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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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 M4njSWZ2dmO2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N MmjCNlA1Ojl3MUG=
NIH3T3 cells NVPZN2N3TnWwY4Tpc44h[XO|YYm= NVTEOItiUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? MkO2NVU6OTF{OEG=
human RPMI-6666 cell M3;1XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvNk[2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvPDFibl2= Mo\kV2FPT0WU
human ML-2 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mk\LTY5pcWKrdHnvckBw\iCqdX3hckBOVC1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOlQhdk1? MYrTRW5ITVJ?
human SIG-M5 cell MlThS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF3mO45KdmirYnn0bY9vKG:oIHj1cYFvKFOLRz3NOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV5IH7N MXrTRW5ITVJ?
human QIMR-WIL cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvOzFibl2= NYrPTXFXW0GQR1XS
human A4-Fuk cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlU6KG6P MVLTRW5ITVJ?
human ETK-1 cell NFq2[YNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYfUVo96UW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV{IH7N M1zhOXNCVkeHUh?=
human MEL-JUSO cell MnXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmHYTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSmXTU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjR2IH7N M2HEOXNCVkeHUh?=
human NALM-6 cell MkDkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFnMe|NKdmirYnn0bY9vKG:oIHj1cYFvKE6DTF2tOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM3NjJzIH7N MnPOV2FPT0WU
human IA-LM cell NF7tbnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXuzTlVUUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjV{IH7N Mmi2V2FPT0WU
human Daoy cell M3TWT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWC4SoczUW6qaXLpeIlwdiCxZjDoeY1idiCGYX;5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVcvPTNibl2= NE\X[pdUSU6JRWK=
human REH cell NH:3SYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEHLfFFKdmirYnn0bY9vKG:oIHj1cYFvKFKHSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUW5MlIhdk1? NF;FflhUSU6JRWK=
human KU812 cell NGHTOHVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYrQdWZqUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk4NjB4IH7N NUOye2FWW0GQR1XS
human KM12 cell NHfmeGhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLxXmJKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=> M{S4[HNCVkeHUh?=
human LCLC-103H cell M1nKOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFrDfHlKdmirYnn0bY9vKG:oIHj1cYFvKEyFTFOtNVA{UCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUK5NFIh|ryP MVrTRW5ITVJ?
human BC-1 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M33RUWlvcGmkaYTpc44hd2ZiaIXtZY4hSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVI6QTZizszN M{[2VXNCVkeHUh?=
human CMK cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1PVXWlvcGmkaYTpc44hd2ZiaIXtZY4hS02NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOVE1PSEQvF2= NV;mcGVkW0GQR1XS
human MCF7 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlzCTY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlY{KM7:TR?= NHzrZ3NUSU6JRWK=
human Calu-1 cell NGXSbplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVgyOzRizszN MYLTRW5ITVJ?
human SK-LMS-1 cell NHzLb2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1zIVmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTF3TMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF6NEC5JO69VQ>? NWT2[GN{W0GQR1XS
human HH cell NHy3b3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYG4Zmh{UW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVkxQDlizszN MmLKV2FPT0WU
human NCI-H2122 cell MnTES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPMUpZbUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= MkfLV2FPT0WU
human SNG-M cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUnjTXJHUW6qaXLpeIlwdiCxZjDoeY1idiCVTletUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB|NUSg{txO NGezXIRUSU6JRWK=
human IGROV-1 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEP2bWxKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? MorSV2FPT0WU
human KYSE-270 cell M3XC[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXjKd21rUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVI4OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkG2Olgh|ryP M2rCV3NCVkeHUh?=
human NTERA-S-cl-D1 cell M17TWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkKzO|Qh|ryP M37hW3NCVkeHUh?=
human LoVo cell NYrrU21[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1SwTmlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQxQTFizszN NYTadnp1W0GQR1XS
human MOLT-16 cell NGrqfJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILIVGtKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ3OEKzJO69VQ>? NXvVUFdlW0GQR1XS
human P30-OHK cell M4r1TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYD0SZFqUW6qaXLpeIlwdiCxZjDoeY1idiCSM{CtU2hMKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{NkO4PEDPxE1? MYnTRW5ITVJ?
human HUTU-80 cell NXfpdmJDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MojzTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQDVyMjFOwG0> NXzCWXNrW0GQR1XS
human MIA-PaCa-2 cell M1LuNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnrETY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkC0JO69VQ>? Mo[1V2FPT0WU
human HCC2157 cell NH\0SJpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVrCO4VOUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|MkOxOkDPxE1? NHj1ephUSU6JRWK=
