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 NGjMV5FHfW6ldHnvckBie3OjeR?= NYK4bGZyUW6qaXLpeIlwdiCxZjDyZZQhemWlb33ibY5idnRiUF\UJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGK7IIPjbY51cWyuYYTpc44heHKxeHntbZR6KGG|c3H5MEBKSzVyPUCuO{BvVQ>? M{PJbVIxPDJ7NUGx
NIH3T3 cells NVH5WHJLTnWwY4Tpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKFKjczDwdo9k\XO|aX7nJIlvKEhvcnHzJJRz[W6|Zn;ycYVlKE6LSEPUN{Bk\WyuczDpckBxemW|ZX7j[UBw\iCWaYDp[oFzdmmkLDDFR|UxRTFwNjDuUS=> MX:xOVkyOTJ6MR?=
human RPMI-6666 cell NYLxb4cyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIjCPFRKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtOlY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdwNEGgcm0> NFL4cYRUSU6JRWK=
human ML-2 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFHJ[XpKdmirYnn0bY9vKG:oIHj1cYFvKE2OLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{43PCCwTR?= MV\TRW5ITVJ?
human SIG-M5 cell NFXENmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYD4cY5EUW6qaXLpeIlwdiCxZjDoeY1idiCVSVetUVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53NzDuUS=> NHLMdnNUSU6JRWK=
human QIMR-WIL cell MnnwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYDUVpdMUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkOxJI5O NH\JeINUSU6JRWK=
human A4-Fuk cell M4rpT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUHwWnRuUW6qaXLpeIlwdiCxZjDoeY1idiCDND3GeYsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOC53OTDuUS=> NXf1cXM1W0GQR1XS
human ETK-1 cell NYrLS2hWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXu0SFAyUW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV{IH7N MkmwV2FPT0WU
human MEL-JUSO cell MlX6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHzsWIRKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3KWXNQKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwNESgcm0> NXf0VVYzW0GQR1XS
human NALM-6 cell Mor6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJG5CVE1vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2MlIyKG6P NYG0b3Y3W0GQR1XS
human IA-LM cell NFjCUHpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGrIXYxKdmirYnn0bY9vKG:oIHj1cYFvKEmDLVzNJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFcvPTJibl2= M4rweHNCVkeHUh?=
human Daoy cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF[yVnZKdmirYnn0bY9vKG:oIHj1cYFvKESjb4mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21O{42OyCwTR?= NFvZb3RUSU6JRWK=
human REH cell MmfHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlOyTY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O M2nMZ3NCVkeHUh?=
human KU812 cell MmPES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;tdGdTUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk4NjB4IH7N M1y5fXNCVkeHUh?=
human KM12 cell M2PBNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LzfmlvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE3QDZizszN MlHWV2FPT0WU
human LCLC-103H cell NITlcFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO Ml3HV2FPT0WU
human BC-1 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUWyU|hJUW6qaXLpeIlwdiCxZjDoeY1idiCEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOjl7NjFOwG0> M1;3ZXNCVkeHUh?=
human CMK cell NHXBdFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVi2WZRmUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=> MVfTRW5ITVJ?
human MCF7 cell NF2zcnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4LqbmlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVY3OyEQvF2= M4jNZXNCVkeHUh?=
human Calu-1 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUSzfXhLUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6MUO0JO69VQ>? NF7UOphUSU6JRWK=
human SK-LMS-1 cell M{m5WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUfFc4oxUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUi0NFkh|ryP MljnV2FPT0WU
human HH cell MmPjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4j2bGlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NFg6KM7:TR?= NXnrUYtoW0GQR1XS
human NCI-H2122 cell NW[5fVlWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmewTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKxNlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF7MUS1JO69VQ>? MkfDV2FPT0WU
human SNG-M cell M2nyZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvITHdKdmirYnn0bY9vKG:oIHj1cYFvKFOQRz3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODN3NDFOwG0> NWrOZZVoW0GQR1XS
human IGROV-1 cell NIqydoRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGlIWk:YLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxQDJ|IN88US=> NFuwNIJUSU6JRWK=
human KYSE-270 cell M4C4S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMkewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOTZ4ODFOwG0> NFu4U3FUSU6JRWK=
human NTERA-S-cl-D1 cell Mn7hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmX6TY5pcWKrdHnvckBw\iCqdX3hckBPXEWUQT3TMYNtNURzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yN|c1KM7:TR?= NUiyXFJlW0GQR1XS
human LoVo cell MkmyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFj0Z|VKdmirYnn0bY9vKG:oIHj1cYFvKEyxVn:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1ODlzIN88US=> M3OzSXNCVkeHUh?=
human MOLT-16 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIH1VWZKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ3OEKzJO69VQ>? M{[2O3NCVkeHUh?=
human P30-OHK cell NF2xfFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{LXfmlvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjZ|OEig{txO NUHvenFIW0GQR1XS
human HUTU-80 cell MoLSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTFZ5hKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ6NUCyJO69VQ>? NX\YU4pjW0GQR1XS
human MIA-PaCa-2 cell NU\Le|FLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVfDc|dVUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlA1KM7:TR?= NFvsN5NUSU6JRWK=
human HCC2157 cell NHnhTItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV:0NFBRUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkOxOkDPxE1? NU\ISWZbW0GQR1XS
human HCT-15 cell NXjFeYFnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXHe5p7UW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{N{C1JO69VQ>? MXHTRW5ITVJ?
