Tipifarnib

For research use only.

Catalog No.S1453 Synonyms: R115777

27 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 27 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 MXTGeY5kfGmxbjDhd5NigQ>? NVvHNml7UW6qaXLpeIlwdiCxZjDyZZQhemWlb33ibY5idnRiUF\UJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGK7IIPjbY51cWyuYYTpc44heHKxeHntbZR6KGG|c3H5MEBKSzVyPUCuO{BvVQ>? MnjvNlA1Ojl3MUG=
NIH3T3 cells NEPzcIFHfW6ldHnvckBie3OjeR?= NE[zcnhKdmirYnn0bY9vKG:oIGLhd{Bxem:lZYPzbY5oKGmwIFitdoF{KHS{YX7z[o9zdWWmIF7JTFNVOyClZXzsd{BqdiCycnXz[Y5k\SCxZjDUbZBq\mG{bnniMEBGSzVyPUGuOkBvVQ>? NUPDWZk1OTV7MUGyPFE>
human RPMI-6666 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIPKPVBKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtOlY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdwNEGgcm0> M3zvSnNCVkeHUh?=
human ML-2 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVLJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>? MULTRW5ITVJ?
human SIG-M5 cell NXLTOYJGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNKTy2PNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlU4KG6P MWDTRW5ITVJ?
human QIMR-WIL cell M1L5TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVrJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvOzFibl2= NHrYfJZUSU6JRWK=
human A4-Fuk cell NX35R2NET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoLyTY5pcWKrdHnvckBw\iCqdX3hckBCPC2IdXugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNE42QSCwTR?= NH3kOWdUSU6JRWK=
human ETK-1 cell Mn7qS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlewTY5pcWKrdHnvckBw\iCqdX3hckBGXEtvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxMlUzKG6P MlfxV2FPT0WU
human MEL-JUSO cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NY\DSlF[UW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTnVUVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ|LkS0JI5O NYTlbIR7W0GQR1XS
human NALM-6 cell NXvnTG4{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF;0UlJKdmirYnn0bY9vKG:oIHj1cYFvKE6DTF2tOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM3NjJzIH7N MkX0V2FPT0WU
human IA-LM cell M4HMPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGXWcFBKdmirYnn0bY9vKG:oIHj1cYFvKEmDLVzNJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFcvPTJibl2= MnvlV2FPT0WU
human Daoy cell NGnNe4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFTSd4RKdmirYnn0bY9vKG:oIHj1cYFvKESjb4mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21O{42OyCwTR?= NEDudmdUSU6JRWK=
human REH cell NGHnZpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYfNNWJFUW6qaXLpeIlwdiCxZjDoeY1idiCURVigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PU4zKG6P NHy0VVdUSU6JRWK=
human KU812 cell Mn;5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmrXTY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3MlA3KG6P M{XIZXNCVkeHUh?=
human KM12 cell MoLxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zV[GlvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE3QDZizszN MWDTRW5ITVJ?
human LCLC-103H cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1e3TWlvcGmkaYTpc44hd2ZiaIXtZY4hVEOOQz2xNFNJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zMkmwNkDPxE1? M37GUnNCVkeHUh?=
human BC-1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGJENTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyPVk3KM7:TR?= MYTTRW5ITVJ?
human CMK cell MmfGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV:zRWhSUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=> NEjsXFBUSU6JRWK=
human MCF7 cell NWe0[YlGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXfJcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG2OlMh|ryP NHKxU4NUSU6JRWK=
human Calu-1 cell M4XxUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIT3V3VKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOThzM{Sg{txO MUXTRW5ITVJ?
human SK-LMS-1 cell M{jGVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NE\rOYlKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOESwPUDPxE1? M2rLR3NCVkeHUh?=
human HH cell NUPhTZVuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOUC4PUDPxE1? MVPTRW5ITVJ?
human NCI-H2122 cell NEn1NIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4WwTWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOUG0OUDPxE1? MUTTRW5ITVJ?
human SNG-M cell NXiybYd1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVPJcohq[mm2aX;uJI9nKGi3bXHuJHNPTy2PIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yNFM2PCEQvF2= NXyyRZJ{W0GQR1XS
human IGROV-1 cell M2HWOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWDI[5NUUW6qaXLpeIlwdiCxZjDoeY1idiCLR2LPWk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MEiyN{DPxE1? M4HSR3NCVkeHUh?=
human KYSE-270 cell M4jUSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1fZWGlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2yO|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJzNk[4JO69VQ>? MV7TRW5ITVJ?
human NTERA-S-cl-D1 cell NXX6Zll[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFv3XmJKdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{PzRizszN NGH6NGlUSU6JRWK=
human LoVo cell M1[0[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEnFd3ZKdmirYnn0bY9vKG:oIHj1cYFvKEyxVn:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1ODlzIN88US=> M3X3cXNCVkeHUh?=
