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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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 MoLUSpVv[3Srb36gZZN{[Xl? NGe3PJlKdmirYnn0bY9vKG:oIILheEBz\WOxbXLpcoFvfCCSRmSg[ZhxemW|c3XkJIlvKGmwc3XjeEBU\jliY3XscJMh[nlic3PpcpRqdGyjdHnvckBxem:6aX3peJkh[XO|YYmsJGlEPTB;MD63JI5O M1XWVlIxPDJ7NUGx
NIH3T3 cells MV;GeY5kfGmxbjDhd5NigQ>? MmjJTY5pcWKrdHnvckBw\iCUYYOgdJJw[2W|c3nu[{BqdiCKLYLhd{B1emGwc3\vdo1m\CCQSVizWFMh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiVHnwbYZiem6rYjygSWM2OD1zLk[gcm0> MXuxOVkyOTJ6MR?=
human RPMI-6666 cell NFmw[mNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1XrdmlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=> NYDC[nc6W0GQR1XS
human ML-2 cell NF;wUWJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVXZWoZXUW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvPjRibl2= M2\ZT3NCVkeHUh?=
human SIG-M5 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NU\OS|VrUW6qaXLpeIlwdiCxZjDoeY1idiCVSVetUVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53NzDuUS=> NFXU[oxUSU6JRWK=
human QIMR-WIL cell NX:4TmNQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1L2OmlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5|MTDuUS=> NYf2Z4txW0GQR1XS
human A4-Fuk cell M3joPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2X5VWlvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlAvPTlibl2= MmjjV2FPT0WU
human ETK-1 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGVVUy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkGuOVIhdk1? NU\XSZRFW0GQR1XS
human MEL-JUSO cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGHNOYhKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3KWXNQKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwNESgcm0> NYPq[2FPW0GQR1XS
human NALM-6 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUfuZnVIUW6qaXLpeIlwdiCxZjDoeY1idiCQQVzNMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Pi5{MTDuUS=> Mm\TV2FPT0WU
human IA-LM cell MlfmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk\ETY5pcWKrdHnvckBw\iCqdX3hckBKSS2OTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS3MlUzKG6P MXPTRW5ITVJ?
human Daoy cell Mn\SS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXzvTpA3UW6qaXLpeIlwdiCxZjDoeY1idiCGYX;5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVcvPTNibl2= NVLPSXBbW0GQR1XS
human REH cell NFPzXWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkTNTY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O MmDSV2FPT0WU
human KU812 cell NWm1[41DT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHi2RmxKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVcvODZibl2= NWjheHNFW0GQR1XS
human KM12 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TxTmlvcGmkaYTpc44hd2ZiaIXtZY4hU01zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE3QDZizszN NX74VVBLW0GQR1XS
human LCLC-103H cell NFHzc|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF;0[HZKdmirYnn0bY9vKG:oIHj1cYFvKEyFTFOtNVA{UCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUK5NFIh|ryP MYXTRW5ITVJ?
human BC-1 cell MnPBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkD1TY5pcWKrdHnvckBw\iCqdX3hckBDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNlk6PiEQvF2= NY\zUI95W0GQR1XS
human CMK cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUDJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUWxOFUh|ryP M1LFe3NCVkeHUh?=
human MCF7 cell Mnq5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXjJcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG2OlMh|ryP NIS5dHFUSU6JRWK=
human Calu-1 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX;NWHB4UW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6MUO0JO69VQ>? M3nN[nNCVkeHUh?=
human SK-LMS-1 cell NFu5R3VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYLLV5JtUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUi0NFkh|ryP NVLjd3JkW0GQR1XS
human HH cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWXJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOUC4PUDPxE1? NU\he5ZiW0GQR1XS
human NCI-H2122 cell NWm0cYg3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTlzNEWg{txO MVTTRW5ITVJ?
human SNG-M cell Ml[zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\ZNVhNUW6qaXLpeIlwdiCxZjDoeY1idiCVTletUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB|NUSg{txO MVzTRW5ITVJ?
human IGROV-1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVWzVVJMUW6qaXLpeIlwdiCxZjDoeY1idiCLR2LPWk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MEiyN{DPxE1? NHvDNGVUSU6JRWK=
human KYSE-270 cell NUPxO5ZMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2TpWmlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2yO|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJzNk[4JO69VQ>? MV7TRW5ITVJ?
human NTERA-S-cl-D1 cell M{jiXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKzO|Qh|ryP MWDTRW5ITVJ?
human LoVo cell NHnQeZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2\sfGlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQxQTFizszN NVrDbFVlW0GQR1XS
human MOLT-16 cell NGP1bnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmjxTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPTh{MzFOwG0> M3;xU3NCVkeHUh?=
