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 NWnRS4VtTnWwY4Tpc44h[XO|YYm= MWLJcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N NVfI[WV4OjB2Mkm1NVE>
NIH3T3 cells NYHibIw5TnWwY4Tpc44h[XO|YYm= NXLMXppQUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1? M4jxRVE2QTFzMkix
human RPMI-6666 cell NUX6RpAzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmTCTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLU[2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjRzIH7N M1TTW3NCVkeHUh?=
human ML-2 cell NGPPZo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PhfmlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlY1KG6P NITpOoJUSU6JRWK=
human SIG-M5 cell NG\UT2RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFGye3pKdmirYnn0bY9vKG:oIHj1cYFvKFOLRz3NOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV5IH7N MkPoV2FPT0WU
human QIMR-WIL cell MkC5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXjJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvOzFibl2= NYn5Z|U2W0GQR1XS
human A4-Fuk cell NIXHd5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFTod5FKdmirYnn0bY9vKG:oIHj1cYFvKEF2LV\1b{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIxNjV7IH7N M3T4cXNCVkeHUh?=
human ETK-1 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUTU[2lOUW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV{IH7N MlrQV2FPT0WU
human MEL-JUSO cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJG1GVC2MVWPPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvPDRibl2= M{XncnNCVkeHUh?=
human NALM-6 cell NYKyPGs6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkD4TY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk4zOSCwTR?= NH\3ZlJUSU6JRWK=
human IA-LM cell NITVZXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEnyb3lKdmirYnn0bY9vKG:oIHj1cYFvKEmDLVzNJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFcvPTJibl2= M{P5XXNCVkeHUh?=
human Daoy cell NX\WeZRFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkK2TY5pcWKrdHnvckBw\iCqdX3hckBF[W:7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUeuOVMhdk1? MYrTRW5ITVJ?
human REH cell MlOzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUPS[o1JUW6qaXLpeIlwdiCxZjDoeY1idiCURVigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PU4zKG6P NXLEe4VOW0GQR1XS
human KU812 cell NEHLToRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVfJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUeuNFYhdk1? NILqOXdUSU6JRWK=
human KM12 cell M4O2SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWnJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGxOlg3KM7:TR?= NYTTcI5WW0GQR1XS
human LCLC-103H cell NV7JcXNLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXTJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO MWrTRW5ITVJ?
human BC-1 cell NInUbFNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGJENTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyPVk3KM7:TR?= NF3iUFhUSU6JRWK=
human CMK cell NXPNcpI5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFXkU4tKdmirYnn0bY9vKG:oIHj1cYFvKEOPSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVUyPDVizszN NWm1fIprW0GQR1XS
human MCF7 cell NH:3TJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXnIXm5GUW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPjZ|IN88US=> MnP2V2FPT0WU
human Calu-1 cell M1Pje2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVgyOzRizszN M3nvWnNCVkeHUh?=
human SK-LMS-1 cell NXT4RVdKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mk\kTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTh2MEmg{txO NIrzVWxUSU6JRWK=
human HH cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUXTeXNTUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVkxQDlizszN M2XIbHNCVkeHUh?=
human NCI-H2122 cell M2PtW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHjUZZnUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?= MX3TRW5ITVJ?
human SNG-M cell NYnHcmdWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH62eIdKdmirYnn0bY9vKG:oIHj1cYFvKFOQRz3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODN3NDFOwG0> MneyV2FPT0WU
human IGROV-1 cell MnrWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYnObnhCUW6qaXLpeIlwdiCxZjDoeY1idiCLR2LPWk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MEiyN{DPxE1? M3jEbnNCVkeHUh?=
human KYSE-270 cell Ml;DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVHBb5NLUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVI4OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkG2Olgh|ryP NETINYRUSU6JRWK=
human NTERA-S-cl-D1 cell NHvoN4JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2\3RWlvcGmkaYTpc44hd2ZiaIXtZY4hVlSHUlGtV{1kdC2GMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlM4PCEQvF2= NHLiXWhUSU6JRWK=
human LoVo cell MlHxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXjQ[3lyUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDB7MTFOwG0> Ml6wV2FPT0WU
human MOLT-16 cell NELzcXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI2QDJ|IN88US=> M1rHeHNCVkeHUh?=
human P30-OHK cell NWHseVIzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFywUIJKdmirYnn0bY9vKG:oIHj1cYFvKFB|MD3PTGsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ4M{i4JO69VQ>? MYXTRW5ITVJ?
