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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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 M1jwU2Z2dmO2aX;uJIF{e2G7 NXrmRYpmUW6qaXLpeIlwdiCxZjDyZZQhemWlb33ibY5idnRiUF\UJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGK7IIPjbY51cWyuYYTpc44heHKxeHntbZR6KGG|c3H5MEBKSzVyPUCuO{BvVQ>? M2\xZlIxPDJ7NUGx
NIH3T3 cells MX3GeY5kfGmxbjDhd5NigQ>? MoPQTY5pcWKrdHnvckBw\iCUYYOgdJJw[2W|c3nu[{BqdiCKLYLhd{B1emGwc3\vdo1m\CCQSVizWFMh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiVHnwbYZiem6rYjygSWM2OD1zLk[gcm0> MnL0NVU6OTF{OEG=
human RPMI-6666 cell M3nKW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvNk[2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvPDFibl2= NHfLWJpUSU6JRWK=
human ML-2 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnTsTY5pcWKrdHnvckBw\iCqdX3hckBOVC1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOlQhdk1? M1nVbXNCVkeHUh?=
human SIG-M5 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3vOcWlvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTdibl2= MXvTRW5ITVJ?
human QIMR-WIL cell NV7vNlFUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkTSTY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjNzIH7N NHLa[HNUSU6JRWK=
human A4-Fuk cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlU6KG6P NXLTNnZrW0GQR1XS
human ETK-1 cell NHvhTIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVzQXo1sUW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV{IH7N M4LGdXNCVkeHUh?=
human MEL-JUSO cell NVHhe5lWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTFTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSmXTU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjR2IH7N NWPOUWtQW0GQR1XS
human NALM-6 cell NWT4dnBqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJG5CVE1vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2MlIyKG6P NEjNflJUSU6JRWK=
human IA-LM cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2nuS2lvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20O{42OiCwTR?= M1XzNXNCVkeHUh?=
human Daoy cell M3fYbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn3UTY5pcWKrdHnvckBw\iCqdX3hckBF[W:7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUeuOVMhdk1? NUG2[YoyW0GQR1XS
human REH cell NHjTOmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYDJcohq[mm2aX;uJI9nKGi3bXHuJHJGUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV7LkKgcm0> NEmwfVVUSU6JRWK=
human KU812 cell NFPuXVRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlq3TY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3MlA3KG6P MoLPV2FPT0WU
human KM12 cell NVfEcGVIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlzGTY5pcWKrdHnvckBw\iCqdX3hckBMVTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVY5PiEQvF2= M3f2eXNCVkeHUh?=
human LCLC-103H cell M3zMUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWjJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO MX;TRW5ITVJ?
human BC-1 cell M1jUPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGTBcnZKdmirYnn0bY9vKG:oIHj1cYFvKEKFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEzQTl4IN88US=> MVvTRW5ITVJ?
human CMK cell M1nYSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlj0TY5pcWKrdHnvckBw\iCqdX3hckBEVUtiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG1NVQ2KM7:TR?= MUjTRW5ITVJ?
human MCF7 cell NEfPZ4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYDJcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG2OlMh|ryP MnfWV2FPT0WU
human Calu-1 cell NULnRYVJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFjRc4RKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOThzM{Sg{txO MXvTRW5ITVJ?
human SK-LMS-1 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHPldpNKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOESwPUDPxE1? NGjmVpBUSU6JRWK=
human HH cell NWPIfZN1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnqwTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUmwPFkh|ryP M4PRdHNCVkeHUh?=
human NCI-H2122 cell NH7keWZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFnTeIVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUmxOFUh|ryP M37BO3NCVkeHUh?=
human SNG-M cell M2W4U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKGi3bXHuJHNPTy2PIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yNFM2PCEQvF2= MUjTRW5ITVJ?
human IGROV-1 cell MoDaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHPDUnhKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? MYrTRW5ITVJ?
human KYSE-270 cell NEf5N3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fsOGlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2yO|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJzNk[4JO69VQ>? MVvTRW5ITVJ?
human NTERA-S-cl-D1 cell Mn;pS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVjJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKzO|Qh|ryP M1rYS3NCVkeHUh?=
human LoVo cell MnXIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0NFkyKM7:TR?= NEf6e5BUSU6JRWK=
human MOLT-16 cell NXHiSGVxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXjTR2xiUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{NUiyN{DPxE1? MWPTRW5ITVJ?