human P30-OHK cell NVfrVplFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkXITY5pcWKrdHnvckBw\iCqdX3hckBROzBvT1jLJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPjN6ODFOwG0> NWD5ZZhbW0GQR1XS
human HUTU-80 cell NHHPdmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIP1TY9KdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ6NUCyJO69VQ>? NFj0VFZUSU6JRWK=
human MIA-PaCa-2 cell MnTOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF\qbY1KdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh|ryP MUPTRW5ITVJ?
human HCC2157 cell NXexNpJKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NViybI5VUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkOxOkDPxE1? NF[yRVFUSU6JRWK=
human HCT-15 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUXJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|I4ODVizszN MVnTRW5ITVJ?
human 786-0 cell MlO0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{Xlc2lvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> M3;F[nNCVkeHUh?=
human GDM-1 cell M1vXVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NULWbWZZUW6qaXLpeIlwdiCxZjDoeY1idiCJRF2tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzV{M{mg{txO M3T2NHNCVkeHUh?=
human NCI-H2009 cell M1PVXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MW\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ|M{[g{txO NX63eZlWW0GQR1XS
human TE-15 cell M17Qcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3PJeWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM3PDZ{IN88US=> NF[3[oZUSU6JRWK=
human NCI-H2342 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmTDTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN5OUizJO69VQ>? NHTSc4JUSU6JRWK=
human RT-112 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYHUcJFlUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6MUe2JO6ddQ>? MYXTRW5ITVJ?
human HCC2998 cell MmnWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM5PDN4IN88US=> NULsbW91W0GQR1XS
human HEL cell M4nNd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV60PZQ2UW6qaXLpeIlwdiCxZjDoeY1idiCKRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM6PDR7IN88US=> NEXxV5VUSU6JRWK=
human NMC-G1 cell M2PGVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYjGcodxUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUC1JO69VQ>? MlrnV2FPT0WU
human 8505C cell NF3rSVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXixe2VKUW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO MVvTRW5ITVJ?
human HLE cell MonIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\FT|hKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ5OTFizszN M4fHUnNCVkeHUh?=
human KGN cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1uyN2lvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= NVLDU4xFW0GQR1XS
human EW-18 cell NIj4T5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlHFTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFU4QTFizszN NWf1TIhjW0GQR1XS
human OCUB-M cell Mof0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4HzfWlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PzF4NDFOwG0> MlmyV2FPT0WU
human SW620 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkPNTY5pcWKrdHnvckBw\iCqdX3hckBUXzZ{MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFgzOjRizszN NHPaWVZUSU6JRWK=
human SK-MEL-2 cell M{jhPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDN5MzFOwG0> MnXYV2FPT0WU
human G-401 cell MnvLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1rRN2lvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> MUfTRW5ITVJ?
human HT-29 cell NEPIN2NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mm\PTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVQ3PyEQvF2= NFKz[GFUSU6JRWK=
human A427 cell Mk\QS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NELENIRKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU4QTF5IN88US=> M{TWeXNCVkeHUh?=
human A375 cell Mln0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHfvfndKdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=> M4XVfHNCVkeHUh?=
SNU-449 cell M4f1[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX\1eFVEUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkK5OEDPxE1? M{P5ZnNCVkeHUh?=
human A431 cell NXvZboJqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4HSd2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlU2OzZizszN MorlV2FPT0WU
human NCI-H1299 cell NUDEenAyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkDGTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGyPVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ7M{C4JO69VQ>? NWf4VJpDW0GQR1XS
human SNU-423 cell NFjtZplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1nFPWlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzB2Nk[g{txO MX3TRW5ITVJ?
human SW1710 cell M33mbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYXHc2xHUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd{NUWg{txO M{nrNnNCVkeHUh?=
human KYSE-450 cell NWjTSmZwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvNEWwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Ojh6NTFOwG0> NEL2VJdUSU6JRWK=

... 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

Molarity Calculator

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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

Tel: +1-832-582-8158 Ext:3

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID