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
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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 M1:2W2Z2dmO2aX;uJIF{e2G7 Mm\sTY5pcWKrdHnvckBw\iC{YYSgdoVkd22kaX7hcpQhWE[WIHX4dJJme3OnZDDpckBqdnOnY4SgV4Y6KGOnbHzzJIJ6KHOlaX70bYxt[XSrb36gdJJwgGmvaYT5JIF{e2G7LDDJR|UxRTBwNzDuUS=> NYDScmRtOjB2Mkm1NVE>
NIH3T3 cells M1nROmZ2dmO2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKFKjczDwdo9k\XO|aX7nJIlvKEhvcnHzJJRz[W6|Zn;ycYVlKE6LSEPUN{Bk\WyuczDpckBxemW|ZX7j[UBw\iCWaYDp[oFzdmmkLDDFR|UxRTFwNjDuUS=> NITVcHQyPTlzMUK4NS=>
human RPMI-6666 cell MkLRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnzDTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLU[2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjRzIH7N NXrWTHdyW0GQR1XS
human ML-2 cell MmHwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUH6Z5JwUW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvPjRibl2= NEXCeVZUSU6JRWK=
human SIG-M5 cell Mn\xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MljPTY5pcWKrdHnvckBw\iCqdX3hckBUUUdvTUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PyCwTR?= MnXRV2FPT0WU
human QIMR-WIL cell MoX2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILTd3FKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwM{Ggcm0> NYnNbWZjW0GQR1XS
human A4-Fuk cell M4DHb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NY\3OIJlUW6qaXLpeIlwdiCxZjDoeY1idiCDND3GeYsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOC53OTDuUS=> NYHTRXFDW0GQR1XS
human ETK-1 cell MnXWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVTJcohq[mm2aX;uJI9nKGi3bXHuJGVVUy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkGuOVIhdk1? NXj4U5Z7W0GQR1XS
human MEL-JUSO cell NGi2UZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGTtSZNKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3KWXNQKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwNESgcm0> MmL0V2FPT0WU
human NALM-6 cell M3j5O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF3GTpZKdmirYnn0bY9vKG:oIHj1cYFvKE6DTF2tOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM3NjJzIH7N MYrTRW5ITVJ?
human IA-LM cell NWS5XI5jT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MknLTY5pcWKrdHnvckBw\iCqdX3hckBKSS2OTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS3MlUzKG6P MUfTRW5ITVJ?
human Daoy cell MnjGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmPWTY5pcWKrdHnvckBw\iCqdX3hckBF[W:7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUeuOVMhdk1? NVLPN5V5W0GQR1XS
human REH cell NUDON4pjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3;hWGlvcGmkaYTpc44hd2ZiaIXtZY4hWkWKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUmuNkBvVQ>? NHz2bndUSU6JRWK=
human KU812 cell NH[5THZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUeuNFYhdk1? MljMV2FPT0WU
human KM12 cell NIH6Ro1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGj6VZRKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=> Mmf0V2FPT0WU
human LCLC-103H cell NVj2Vo52T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGC1[ZZKdmirYnn0bY9vKG:oIHj1cYFvKEyFTFOtNVA{UCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUK5NFIh|ryP M1O5UHNCVkeHUh?=
human BC-1 cell M4LNOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mkf2TY5pcWKrdHnvckBw\iCqdX3hckBDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNlk6PiEQvF2= NIXlUJdUSU6JRWK=
human CMK cell MnrVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1[xOmlvcGmkaYTpc44hd2ZiaIXtZY4hS02NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOVE1PSEQvF2= MWfTRW5ITVJ?
human MCF7 cell NGPwd4RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;HS2lvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVY3OyEQvF2= MlPxV2FPT0WU
human Calu-1 cell M3LCfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4PJPGlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDF|NDFOwG0> NYfaNIl7W0GQR1XS
human SK-LMS-1 cell MnXYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TCXWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTF3TMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6NEC5JO69VQ>? MmjVV2FPT0WU
human HH cell M3PyUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVHzeYdvUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVkxQDlizszN M2PEc3NCVkeHUh?=
human NCI-H2122 cell NGjQVVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTlzNEWg{txO M2PKVHNCVkeHUh?=
human SNG-M cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoDSTY5pcWKrdHnvckBw\iCqdX3hckBUVkdvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlA{PTRizszN MXHTRW5ITVJ?
human IGROV-1 cell M1e4Rmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEnSUHdKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? NUXHZlR5W0GQR1XS
human KYSE-270 cell MlT6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{Lub2lvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2yO|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJzNk[4JO69VQ>? M1ftRXNCVkeHUh?=
human NTERA-S-cl-D1 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4O1bmlvcGmkaYTpc44hd2ZiaIXtZY4hVlSHUlGtV{1kdC2GMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlM4PCEQvF2= MX3TRW5ITVJ?
human LoVo cell MomyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoXVTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFA6OSEQvF2= NWfyN4tCW0GQR1XS
human MOLT-16 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVnJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI2QDJ|IN88US=> MVTTRW5ITVJ?
