWlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=> M1jaPXNCVkeHUh?=
human ML-2 cell NIG5OGpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH3qPFRKdmirYnn0bY9vKG:oIHj1cYFvKE2OLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{43PCCwTR?= NUfHO2VqW0GQR1XS
human SIG-M5 cell NWHwV3dST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4DWOWlvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTdibl2= MX;TRW5ITVJ?
human QIMR-WIL cell M{HXW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUnh[JB5UW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkOxJI5O NEHl[ZFUSU6JRWK=
human A4-Fuk cell NH7RUpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIf5RoRKdmirYnn0bY9vKG:oIHj1cYFvKEF2LV\1b{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIxNjV7IH7N NYe1elNpW0GQR1XS
human ETK-1 cell M1HQZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrX[plKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTJibl2= M4rYNHNCVkeHUh?=
human MEL-JUSO cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIP0Z|FKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3KWXNQKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwNESgcm0> NV\hNI0xW0GQR1XS
human NALM-6 cell NW\hZXNVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKGi3bXHuJG5CVE1vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2MlIyKG6P NHL1bFBUSU6JRWK=
human IA-LM cell M{mwXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEeuOVIhdk1? Mkn3V2FPT0WU
human Daoy cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKGi3bXHuJGRid3liY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Nz61N{BvVQ>? MoPYV2FPT0WU
human REH cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmrhTY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O NHi0RY9USU6JRWK=
human KU812 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{XpVWlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{4xPiCwTR?= NX7D[ndUW0GQR1XS
human KM12 cell NHvSUGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;qfmlvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE3QDZizszN Mn7LV2FPT0WU
human LCLC-103H cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO MW\TRW5ITVJ?
human BC-1 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXnT[llDUW6qaXLpeIlwdiCxZjDoeY1idiCEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOjl7NjFOwG0> NIHWV5BUSU6JRWK=
human CMK cell M2CwRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHMWFNQUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=> NX7WenU1W0GQR1XS
human MCF7 cell NXKzdVJQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3S5fGlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVY3OyEQvF2= NIrEVWVUSU6JRWK=
human Calu-1 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGi5OVdKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOThzM{Sg{txO NXX5fG9sW0GQR1XS
human SK-LMS-1 cell NW\WfZJLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDRyOTFOwG0> NUSyboJxW0GQR1XS
human HH cell NV;KdWlTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHXZVYRKdmirYnn0bY9vKG:oIHj1cYFvKEiKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xPVA5QSEQvF2= NUD4SoQxW0GQR1XS
human NCI-H2122 cell M3e5bGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\TdYx1UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= NHLSOotUSU6JRWK=
human SNG-M cell MmHyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIrqNIJKdmirYnn0bY9vKG:oIHj1cYFvKFOQRz3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODN3NDFOwG0> MYHTRW5ITVJ?
human IGROV-1 cell MonnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI[0NlFKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? MVXTRW5ITVJ?
human KYSE-270 cell NHXxZWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMkewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOTZ4ODFOwG0> MYTTRW5ITVJ?
human NTERA-S-cl-D1 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVrJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKzO|Qh|ryP NHHIUmZUSU6JRWK=
human LoVo cell M3T2Z2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0NFkyKM7:TR?= NH3Nd3dUSU6JRWK=
human MOLT-16 cell NIf3dXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWPJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI2QDJ|IN88US=> MkKzV2FPT0WU
human P30-OHK cell MmX3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\vTY5pcWKrdHnvckBw\iCqdX3hckBROzBvT1jLJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPjN6ODFOwG0> MXLTRW5ITVJ?
human HUTU-80 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mo\tTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQDVyMjFOwG0> MWXTRW5ITVJ?
human MIA-PaCa-2 cell MnXES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XRdGlvcGmkaYTpc44hd2ZiaIXtZY4hVUmDLWDhR4EuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{KwOEDPxE1? M3SzOnNCVkeHUh?=
human HCC2157 cell NVG5SmU6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{XxPWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkG1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ|MU[g{txO MXXTRW5ITVJ?