human HCT-15 cell NWq4XphvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXm5eJp6UW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{N{C1JO69VQ>? M3nneHNCVkeHUh?=
human 786-0 cell NFPpT3NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEDNU3FKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjF5MzFOwG0> NX7uXpV5W0GQR1XS
human GDM-1 cell M2rSW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml\TTY5pcWKrdHnvckBw\iCqdX3hckBITE1vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|UzOzlizszN NGXzNJpUSU6JRWK=
human NCI-H2009 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NELGSFVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlAxQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{[zN|Yh|ryP MlvQV2FPT0WU
human TE-15 cell NUnsfmlFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOlQ3OiEQvF2= M13Vd3NCVkeHUh?=
human NCI-H2342 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzd7OEOg{txO M{Hmb3NCVkeHUh?=
human RT-112 cell NFrJc|VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWXJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|gyPzZizqzt NXntU4JCW0GQR1XS
human HCC2998 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWXtXJNqUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|OESzOkDPxE1? NWfGfZZjW0GQR1XS
human HEL cell NGO0UWtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXnhTGFkUW6qaXLpeIlwdiCxZjDoeY1idiCKRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM6PDR7IN88US=> MoHnV2FPT0WU
human NMC-G1 cell MkmxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFI2ODVizszN MlK5V2FPT0WU
human 8505C cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF:ze49KdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0> M4jMS3NCVkeHUh?=
human HLE cell MmrJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNES4NVEh|ryP M1LrWXNCVkeHUh?=
human KGN cell NYHncIFsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGtIViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEWyOFkh|ryP MmL3V2FPT0WU
human EW-18 cell M{LIcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHvFTINKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PTd7MTFOwG0> MUTTRW5ITVJ?
human OCUB-M cell M1\BUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFcyPjRizszN MnKwV2FPT0WU
human SW620 cell MonJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFfacpFKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDJ{NDFOwG0> M4LsOXNCVkeHUh?=
human SK-MEL-2 cell MmTPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NELhTnVKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OEO3N{DPxE1? MnS2V2FPT0WU
human G-401 cell NVi1RY9mT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TmbGlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> NY\ybHhJW0GQR1XS
human HT-29 cell NIPSUW5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61OFY4KM7:TR?= NXnoTGVzW0GQR1XS
human A427 cell NFS4dVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXjhUoJqUW6qaXLpeIlwdiCxZjDoeY1idiCDNEK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42PzlzNzFOwG0> MmD3V2FPT0WU
human A375 cell MmLlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoH4TY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62NVY1QCEQvF2= MkXFV2FPT0WU
SNU-449 cell M3PkUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU\wRYE{UW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkK5OEDPxE1? MlTFV2FPT0WU
human A431 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUDIeJJtUW6qaXLpeIlwdiCxZjDoeY1idiCDNEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43PTV|NjFOwG0> M13GZ3NCVkeHUh?=
human NCI-H1299 cell NFjZZZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXiZW1KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVI6QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkmzNFgh|ryP M{nSVHNCVkeHUh?=
human SNU-423 cell NFHqOWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH\ZdnZKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjdyNE[2JO69VQ>? MkXRV2FPT0WU
human SW1710 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4fNeWlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjV3IN88US=> MojWV2FPT0WU
human KYSE-450 cell NGmwV5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjTWo0xUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{K4PFUh|ryP MoLwV2FPT0WU

... 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

Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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).

Dilution Calculator

Dilution Calculator

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

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Molecular Weight Calculator

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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03496766 Recruiting Non Small Cell Lung Cancer Spanish Lung Cancer Group May 7 2018 Phase 2
NCT00082888 Active not recruiting Anaplastic Large Cell Lymphoma|Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue|Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Nodal Marginal Zone Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-Cell Leukemia/Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma National Cancer Institute (NCI) March 24 2004 Phase 2
NCT02807272 Recruiting Leukemia Myelomonocytic Chronic Kura Oncology Inc. October 2016 Phase 2
NCT02779777 Recruiting Myelodysplastic Syndromes Kura Oncology Inc. May 2016 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

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