human P30-OHK cell NWHjfJNzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnzbYVKdmirYnn0bY9vKG:oIHj1cYFvKFB|MD3PTGsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ4M{i4JO69VQ>? MmT1V2FPT0WU
human HUTU-80 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGhWXFVvOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI5PTB{IN88US=> MWLTRW5ITVJ?
human MIA-PaCa-2 cell Mme0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnQNHJFUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlA1KM7:TR?= NYTI[G9CW0GQR1XS
human HCC2157 cell NWW1XFI4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUjqdoYyUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkOxOkDPxE1? NWLVe|JkW0GQR1XS
human HCT-15 cell NU\IRmszT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFjtfo1KdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ5MEWg{txO NXTR[XNrW0GQR1XS
human 786-0 cell M2XJOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HlVGlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> NXHOdWpyW0GQR1XS
human GDM-1 cell M2nCWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVXGTHh{UW6qaXLpeIlwdiCxZjDoeY1idiCJRF2tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzV{M{mg{txO NX;0UpFVW0GQR1XS
human NCI-H2009 cell M3HyeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGXQ[Y9KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlAxQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{[zN|Yh|ryP NWTLcWFGW0GQR1XS
human TE-15 cell NGLzco5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOlQ3OiEQvF2= NYP5dWl7W0GQR1XS
human NCI-H2342 cell NU\0b25QT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzd7OEOg{txO M4DmO3NCVkeHUh?=
human RT-112 cell NXvaOW1qT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1rjU2lvcGmkaYTpc44hd2ZiaIXtZY4hWlRvMUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QDF5NjFOoI0> NULtU3hIW0GQR1XS
human HCC2998 cell NHvsPItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHPenhKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6NEO2JO69VQ>? NH72PFRUSU6JRWK=
human HEL cell M4[ycmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{m0OFkh|ryP MVzTRW5ITVJ?
human NMC-G1 cell M3LabWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1T3cmlvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjVyNTFOwG0> NFTP[2ZUSU6JRWK=
human 8505C cell NUTaS29WT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\BPXNtUW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO NXHX[pFtW0GQR1XS
human HLE cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3m5e2lvcGmkaYTpc44hd2ZiaIXtZY4hUEyHIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OFgyOSEQvF2= MX3TRW5ITVJ?
human KGN cell NEeyVYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFvqO|hKdmirYnn0bY9vKG:oIHj1cYFvKEuJTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFUzPDlizszN MY\TRW5ITVJ?
human EW-18 cell Mmq1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTF6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVc6OSEQvF2= NH:xVoZUSU6JRWK=
human OCUB-M cell NH7wdpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXzmU5BJUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2XCMW0h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR5MU[0JO69VQ>? M3ToOHNCVkeHUh?=
human SW620 cell M1O1XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIX6S2NKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDJ{NDFOwG0> Ml3wV2FPT0WU
human SK-MEL-2 cell NWXDZnhmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4DEfWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR6M{ezJO69VQ>? NXj0c20zW0GQR1XS
human G-401 cell NYLZeIlHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmnwTY5pcWKrdHnvckBw\iCqdX3hckBINTRyMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVAzPjFizszN MnTMV2FPT0WU
human HT-29 cell NFy1fpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXLJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61OFY4KM7:TR?= NILqWZpUSU6JRWK=
human A427 cell NHj2XnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlH6TY5pcWKrdHnvckBw\iCqdX3hckBCPDJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61O|kyPyEQvF2= MUDTRW5ITVJ?
human A375 cell NXvs[nVMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGE{PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[xOlQ5KM7:TR?= MVvTRW5ITVJ?
SNU-449 cell M3HQ[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVnJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYzOjl2IN88US=> NVjQXIwxW0GQR1XS
human A431 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NU\mfFFzUW6qaXLpeIlwdiCxZjDoeY1idiCDNEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43PTV|NjFOwG0> NHj4fo5USU6JRWK=
human NCI-H1299 cell M3G2Rmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV;Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUK5PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjl|MEig{txO NELDW4pUSU6JRWK=
human SNU-423 cell NETLb|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{GxT2lvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzB2Nk[g{txO MXzTRW5ITVJ?
human SW1710 cell Ml32S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml7aTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlczPTVizszN NF;tTFhUSU6JRWK=
human KYSE-450 cell NE\WTohIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NULtWmVMUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{K4PFUh|ryP NGDZfYRUSU6JRWK=

... 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
in solvent
Synonyms R115777

Bio Calculators

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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