human MOLT-16 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXjucnZuUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{NUiyN{DPxE1? NX7o[lVYW0GQR1XS
human P30-OHK cell MnnGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJHA{OC2RSFugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3Ozh6IN88US=> M4rRZ3NCVkeHUh?=
human HUTU-80 cell MkPyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFvXeVBKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ6NUCyJO69VQ>? MnTXV2FPT0WU
human MIA-PaCa-2 cell Mk\rS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHvRdnNKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh|ryP MoPaV2FPT0WU
human HCC2157 cell NUXYT|ZuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlXiTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MUW3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjNzNjFOwG0> MmPHV2FPT0WU
human HCT-15 cell NFr5O3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NInmZW5KdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ5MEWg{txO MkLYV2FPT0WU
human 786-0 cell M1zYPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{Pyd2lvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> NUi3fVdWW0GQR1XS
human GDM-1 cell NVW3RY5yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{jWNmlvcGmkaYTpc44hd2ZiaIXtZY4hT0SPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2OjN7IN88US=> M{HIVHNCVkeHUh?=
human NCI-H2009 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFXCOYNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlAxQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{[zN|Yh|ryP M3\jO3NCVkeHUh?=
human TE-15 cell NEHvNHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOlQ3OiEQvF2= M2TCfXNCVkeHUh?=
human NCI-H2342 cell MmPMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzd7OEOg{txO M4DNU3NCVkeHUh?=
human RT-112 cell NFfVVmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGL6eHdKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzhzN{[g{rxu NH\uSY5USU6JRWK=
human HCC2998 cell M2jxcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3ztcmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzh2M{[g{txO NXfSXY9CW0GQR1XS
human HEL cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHzScpBKdmirYnn0bY9vKG:oIHj1cYFvKEiHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|k1PDlizszN NFTWXW9USU6JRWK=
human NMC-G1 cell NXzwOGNQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFI2ODVizszN NYC4UVdYW0GQR1XS
human 8505C cell M3jhTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2T4[mlvcGmkaYTpc44hd2ZiaIXtZY4hQDVyNVOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ{OTB7IN88US=> NHjrdVVUSU6JRWK=
human HLE cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlPzTY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFEyKM7:TR?= Mlf6V2FPT0WU
human KGN cell NWDZXItYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXvJcohq[mm2aX;uJI9nKGi3bXHuJGtIViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEWyOFkh|ryP NVXxT|kxW0GQR1XS
human EW-18 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXTmNplOUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDV5OUGg{txO MX7TRW5ITVJ?
human OCUB-M cell MoTaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFTHeHJKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDdzNkSg{txO M{jPOXNCVkeHUh?=
human SW620 cell NEjpTYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37OWGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> M4jqdnNCVkeHUh?=
human SK-MEL-2 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDN5MzFOwG0> M3fQOnNCVkeHUh?=
human G-401 cell MlrxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPKW|lQUW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTB{NkGg{txO M37YTXNCVkeHUh?=
human HT-29 cell Mn\sS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61OFY4KM7:TR?= MX\TRW5ITVJ?
human A427 cell M{PBdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHW4[I5KdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU4QTF5IN88US=> NF3YUIZUSU6JRWK=
human A375 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmjMTY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62NVY1QCEQvF2= MWLTRW5ITVJ?
SNU-449 cell NHHae5BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGHzV4JKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20OFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ{Mkm0JO69VQ>? NH3zZnBUSU6JRWK=
human A431 cell NHzwN4pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHLGRVBKdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY2PTN4IN88US=> M3HKNHNCVkeHUh?=
human NCI-H1299 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH\2U2RKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVI6QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkmzNFgh|ryP MYXTRW5ITVJ?
human SNU-423 cell M4DZRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LKU2lvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzB2Nk[g{txO MlzNV2FPT0WU
human SW1710 cell MojrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|I2PSEQvF2= NVPtdJplW0GQR1XS
human KYSE-450 cell Mo\1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvNEWwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Ojh6NTFOwG0> M3vCSXNCVkeHUh?=

... 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