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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6 Customer Reviews

  • Effect of the inhibition of mutated RAS on thyroid cancer cell response to gefitinib . C-643 (RAS mutated thyroid cancer cells) and BC-PAP (wild type RAS thyroid cancer cells) were seeded in 96-well plates and incubated with increasing doses of gefitinib (Gef.; 0.5, 1.0 , and 5.0 uM), the RAS inhibitor tipifarnib (0.1, 1.0 and 10 uM) or both for 48 hours. Cell viability was then measured by the MTT assay.

    J Clin Endocrinol Metab 2013 98(6), 2502-12. Tipifarnib purchased from Selleck.

    Effects of tipifarnib on GalN/LPS-induced mortality and ALF in mice. Representative liver histology (H/E staining at 5 h after saline or GalN/LPS) by microscopic images are shown.

    Shock 2014 42(6), 570-7. Tipifarnib purchased from Selleck.

  • Simvastatin/tipifarnib alters subcellular localization of RAS in human leukemia cells. Leukemia cells were treated with simvastatin (4 uM) and tipifarnib (1 uM), alone and in combination for 72hrs. Cytosolic and membrane fractions were prepared and western blot analysis was performed as described in the method section using the indicated antibodies. Calnexin was used as a membrane marker, whereas GAPDH is a marker of the cytosolic fraction. SIM, simvastatin. TIP, tipifarnib.

    Leuk Res 2014 10.1016/j.leukres.2014.09.002. Tipifarnib purchased from Selleck.

    Effects of FTIs on body weight and food intake in mice treated with LPV/RTV. (A) Treatment with LPV/RTV for 2 weeks significantly decreased body weight compared with vehicle alone. The effect of LPV/RTV on body weight was attenuated by FTIs: When the mice were co-treated with tipifarnib or lonafarnib, LPV/RTV failed to significantly decrease body weight. (B) LPV/RTV significantly increased food intake in the second week of the treatment compared with vehicle alone. FTIs prevented LPV/RTV-induced increased food intake. In the first week of the treatments, no significant difference in food intake between the groups was observed, although LPV/RTV tended to increase it. *P<0.05, **P<0.01 vs. LPV/RTV treatment, n=8 mice per group. FTI, farnesyltransferase inhibitor; LPV, lopinavir; RTV, ritonavir; NS, not significant.

    Exp Ther Med, 2018, 15(2):1314-1320. Tipifarnib purchased from Selleck.

  • The effects of SelleckChem inhibitors on sea urchin embryo development evaluated 24 h after fertilization. All compounds were added to embryos suspension 20 min after fertilization. The relative presence of late gastrula, swimming blastula, undeveloped embryos and dead embryos was compared next to untreated control embryos (A). Fertilized egg, swimming blastula and late gastrula are illustrated (B). The embryonic development was relatively synchronized in untreated control samples after 24 h (A, E). GSK690693 treatment sustained the development of embryos. Swimming blastulas kept normal motility regardless the deformities in their shape. Tipifarnib treatment induced significant toxicity due to occurrence of dead fragmented embryos. Some abnormal blastulas kept the motility. AZD2014 treatment sustained the development of embryos. Some developed gastrulas and blastulas were less motile in comparison with control (A, C). WZ811 was the least toxic compound. Significant number of gastrulas and blastulas was developed. However, their motility was considerably suppressed (A, D). In contrast to SelleckChem inhibitors, classic anticancer agent – cisplatin was extremely toxic to sea urchin embryos (A). Cisplatin killed many embryos, while a small amount of survived embryos was stopped at early phases of development: immediately after fertilization or after first and second division (A, F).

    Dr. Milica Pesic from Institute for Biological Research. Tipifarnib purchased from Selleck.

     

    WZ 811 and Tipifarnib inhibit the cell growth of anaplastic thyroid carcinoma cell lines (FRO and SW1736). There is no difference in sensitivity of tested cell lines to WZ 811, while FRO cells are more sensitive to Tipifarnib in comparison with SW1736 cells. Both cell lines are p53 null. FRO cells possess mutated HRas and SW1736 cells possess mutated BRaf.

    Tipifarnib purchased from Selleck.

