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
USD 480 In stock
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Cited by 14 Publications

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 MVjGeY5kfGmxbjDhd5NigQ>? M3\H[WlvcGmkaYTpc44hd2ZicnH0JJJm[2:vYnnuZY51KFCIVDDlfJBz\XO|ZXSgbY4hcW6|ZXP0JHNnQSClZXzsd{BjgSC|Y3nueIltdGG2aX;uJJBzd3irbXn0fUBie3OjeTygTWM2OD1yLkegcm0> Mle1NlA1Ojl3MUG=
NIH3T3 cells MUjGeY5kfGmxbjDhd5NigQ>? M1voUmlvcGmkaYTpc44hd2ZiUnHzJJBzd2Onc4PpcochcW5iSD3yZZMhfHKjboPmc5Ju\WRiTlnIN3Q{KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIGTpdIln[XKwaXKsJGVEPTB;MT62JI5O NGDncHYyPTlzMUK4NS=>
human RPMI-6666 cell NUTJeXFiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHKwW3NKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtOlY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdwNEGgcm0> MWrTRW5ITVJ?
human ML-2 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>? MWPTRW5ITVJ?
human SIG-M5 cell M3n0O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\iTY5pcWKrdHnvckBw\iCqdX3hckBUUUdvTUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PyCwTR?= NHfDOVFUSU6JRWK=
human QIMR-WIL cell NEPRNo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYTnR4dxUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkOxJI5O NILxZ2hUSU6JRWK=
human A4-Fuk cell NEf4UJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkTzTY5pcWKrdHnvckBw\iCqdX3hckBCPC2IdXugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNE42QSCwTR?= NGO4UW9USU6JRWK=
human ETK-1 cell MnHjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkTPTY5pcWKrdHnvckBw\iCqdX3hckBGXEtvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxMlUzKG6P NU\4epVsW0GQR1XS
human MEL-JUSO cell M{C2Zmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVPMVYNrUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTnVUVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ|LkS0JI5O MlGyV2FPT0WU
human NALM-6 cell M1nHWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1j5UGlvcGmkaYTpc44hd2ZiaIXtZY4hVkGOTT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|YvOjFibl2= M1z4O3NCVkeHUh?=
human IA-LM cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXnJcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEeuOVIhdk1? MXnTRW5ITVJ?
human Daoy cell NI\mfGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIXDeXFKdmirYnn0bY9vKG:oIHj1cYFvKESjb4mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21O{42OyCwTR?= NVvReHUxW0GQR1XS
human REH cell M1zmNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlS5TY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O NGLublFUSU6JRWK=
human KU812 cell NHvUV2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4TEVGlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{4xPiCwTR?= MXjTRW5ITVJ?
human KM12 cell NXO0[YFnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3nuZ2lvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE3QDZizszN MmfRV2FPT0WU
human LCLC-103H cell M1PXZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO MUDTRW5ITVJ?
human BC-1 cell M3q3S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGJENTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyPVk3KM7:TR?= MVPTRW5ITVJ?
human CMK cell NX\0cZFwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXTTV4RRUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=> M1P6WnNCVkeHUh?=
human MCF7 cell NXz5b3BJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWLJcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG2OlMh|ryP M13hZ3NCVkeHUh?=
human Calu-1 cell NUHoPFk4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTEO2NlUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6MUO0JO69VQ>? MUjTRW5ITVJ?
human SK-LMS-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnHhTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTh2MEmg{txO M3LpfXNCVkeHUh?=
human HH cell NX7oZWE{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3fYUmlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NFg6KM7:TR?= MoT2V2FPT0WU
human NCI-H2122 cell NWezRY9bT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoDDTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKxNlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF7MUS1JO69VQ>? NEWxT5BUSU6JRWK=
human SNG-M cell NH;MSVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXfJcohq[mm2aX;uJI9nKGi3bXHuJHNPTy2PIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yNFM2PCEQvF2= MXTTRW5ITVJ?
human IGROV-1 cell M1fNWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHuRppKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? NXv4bpZFW0GQR1XS
human KYSE-270 cell NFGxfG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmHFTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUK3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjF4Nkig{txO M1fxbXNCVkeHUh?=
human NTERA-S-cl-D1 cell Mm\lS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVjJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKzO|Qh|ryP MUjTRW5ITVJ?
human LoVo cell M3jyOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVfXVHdJUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDB7MTFOwG0> MYfTRW5ITVJ?
human MOLT-16 cell NWP3[ohLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2LrdmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO M4XiRXNCVkeHUh?=
human P30-OHK cell NVS5Vpg4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYnJcohq[mm2aX;uJI9nKGi3bXHuJHA{OC2RSFugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3Ozh6IN88US=> NWPGTJhnW0GQR1XS
human HUTU-80 cell NHHCdIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWTrPYw{UW6qaXLpeIlwdiCxZjDoeY1idiCKVWTVMVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{OEWwNkDPxE1? MVzTRW5ITVJ?
