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.

Size Price Stock Quantity  
In DMSO USD 620 In stock
USD 480 In stock
USD 980 In stock
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5 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.

    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 NIDiUZFHfW6ldHnvckBie3OjeR?= MYnJcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N NIjTfIQzODR{OUWxNS=>
NIH3T3 cells MWDGeY5kfGmxbjDhd5NigQ>? NXXKZopEUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? MknKNVU6OTF{OEG=
human RPMI-6666 cell M2XMNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnX6TY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLU[2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjRzIH7N NWTlXld[W0GQR1XS
human ML-2 cell NWSzdnB3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>? NHf1c25USU6JRWK=
human SIG-M5 cell NHTVSYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4T5WGlvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTdibl2= NHT6WFBUSU6JRWK=
human QIMR-WIL cell MlHuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvOzFibl2= Ml3xV2FPT0WU
human A4-Fuk cell NFewXXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn3uTY5pcWKrdHnvckBw\iCqdX3hckBCPC2IdXugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNE42QSCwTR?= M37We3NCVkeHUh?=
human ETK-1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{HkWGlvcGmkaYTpc44hd2ZiaIXtZY4hTVSNLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU42OiCwTR?= M4f4ZnNCVkeHUh?=
human MEL-JUSO cell NFjlZVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4Dr[WlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVrVV28h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOy52NDDuUS=> M1PPUXNCVkeHUh?=
human NALM-6 cell NHLyWo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjJV|dbUW6qaXLpeIlwdiCxZjDoeY1idiCQQVzNMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Pi5{MTDuUS=> NV7oe|h7W0GQR1XS
human IA-LM cell M3PVZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfFTY5pcWKrdHnvckBw\iCqdX3hckBKSS2OTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS3MlUzKG6P NVfTdmZUW0GQR1XS
human Daoy cell M2\PNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnnlTY5pcWKrdHnvckBw\iCqdX3hckBF[W:7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUeuOVMhdk1? NUnuSVNMW0GQR1XS
human REH cell NXr6SJJOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlXUTY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O MmmxV2FPT0WU
human KU812 cell NXTwWJgzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlu0TY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3MlA3KG6P MmLwV2FPT0WU
human KM12 cell NHTmbXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlXTTY5pcWKrdHnvckBw\iCqdX3hckBMVTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVY5PiEQvF2= MUnTRW5ITVJ?
human LCLC-103H cell MkLpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;xPXp1UW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVExO0hiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyPVAzKM7:TR?= NELSbmNUSU6JRWK=
human BC-1 cell MonLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEDNSW9KdmirYnn0bY9vKG:oIHj1cYFvKEKFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEzQTl4IN88US=> NVTSe2hbW0GQR1XS
human CMK cell MoS2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHj1NFhKdmirYnn0bY9vKG:oIHj1cYFvKEOPSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVUyPDVizszN MlP1V2FPT0WU
human MCF7 cell NVmwe5EzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWfLS5d{UW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPjZ|IN88US=> MnHWV2FPT0WU
human Calu-1 cell M{HLc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYLaTY17UW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6MUO0JO69VQ>? Mnn1V2FPT0WU
human SK-LMS-1 cell NUfCXnB5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHG3S5JKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOESwPUDPxE1? NX:3b3c6W0GQR1XS
human HH cell NYTEcIZDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlq0TY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUmwPFkh|ryP NXvIN3JoW0GQR1XS
human NCI-H2122 cell M3r0dWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUfSZXh5UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= NGHFcJlUSU6JRWK=
human SNG-M cell NUXEU2xjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{nCV2lvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxOzV2IN88US=> NX23WmZOW0GQR1XS
human IGROV-1 cell M4K2eGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NILqW3lKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? NY\nSHVHW0GQR1XS
human KYSE-270 cell M3;0Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVnJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMkewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOTZ4ODFOwG0> NWHoZ5hGW0GQR1XS
human NTERA-S-cl-D1 cell NGj6dJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkG4TY5pcWKrdHnvckBw\iCqdX3hckBPXEWUQT3TMYNtNURzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yN|c1KM7:TR?= NYHiS5FKW0GQR1XS
human LoVo cell Mn\2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M165cmlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQxQTFizszN Mnf1V2FPT0WU
human MOLT-16 cell M4LXe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGTve4tKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ3OEKzJO69VQ>? MkXoV2FPT0WU