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 NY\5NnBsTnWwY4Tpc44h[XO|YYm= NXjk[2NQUW6qaXLpeIlwdiCxZjDyZZQhemWlb33ibY5idnRiUF\UJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGK7IIPjbY51cWyuYYTpc44heHKxeHntbZR6KGG|c3H5MEBKSzVyPUCuO{BvVQ>? NGjSdm8zODR{OUWxNS=>
NIH3T3 cells Ml7ZSpVv[3Srb36gZZN{[Xl? NX\qZpZEUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? NU[yWWFbOTV7MUGyPFE>
human RPMI-6666 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH3kW29KdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtOlY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdwNEGgcm0> NX;JTG5UW0GQR1XS
human ML-2 cell M4fUTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVvJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>? M2XyW3NCVkeHUh?=
human SIG-M5 cell M3jDW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4Sxc2lvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTdibl2= MXTTRW5ITVJ?
human QIMR-WIL cell NUj4cXh4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvOzFibl2= M1zSVHNCVkeHUh?=
human A4-Fuk cell M2T2Vmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3XGTGlvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlAvPTlibl2= Ml;lV2FPT0WU
human ETK-1 cell MlyyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTs[3JKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTJibl2= M4\YdnNCVkeHUh?=
human MEL-JUSO cell NGHzV4ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MljCTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSmXTU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjR2IH7N MkCxV2FPT0WU
human NALM-6 cell NUXZVo11T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3jsXWlvcGmkaYTpc44hd2ZiaIXtZY4hVkGOTT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|YvOjFibl2= NEH6WnBUSU6JRWK=
human IA-LM cell NUDxR4xNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEeuOVIhdk1? M1nKOXNCVkeHUh?=
human Daoy cell NFOzOmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXzJcohq[mm2aX;uJI9nKGi3bXHuJGRid3liY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Nz61N{BvVQ>? NHS3XZVUSU6JRWK=
human REH cell NHLhSmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2O4RmlvcGmkaYTpc44hd2ZiaIXtZY4hWkWKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUmuNkBvVQ>? MUTTRW5ITVJ?
human KU812 cell NVHBZ2lDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2[xcGlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{4xPiCwTR?= MX;TRW5ITVJ?
human KM12 cell NV[3TINiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGxOlg3KM7:TR?= MWPTRW5ITVJ?
human LCLC-103H cell NEjsTmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnm0TY5pcWKrdHnvckBw\iCqdX3hckBNS0yFLUGwN2gh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF{OUCyJO69VQ>? Ml3SV2FPT0WU
human BC-1 cell NHvvfYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1yxbmlvcGmkaYTpc44hd2ZiaIXtZY4hSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVI6QTZizszN M1vF[XNCVkeHUh?=
human CMK cell Mn:yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIfQTIlKdmirYnn0bY9vKG:oIHj1cYFvKEOPSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVUyPDVizszN NYDBVnJ2W0GQR1XS
human MCF7 cell NGm2cnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG2OlMh|ryP NFzJU2NUSU6JRWK=
human Calu-1 cell M{LMbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MonFTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE5OTN2IN88US=> NXy0Z3ExW0GQR1XS
human SK-LMS-1 cell NF3sOYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDRyOTFOwG0> Mo\MV2FPT0WU
human HH cell M{HTdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEntZWxKdmirYnn0bY9vKG:oIHj1cYFvKEiKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xPVA5QSEQvF2= NVPue5hZW0GQR1XS
human NCI-H2122 cell MljYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfPdJk4UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= NV3GbmgyW0GQR1XS
human SNG-M cell MlLtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFrTN3RKdmirYnn0bY9vKG:oIHj1cYFvKFOQRz3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODN3NDFOwG0> NUDUVoJ[W0GQR1XS
human IGROV-1 cell M1vF[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4\Z[WlvcGmkaYTpc44hd2ZiaIXtZY4hUUeUT2[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB6MkOg{txO NH2yNZBUSU6JRWK=
human KYSE-270 cell NGWzXnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWrkU2d1UW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVI4OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkG2Olgh|ryP NVfQdJI5W0GQR1XS
human NTERA-S-cl-D1 cell Ml3MS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGK3bmRKdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{PzRizszN NH\KbFlUSU6JRWK=
human LoVo cell NH\WbJNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDTdIZ1UW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDB7MTFOwG0> NYHGcHpTW0GQR1XS
human MOLT-16 cell NGPEUHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmDKTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPTh{MzFOwG0> M{HoNHNCVkeHUh?=
human P30-OHK cell MnnWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2K2XmlvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjZ|OEig{txO MWrTRW5ITVJ?
human HUTU-80 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGhWXFVvOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI5PTB{IN88US=> M{DVcHNCVkeHUh?=
human MIA-PaCa-2 cell NEOz[5hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{MESg{txO NFLMXFlUSU6JRWK=
human HCC2157 cell MmTmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGm5TFNKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{KxOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{M{G2JO69VQ>? M4rY[3NCVkeHUh?=
human HCT-15 cell M4rYN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|I4ODVizszN M4rWSXNCVkeHUh?=
human 786-0 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGizeHdKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjF5MzFOwG0> MYrTRW5ITVJ?
human GDM-1 cell NVHMR|VGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXPxd2I4UW6qaXLpeIlwdiCxZjDoeY1idiCJRF2tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzV{M{mg{txO NEnNcppUSU6JRWK=
human NCI-H2009 cell M172SGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmG3TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN4M{O2JO69VQ>? M3LDcXNCVkeHUh?=
human TE-15 cell M3fuXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXfLRZVDUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO MUHTRW5ITVJ?
human NCI-H2342 cell M4j6cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUP3cZMxUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO3PVg{KM7:TR?= NGrKU4lUSU6JRWK=
human RT-112 cell NEjZenZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|gyPzZizqzt MkjPV2FPT0WU
human HCC2998 cell MlPtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUXNWpl{UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|OESzOkDPxE1? MnfiV2FPT0WU
human HEL cell NU[2WVJFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH3pNGZKdmirYnn0bY9vKG:oIHj1cYFvKEiHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|k1PDlizszN M3vITnNCVkeHUh?=
human NMC-G1 cell NYT3NJdzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYroUHN7UW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUC1JO69VQ>? MnH2V2FPT0WU
human 8505C cell NGHVSIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnz0TY5pcWKrdHnvckBw\iCqdX3hckA5PTB3QzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFMyODlizszN MoP1V2FPT0WU
human HLE cell NE[0NY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NY\aZ3VCUW6qaXLpeIlwdiCxZjDoeY1idiCKTFWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDFzIN88US=> M2S2TnNCVkeHUh?=
human KGN cell NInENFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXnJcohq[mm2aX;uJI9nKGi3bXHuJGtIViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEWyOFkh|ryP NVHTVVQ5W0GQR1XS
human EW-18 cell NH;ZVYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFn0e|JKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PTd7MTFOwG0> NHXlPJNUSU6JRWK=
human OCUB-M cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFcyPjRizszN MlXTV2FPT0WU
human SW620 cell NWeyOGZDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1vWZ2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> M4nvT3NCVkeHUh?=
human SK-MEL-2 cell MoXrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDN5MzFOwG0> NW\qOYVVW0GQR1XS
human G-401 cell M17TPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUHxZ5g2UW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTB{NkGg{txO NFjXXXBUSU6JRWK=
human HT-29 cell MkCyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61OFY4KM7:TR?= M1fxO3NCVkeHUh?=
human A427 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?= NFvHTWdUSU6JRWK=
human A375 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4TwT2lvcGmkaYTpc44hd2ZiaIXtZY4hSTN5NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlE3PDhizszN MmDBV2FPT0WU
SNU-449 cell Mkj4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFjQeZZKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20OFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ{Mkm0JO69VQ>? NFfGcIdUSU6JRWK=
human A431 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2X4OmlvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlU2OzZizszN M2\vbHNCVkeHUh?=
human NCI-H1299 cell M{jaeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFy4SGNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVI6QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkmzNFgh|ryP MkHVV2FPT0WU
human SNU-423 cell NULUeYFFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHHZ[5VKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjdyNE[2JO69VQ>? M2KzVHNCVkeHUh?=
human SW1710 cell NV7xdIlGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4foZmlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjV3IN88US=> NF6xTJZUSU6JRWK=
human KYSE-450 cell NWH3UYpLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTYTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ6OEWg{txO MVXTRW5ITVJ?