human HUTU-80 cell M3jMN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFy4TVZKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ6NUCyJO69VQ>? NGTYcXVUSU6JRWK=
human MIA-PaCa-2 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEW5cmNKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh|ryP NXfuc21{W0GQR1XS
human HCC2157 cell MnfhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOzF4IN88US=> NXW2N3I6W0GQR1XS
human HCT-15 cell NIfKe4RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|I4ODVizszN M{jBfHNCVkeHUh?=
human 786-0 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mom1TY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN MoLxV2FPT0WU
human GDM-1 cell NWHWbIRJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEGwb5NKdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTJ|OTFOwG0> MkW1V2FPT0WU
human NCI-H2009 cell MmTFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkK4TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN4M{O2JO69VQ>? NHToS|JUSU6JRWK=
human TE-15 cell NEDNbVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWHJXFNZUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO MVHTRW5ITVJ?
human NCI-H2342 cell NHHJRZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoDYTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN5OUizJO69VQ>? NYfX[4hJW0GQR1XS
human RT-112 cell NF\Nc2tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|gyPzZizqzt MXzTRW5ITVJ?
human HCC2998 cell NF3S[41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFzGflNKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6NEO2JO69VQ>? MnKzV2FPT0WU
human HEL cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4DXXGlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zPVQ1QSEQvF2= M1HkZnNCVkeHUh?=
human NMC-G1 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkOzTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQzPTB3IN88US=> NV6zeVVJW0GQR1XS
human 8505C cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH\kbnhKdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0> NU\ac3g6W0GQR1XS
human HLE cell NFTIdnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNES4NVEh|ryP Ml3lV2FPT0WU
human KGN cell Mn;DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4j1d2lvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= MoTSV2FPT0WU
human EW-18 cell NEjoXJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUjtPVZ6UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDV5OUGg{txO MUTTRW5ITVJ?
human OCUB-M cell M3TnSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M176eWlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PzF4NDFOwG0> NV\OVGsyW0GQR1XS
human SW620 cell MofGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1\mSGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=> M1fOZ3NCVkeHUh?=
human SK-MEL-2 cell NWDkcmNiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUL0Om1VUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEizO|Mh|ryP MUXTRW5ITVJ?
human G-401 cell M1rEZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{fJ[WlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=> MV3TRW5ITVJ?
human HT-29 cell MnjJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmL0TY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVQ3PyEQvF2= NWXGNIdIW0GQR1XS
human A427 cell NHvjc4NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGC1cINKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU4QTF5IN88US=> M1vuc3NCVkeHUh?=
human A375 cell MkCwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;CR4lKdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=> NHzIOoNUSU6JRWK=
SNU-449 cell NY\WS2w1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\mXIRrUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkK5OEDPxE1? M17aPXNCVkeHUh?=
human A431 cell M1;PVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn7vTY5pcWKrdHnvckBw\iCqdX3hckBCPDNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62OVU{PiEQvF2= M1rSdXNCVkeHUh?=
human NCI-H1299 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnvaTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGyPVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ7M{C4JO69VQ>? MX7TRW5ITVJ?
human SNU-423 cell NH;1[WlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLhTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0> MUHTRW5ITVJ?
human SW1710 cell NXvRcFVST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUXuUYlPUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd{NUWg{txO MXHTRW5ITVJ?
human KYSE-450 cell M{TCRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\wS2lvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT20OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd{OEi1JO69VQ>? M1;s[nNCVkeHUh?=

... 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:

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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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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