human P30-OHK cell NUTFR|hTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1W2Z2lvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjZ|OEig{txO MnvOV2FPT0WU
human HUTU-80 cell M3LXXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIHtNFJKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ6NUCyJO69VQ>? NWW4RXliW0GQR1XS
human MIA-PaCa-2 cell NETTdGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlSzTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkC0JO69VQ>? MU\TRW5ITVJ?
human HCC2157 cell NHK2b3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3r4VWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkG1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ|MU[g{txO NXHKRlRxW0GQR1XS
human HCT-15 cell NH\hRXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFrzNlFKdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ5MEWg{txO M3rDZ3NCVkeHUh?=
human 786-0 cell MoTrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlE4OyEQvF2= NU\Q[lE2W0GQR1XS
human GDM-1 cell MonsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkX1TY5pcWKrdHnvckBw\iCqdX3hckBITE1vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|UzOzlizszN M3yx[XNCVkeHUh?=
human NCI-H2009 cell M1PuSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1rQc2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|NkOzOkDPxE1? MlfyV2FPT0WU
human TE-15 cell NIfDN2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NI\Y[G9KdmirYnn0bY9vKG:oIHj1cYFvKFSHLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PjR4MjFOwG0> MlL3V2FPT0WU
human NCI-H2342 cell Mlj5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzd7OEOg{txO NVjIRpN7W0GQR1XS
human RT-112 cell M4\OVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFjEfWNKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzhzN{[g{rxu NVHvWI05W0GQR1XS
human HCC2998 cell NF3EWlFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM5PDN4IN88US=> NI\jSXZUSU6JRWK=
human HEL cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m0OFkh|ryP M2jHOHNCVkeHUh?=
human NMC-G1 cell MkDTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWjJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFI2ODVizszN NE\mfppUSU6JRWK=
human 8505C cell NVzlZYZ5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoroTY5pcWKrdHnvckBw\iCqdX3hckA5PTB3QzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFMyODlizszN M3LiUXNCVkeHUh?=
human HLE cell NYLiWlFuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULldW1VUW6qaXLpeIlwdiCxZjDoeY1idiCKTFWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDFzIN88US=> M3v0O3NCVkeHUh?=
human KGN cell M3PpfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{e0b2lvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= NXTVXWRNW0GQR1XS
human EW-18 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M13UVWlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2PzlzIN88US=> M37PfHNCVkeHUh?=
human OCUB-M cell NETrZlZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmTNTY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4OTZ2IN88US=> NIDqVZJUSU6JRWK=
human SW620 cell M3\ZZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NELiWVRKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDJ{NDFOwG0> NW[wbHg6W0GQR1XS
human SK-MEL-2 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmLiTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDh|N{Og{txO M32wTXNCVkeHUh?=
human G-401 cell NXPVNWNXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2TFc2lvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> MYrTRW5ITVJ?
human HT-29 cell NXLZcoQ6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlzGTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVQ3PyEQvF2= MnPZV2FPT0WU
human A427 cell NXG2RYFRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGnVOGtKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU4QTF5IN88US=> MojkV2FPT0WU
human A375 cell NYjFVnJ3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIfCcodKdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=> NEPVe4lUSU6JRWK=
SNU-449 cell M4TWTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn:3TY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNES5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OjJ7NDFOwG0> MUnTRW5ITVJ?
human A431 cell NWLEUIhoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGE1OzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[1OVM3KM7:TR?= MkLOV2FPT0WU
human NCI-H1299 cell MnrVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zkO2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixNlk6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54OUOwPEDPxE1? NXrndVRpW0GQR1XS
human SNU-423 cell Ml3sS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1OwTmlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzB2Nk[g{txO NVzvV4xCW0GQR1XS
human SW1710 cell M2TCRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|I2PSEQvF2= NEjKRVFUSU6JRWK=
human KYSE-450 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvNEWwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Ojh6NTFOwG0> NUjwfGQyW0GQR1XS

... 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
Synonyms R115777

Bio Calculators

Molarity Calculator

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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