human MIA-PaCa-2 cell NGHrWINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MljPTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkC0JO69VQ>? MmrnV2FPT0WU
human HCC2157 cell M4\5PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX3hd4pMUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkOxOkDPxE1? NUHNbZo{W0GQR1XS
human HCT-15 cell NECxepFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoHqTY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=> MYnTRW5ITVJ?
human 786-0 cell MoPHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmPoTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN NXLBdo9MW0GQR1XS
human GDM-1 cell M4XpbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4j2UGlvcGmkaYTpc44hd2ZiaIXtZY4hT0SPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2OjN7IN88US=> MYLTRW5ITVJ?
human NCI-H2009 cell MlLRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MorITY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN4M{O2JO69VQ>? NEXZVlJUSU6JRWK=
human TE-15 cell NYTQ[|N{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHTlbmJKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PjR4MjFOwG0> NXLQU2J4W0GQR1XS
human NCI-H2342 cell NYm1THZvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NE\hO3hKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlM1OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{e5PFMh|ryP MYfTRW5ITVJ?
human RT-112 cell Mn[4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|gyPzZizqzt NFvqcGNUSU6JRWK=
human HCC2998 cell NIPyXnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlnmTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QDR|NjFOwG0> NV3BNpdsW0GQR1XS
human HEL cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV[3cnNrUW6qaXLpeIlwdiCxZjDoeY1idiCKRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM6PDR7IN88US=> MYnTRW5ITVJ?
human NMC-G1 cell MnXDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX;NXoI3UW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUC1JO69VQ>? NEHDTXlUSU6JRWK=
human 8505C cell NWTHV|FCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYfMZllCUW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO MULTRW5ITVJ?
human HLE cell MmixS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY\aRYlpUW6qaXLpeIlwdiCxZjDoeY1idiCKTFWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDFzIN88US=> MnjEV2FPT0WU
human KGN cell MnqzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NELRUIlKdmirYnn0bY9vKG:oIHj1cYFvKEuJTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFUzPDlizszN NWC0XoNUW0GQR1XS
human EW-18 cell NH\EdXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnvLTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFU4QTFizszN NFXSNZlUSU6JRWK=
human OCUB-M cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHLIXG5KdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDdzNkSg{txO MW\TRW5ITVJ?
human SW620 cell NVHETpRmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjJyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PFIzPCEQvF2= MmfIV2FPT0WU
human SK-MEL-2 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUXJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDN5MzFOwG0> MofQV2FPT0WU
human G-401 cell M4PmRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2n6TGlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> NFzHOlRUSU6JRWK=
human HT-29 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHTNYNHUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2yPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTR4NzFOwG0> NXvKWG84W0GQR1XS
human A427 cell NXjWTWVUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{DZNWlvcGmkaYTpc44hd2ZiaIXtZY4hSTR{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVc6OTdizszN NVLv[ZVWW0GQR1XS
human A375 cell M4iyd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3wR5F7UW6qaXLpeIlwdiCxZjDoeY1idiCDM{e1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OTZ2ODFOwG0> MXjTRW5ITVJ?
SNU-449 cell Mn2zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWj1VGxNUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkK5OEDPxE1? M3jlVnNCVkeHUh?=
human A431 cell Ml;FS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{LGb2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlU2OzZizszN NGC3bW5USU6JRWK=
human NCI-H1299 cell Mlv1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3vvPGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixNlk6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54OUOwPEDPxE1? NVfYfWVLW0GQR1XS
human SNU-423 cell NFy3XI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlcxPDZ4IN88US=> NH7oe3NUSU6JRWK=
human SW1710 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYD6SVZSUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd{NUWg{txO M3O1bXNCVkeHUh?=
human KYSE-450 cell Moj4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmTrTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ6OEWg{txO NUTOb5RzW0GQR1XS

... 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(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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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03719690 Not yet recruiting HRAS Gene Mutation|HNSCC Kura Oncology Inc. December 2018 Phase 2
NCT03719690 Not yet recruiting HRAS Gene Mutation|HNSCC Kura Oncology Inc. December 2018 Phase 2
NCT03496766 Recruiting Non Small Cell Lung Cancer Spanish Lung Cancer Group May 7 2018 Phase 2
NCT03496766 Recruiting Non Small Cell Lung Cancer Spanish Lung Cancer Group May 7 2018 Phase 2
NCT02807272 Recruiting Leukemia Myelomonocytic Chronic Kura Oncology Inc. October 2016 Phase 2
NCT02807272 Recruiting Leukemia Myelomonocytic Chronic Kura Oncology Inc. October 2016 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