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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]
+ Expand
  • 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:
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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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02807272 Recruiting Leukemia, Myelomonocytic, Chronic Kura Oncology, Inc. October 2016 Phase 2
NCT02779777 Recruiting Myelodysplastic Syndromes Kura Oncology, Inc. May 2016 Phase 2
NCT02535650 Not yet recruiting Urothelial Carcinoma Samsung Medical Center September 2015 Phase 2
NCT02464228 Recruiting Relapsed Peripheral T-Cell Lymphoma|Refractory Peripheral T-Cell Lymphoma Kura Oncology, Inc. September 2015 Phase 2
NCT02383927 Recruiting Thyroid Cancer|Squamous Head and Neck Cancer|HRAS Mutant Tumor Kura Oncology, Inc. March 2015 Phase 2
NCT01361464 Completed Adult Acute Megakaryoblastic Leukemia|Adult Acute Monoblastic Leukemia|Adult Acute Monocytic Leukemia|Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With Maturation|Adult Acute Myeloid Leukemia With Minimal Differentiation|Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22); RUNX1-RUNX1T1|Adult Acute Myeloid Leukemia With t(9;11)(p22;q23); MLLT3-MLL|Adult Acute Myeloid Leukemia Without Maturation|Adult Acute Myelomonocytic Leukemia|Adult Erythroleukemia|Adult Pure Erythroid Leukemia|Alkylating Agent-Related Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia National Cancer Institute (NCI) May 2011 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