human HCT-15 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHfG[W1KdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ5MEWg{txO MojyV2FPT0WU
human 786-0 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXPrNFZwUW6qaXLpeIlwdiCxZjDoeY1idiB5OE[tNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJzN{Og{txO Mnm4V2FPT0WU
human GDM-1 cell NEPsWWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOVI{QSEQvF2= M2Di[HNCVkeHUh?=
human NCI-H2009 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVWzcodHUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxODliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2N|M3KM7:TR?= NHfCdZJUSU6JRWK=
human TE-15 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX;mWFF{UW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO Mn:2V2FPT0WU
human NCI-H2342 cell NV3QfHFGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnLHTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN5OUizJO69VQ>? MmrCV2FPT0WU
human RT-112 cell NWPUbHhOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2DxPWlvcGmkaYTpc44hd2ZiaIXtZY4hWlRvMUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QDF5NjFOoI0> NG\4VppUSU6JRWK=
human HCC2998 cell NXiyU3VKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM5PDN4IN88US=> MV7TRW5ITVJ?
human HEL cell Mk\4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;0b3ZKdmirYnn0bY9vKG:oIHj1cYFvKEiHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|k1PDlizszN NUTxbG9iW0GQR1XS
human NMC-G1 cell NYLiNYsxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mnr6TY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQzPTB3IN88US=> MnPxV2FPT0WU
human 8505C cell NXS1b5hnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHG0U4dKdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0> M4rRSHNCVkeHUh?=
human HLE cell M{nvfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGrLUmxKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ5OTFizszN NFLCWGpUSU6JRWK=
human KGN cell M4HwVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1\IXWlvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= MUXTRW5ITVJ?
human EW-18 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEO1XXZKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PTd7MTFOwG0> MkG3V2FPT0WU
human OCUB-M cell MofnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvGXIdnUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2XCMW0h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR5MU[0JO69VQ>? NUnFNYhlW0GQR1XS
human SW620 cell MkK0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjFVpVKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDJ{NDFOwG0> NVPPSpM3W0GQR1XS
human SK-MEL-2 cell M{PLNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlXVTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDh|N{Og{txO MWPTRW5ITVJ?
human G-401 cell M4e0[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzWcZFEUW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTB{NkGg{txO NHTHUY5USU6JRWK=
human HT-29 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHTrOnVKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42PDZ5IN88US=> M2T3cXNCVkeHUh?=
human A427 cell MnqyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzhNppXUW6qaXLpeIlwdiCxZjDoeY1idiCDNEK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42PzlzNzFOwG0> NGDieXJUSU6JRWK=
human A375 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnLzTY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62NVY1QCEQvF2= MVzTRW5ITVJ?
SNU-449 cell NV[5dGptT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nsSGlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUS0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjJ{OUSg{txO M3G5XHNCVkeHUh?=
human A431 cell NGrzd|JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1q2eWlvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlU2OzZizszN MY\TRW5ITVJ?
human NCI-H1299 cell M{\DR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoPqTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGyPVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ7M{C4JO69VQ>? NHHqRmFUSU6JRWK=
human SNU-423 cell NYq5VlVlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M33CV2lvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzB2Nk[g{txO M4jWc3NCVkeHUh?=
human SW1710 cell NGrNWpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|I2PSEQvF2= MWPTRW5ITVJ?
human KYSE-450 cell NXHidmNzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MorJTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ6OEWg{txO M4fFdXNCVkeHUh?=

... 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]
- Collapse
  • 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
  • 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 CN1C=NC=C1C(C2=CC=C(C=C2)Cl)(C3=CC4=C(C=C3)N(C(=O)C=C4C5=CC(=CC=C5)Cl)C)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04284774 Recruiting Drug: Tipifarnib Recurrent Adrenal Gland Pheochromocytoma|Recurrent Ectomesenchymoma|Recurrent Ependymoma|Recurrent Ewing Sarcoma|Recurrent Hepatoblastoma|Recurrent Kidney Wilms Tumor|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Glioma|Recurrent Medulloblastoma|Recurrent Melanoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Recurrent Rhabdoid Tumor of the Kidney|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Recurrent Thyroid Gland Carcinoma|Recurrent WHO Grade II Glioma|Refractory Adrenal Gland Pheochromocytoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Hepatoblastoma|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Glioma|Refractory Medulloblastoma|Refractory Melanoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdoid Tumor of the Kidney|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Refractory Thyroid Gland Carcinoma|Refractory WHO Grade II Glioma National Cancer Institute (NCI) July 13 2020 Phase 2
NCT03496766 Recruiting Drug: Tipifarnib Non Small Cell Lung Cancer Spanish Lung Cancer Group May 7 2018 Phase 2
NCT02807272 Active not recruiting Drug: Tipifarnib Leukemia Myelomonocytic Chronic Kura Oncology Inc. October 2016 Phase 2
NCT02779777 Terminated Drug: Tipifarnib Myelodysplastic Syndromes Kura Oncology Inc. May 2016 Phase 2

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID