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 NFTqeFVHfW6ldHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N NXf2coRGOjB2Mkm1NVE>
NIH3T3 cells MkjMSpVv[3Srb36gZZN{[Xl? M2C0OGlvcGmkaYTpc44hd2ZiUnHzJJBzd2Onc4PpcochcW5iSD3yZZMhfHKjboPmc5Ju\WRiTlnIN3Q{KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIGTpdIln[XKwaXKsJGVEPTB;MT62JI5O MmXQNVU6OTF{OEG=
human RPMI-6666 cell NW\DbYdET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoP4TY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLU[2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjRzIH7N M2XlVXNCVkeHUh?=
human ML-2 cell NV;0e|BZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEfaZ5dKdmirYnn0bY9vKG:oIHj1cYFvKE2OLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{43PCCwTR?= MYjTRW5ITVJ?
human SIG-M5 cell M{LBbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\nTY5pcWKrdHnvckBw\iCqdX3hckBUUUdvTUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PyCwTR?= NWSzOJNPW0GQR1XS
human QIMR-WIL cell M2fQXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1rCV2lvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5|MTDuUS=> MX3TRW5ITVJ?
human A4-Fuk cell NETV[WJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NY\BZW86UW6qaXLpeIlwdiCxZjDoeY1idiCDND3GeYsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOC53OTDuUS=> MnzXV2FPT0WU
human ETK-1 cell NUGwT|FOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFT5bG9KdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTJibl2= M3vNcXNCVkeHUh?=
human MEL-JUSO cell MoK0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkT6TY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSmXTU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjR2IH7N NW\XcHdUW0GQR1XS
human NALM-6 cell NGHSdoRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFj1WVNKdmirYnn0bY9vKG:oIHj1cYFvKE6DTF2tOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM3NjJzIH7N NXTmXnljW0GQR1XS
human IA-LM cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXvJcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEeuOVIhdk1? M4T4N3NCVkeHUh?=
human Daoy cell MmnlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLLTY5pcWKrdHnvckBw\iCqdX3hckBF[W:7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUeuOVMhdk1? M{OyWXNCVkeHUh?=
human REH cell NXPwXmFqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnnyTY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O NGm2V|FUSU6JRWK=
human KU812 cell MmPaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUeuNFYhdk1? MVPTRW5ITVJ?
human KM12 cell NFHpU5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NES5S2tKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=> NV74ZnNFW0GQR1XS
human LCLC-103H cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3rodWlvcGmkaYTpc44hd2ZiaIXtZY4hVEOOQz2xNFNJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zMkmwNkDPxE1? NFKyPXpUSU6JRWK=
human BC-1 cell M1n1Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjlbVJnUW6qaXLpeIlwdiCxZjDoeY1idiCEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOjl7NjFOwG0> M1zNc3NCVkeHUh?=
human CMK cell M4LZNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2LJR2lvcGmkaYTpc44hd2ZiaIXtZY4hS02NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOVE1PSEQvF2= M4HBfnNCVkeHUh?=
human MCF7 cell MoDOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\zTY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlY{KM7:TR?= MnTzV2FPT0WU
human Calu-1 cell NVHOUZUyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVgyOzRizszN M3nGd3NCVkeHUh?=
human SK-LMS-1 cell NXyxdJY3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUXoWmp{UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUi0NFkh|ryP MVLTRW5ITVJ?
human HH cell NUT2enJIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{PXOWlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NFg6KM7:TR?= NWnsUGF2W0GQR1XS
human NCI-H2122 cell NFHKeWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTlzNEWg{txO MXLTRW5ITVJ?
human SNG-M cell NGPRd2RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4nwbWlvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxOzV2IN88US=> MVzTRW5ITVJ?
human IGROV-1 cell M2W1WWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkTJTY5pcWKrdHnvckBw\iCqdX3hckBKT1KRVj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODh{MzFOwG0> MoDTV2FPT0WU
human KYSE-270 cell NV6xRYtQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFWzflJKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1? Mn\5V2FPT0WU
human NTERA-S-cl-D1 cell M2LjcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHXDPJBKdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{PzRizszN Mmq4V2FPT0WU
human LoVo cell NIjre25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0NFkyKM7:TR?= NYizd414W0GQR1XS
human MOLT-16 cell NHPqOoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlHRTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPTh{MzFOwG0> NIXpeIZUSU6JRWK=
human P30-OHK cell M4DOXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXjOVppGUW6qaXLpeIlwdiCxZjDoeY1idiCSM{CtU2hMKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{NkO4PEDPxE1? MVnTRW5ITVJ?
human HUTU-80 cell NF;DcpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLhZmhJUW6qaXLpeIlwdiCxZjDoeY1idiCKVWTVMVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{OEWwNkDPxE1? NFv0OINUSU6JRWK=
human MIA-PaCa-2 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFWwUJNKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh|ryP MYTTRW5ITVJ?
human HCC2157 cell M{LZXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4Kz[WlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkG1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ|MU[g{txO M{HU[XNCVkeHUh?=
human HCT-15 cell M2Wzcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M325PWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjdyNTFOwG0> M4DkZXNCVkeHUh?=
human 786-0 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofoTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN MljtV2FPT0WU
human GDM-1 cell Ml;4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGjVWpNKdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTJ|OTFOwG0> MWLTRW5ITVJ?
human NCI-H2009 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYjJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ|M{[g{txO NIjpRpZUSU6JRWK=
human TE-15 cell M4r3NGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2e0bWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM3PDZ{IN88US=> Ml[wV2FPT0WU
human NCI-H2342 cell NULsNJpFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzd7OEOg{txO M3S1dHNCVkeHUh?=
human RT-112 cell M4PNO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1;jWmlvcGmkaYTpc44hd2ZiaIXtZY4hWlRvMUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QDF5NjFOoI0> MV7TRW5ITVJ?
human HCC2998 cell NHXvWYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWXJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM5PDN4IN88US=> NG\jUWRUSU6JRWK=
human HEL cell M1HVUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{XVV2lvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zPVQ1QSEQvF2= NUT2bWJ[W0GQR1XS
human NMC-G1 cell NFPoOo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkPMTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQzPTB3IN88US=> M4DxfXNCVkeHUh?=
human 8505C cell NXfJcVh4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYfsRXlHUW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO MUfTRW5ITVJ?
human HLE cell M3;WU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNES4NVEh|ryP NW\4Z4IzW0GQR1XS
human KGN cell NGq3WpNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlLXTY5pcWKrdHnvckBw\iCqdX3hckBMT05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS1NlQ6KM7:TR?= M17EUnNCVkeHUh?=
human EW-18 cell MnKxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILzW|FKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PTd7MTFOwG0> MU\TRW5ITVJ?
human OCUB-M cell NH7nUG1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnMTY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4OTZ2IN88US=> M2qyeHNCVkeHUh?=
human SW620 cell NF3qZotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjJyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PFIzPCEQvF2= MkXRV2FPT0WU
human SK-MEL-2 cell M4WwSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDN5MzFOwG0> MXzTRW5ITVJ?
human G-401 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3v4eWlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> M17iNXNCVkeHUh?=
human HT-29 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml35TY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVQ3PyEQvF2= NGXBU4pUSU6JRWK=
human A427 cell NULMXY04T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUHJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?= M{jwNXNCVkeHUh?=
human A375 cell M{jGbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrJcohq[mm2aX;uJI9nKGi3bXHuJGE{PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[xOlQ5KM7:TR?= MVfTRW5ITVJ?
SNU-449 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYDXTY5TUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkK5OEDPxE1? Mmf6V2FPT0WU
human A431 cell MoXLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWrSUXc1UW6qaXLpeIlwdiCxZjDoeY1idiCDNEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43PTV|NjFOwG0> Mk[3V2FPT0WU
human NCI-H1299 cell MkT3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;SdpE3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFEzQTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[5N|A5KM7:TR?= M1;qcXNCVkeHUh?=
human SNU-423 cell NXfHdHBVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIPtNXpKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjdyNE[2JO69VQ>? NY\XPIlkW0GQR1XS
human SW1710 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHnvNmtKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ3NTFOwG0> NF75c4ZUSU6JRWK=
human KYSE-450 cell M1TybGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFXpbWRKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtOFUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55Mki4OUDPxE1? MUDTRW5ITVJ?

... 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
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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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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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