human P30-OHK cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlzNTY5pcWKrdHnvckBw\iCqdX3hckBROzBvT1jLJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPjN6ODFOwG0> MlH0V2FPT0WU
human HUTU-80 cell NHqxUGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3fXNGlvcGmkaYTpc44hd2ZiaIXtZY4hUFWWVT24NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjh3MEKg{txO MUnTRW5ITVJ?
human MIA-PaCa-2 cell M1PySWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlnKTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkC0JO69VQ>? MmToV2FPT0WU
human HCC2157 cell NI\tR4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYTJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOzF4IN88US=> M3G4fXNCVkeHUh?=
human HCT-15 cell MoDSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGDaVYtKdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ5MEWg{txO NFzIeYVUSU6JRWK=
human 786-0 cell MoTSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkLXTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN MmmzV2FPT0WU
human GDM-1 cell NVnLbIY5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml\KTY5pcWKrdHnvckBw\iCqdX3hckBITE1vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|UzOzlizszN MlT4V2FPT0WU
human NCI-H2009 cell M{\WTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHL3OJNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlAxQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{[zN|Yh|ryP MXHTRW5ITVJ?
human TE-15 cell M1HuUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoPUTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|Y1PjJizszN MYfTRW5ITVJ?
human NCI-H2342 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnKzTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN5OUizJO69VQ>? MknnV2FPT0WU
human RT-112 cell M2DPVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|gyPzZizqzt MlHkV2FPT0WU
human HCC2998 cell NWCzTYpET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVm0OY5tUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|OESzOkDPxE1? M{f1NnNCVkeHUh?=
human HEL cell NHzaWIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m0OFkh|ryP MV7TRW5ITVJ?
human NMC-G1 cell MoDzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUnhW|JbUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUC1JO69VQ>? M{KyVXNCVkeHUh?=
human 8505C cell MkO4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUPP[3o6UW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO NIrUXlRUSU6JRWK=
human HLE cell MnPQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnzJTY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFEyKM7:TR?= NX3QZXpoW0GQR1XS
human KGN cell NXXmOlFUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGtIViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEWyOFkh|ryP NF\WenFUSU6JRWK=
human EW-18 cell M{jKS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{GzfWlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2PzlzIN88US=> NFXyPVVUSU6JRWK=
human OCUB-M cell NHTqTXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jRVWlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PzF4NDFOwG0> NIf6VpVUSU6JRWK=
human SW620 cell NV7qenpkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkDaTY5pcWKrdHnvckBw\iCqdX3hckBUXzZ{MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFgzOjRizszN M4LFSHNCVkeHUh?=
human SK-MEL-2 cell M163bmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnjYTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDh|N{Og{txO NFmwdnFUSU6JRWK=
human G-401 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGcuPDBzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61NFI3OSEQvF2= MoHEV2FPT0WU
human HT-29 cell MoPwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3rFV2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU1PjdizszN M1jCVnNCVkeHUh?=
human A427 cell MkT1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWniWIFtUW6qaXLpeIlwdiCxZjDoeY1idiCDNEK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42PzlzNzFOwG0> M2G1enNCVkeHUh?=
human A375 cell NVLyNGZUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVP0Nm5nUW6qaXLpeIlwdiCxZjDoeY1idiCDM{e1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OTZ2ODFOwG0> NVXOUodMW0GQR1XS
SNU-449 cell NWO5VnhKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MofCTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNES5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OjJ7NDFOwG0> M{fEU3NCVkeHUh?=
human A431 cell MmruS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXjNohKdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY2PTN4IN88US=> MYXTRW5ITVJ?
human NCI-H1299 cell MoHhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnHFTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGyPVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ7M{C4JO69VQ>? MYTTRW5ITVJ?
human SNU-423 cell M3vSXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlcxPDZ4IN88US=> MXXTRW5ITVJ?
human SW1710 cell Ml;uS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|I2PSEQvF2= NHfETGhUSU6JRWK=
human KYSE-450 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWfpO5lRUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{K4PFUh|ryP MmDuV2FPT0WU

... 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 individually and in order:
15% Captisol+citrate vehicle
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

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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