human 786-0 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmTGTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN NYT6WVdFW0GQR1XS
human GDM-1 cell NImxc|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoGzTY5pcWKrdHnvckBw\iCqdX3hckBITE1vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|UzOzlizszN M2PRc3NCVkeHUh?=
human NCI-H2009 cell MlP6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3\CVGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|NkOzOkDPxE1? M1\IfnNCVkeHUh?=
human TE-15 cell NY\FRVY3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoLiTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|Y1PjJizszN NILRTnNUSU6JRWK=
human NCI-H2342 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUTuVGRiUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO3PVg{KM7:TR?= M2f3OnNCVkeHUh?=
human RT-112 cell NVu5W3ZWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|gyPzZizqzt MmjhV2FPT0WU
human HCC2998 cell NUfUeFdHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmHuTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QDR|NjFOwG0> M1HvOXNCVkeHUh?=
human HEL cell NVj2OGN[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m0OFkh|ryP MofRV2FPT0WU
human NMC-G1 cell NEXWfXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlvSTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQzPTB3IN88US=> NFfjOIpUSU6JRWK=
human 8505C cell M4D5VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXjjV2Z{UW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO NWjSeHFQW0GQR1XS
human HLE cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn\3TY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFEyKM7:TR?= NGHCTYhUSU6JRWK=
human KGN cell M3n3fWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1f5RmlvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= NGnsXWNUSU6JRWK=
human EW-18 cell NHLreFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXrJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTF6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVc6OSEQvF2= NV\kdI5DW0GQR1XS
human OCUB-M cell NVXRboR1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFcyPjRizszN NEjJWmpUSU6JRWK=
human SW620 cell NF\BWlJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1:2OmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> MYfTRW5ITVJ?
human SK-MEL-2 cell NYOyfVh1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnzU3VrUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEizO|Mh|ryP NXzXWGcyW0GQR1XS
human G-401 cell M{LVO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTZfXdZUW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTB{NkGg{txO NHPJS5lUSU6JRWK=
human HT-29 cell M2HqT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkfmTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVQ3PyEQvF2= NIHXboZUSU6JRWK=
human A427 cell NUO4RpU2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUTJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?= MlLQV2FPT0WU
human A375 cell NXOzW5NyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkP4TY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62NVY1QCEQvF2= MnTWV2FPT0WU
SNU-449 cell M3;RbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnW1TY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNES5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OjJ7NDFOwG0> MoTKV2FPT0WU
human A431 cell MmqyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{TzfWlvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlU2OzZizszN MVLTRW5ITVJ?
human NCI-H1299 cell M1f0Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUK5PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjl|MEig{txO MXfTRW5ITVJ?
human SNU-423 cell NIXPW21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVq5NoM3UW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55MES2OkDPxE1? NWDJS5c5W0GQR1XS
human SW1710 cell M1XhcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkLiTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlczPTVizszN NFLUU2ZUSU6JRWK=
human KYSE-450 cell M1vTcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUnJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvNEWwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Ojh6NTFOwG0> NUfKT|NYW0GQR1XS

... 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
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
NCT02779777 Recruiting Myelodysplastic Syndromes Kura Oncology Inc. May 2016 Phase 2
NCT02535650 Recruiting Urothelial Carcinoma Samsung Medical Center November 12 2015 Phase 2
NCT02464228 Recruiting Relapsed Peripheral T-Cell Lymphoma|Refractory Peripheral T-Cell Lymphoma Kura Oncology Inc. September 2015 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