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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Cited by 18 Publications

6 Customer Reviews

  • 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.

  • 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.

  • 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.

  • 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.

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 Mki0SpVv[3Srb36gZZN{[Xl? M1TiU2lvcGmkaYTpc44hd2ZicnH0JJJm[2:vYnnuZY51KFCIVDDlfJBz\XO|ZXSgbY4hcW6|ZXP0JHNnQSClZXzsd{BjgSC|Y3nueIltdGG2aX;uJJBzd3irbXn0fUBie3OjeTygTWM2OD1yLkegcm0> NFT6XWQzODR{OUWxNS=>
NIH3T3 cells NE\EOG1HfW6ldHnvckBie3OjeR?= NFPI[G1KdmirYnn0bY9vKG:oIGLhd{Bxem:lZYPzbY5oKGmwIFitdoF{KHS{YX7z[o9zdWWmIF7JTFNVOyClZXzsd{BqdiCycnXz[Y5k\SCxZjDUbZBq\mG{bnniMEBGSzVyPUGuOkBvVQ>? MUWxOVkyOTJ6MR?=
human RPMI-6666 cell NYSwSGdTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nQemlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=> M1vrbnNCVkeHUh?=
human ML-2 cell NFrNN49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXzJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>? MmjIV2FPT0WU
human SIG-M5 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{fNPWlvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTdibl2= M2jiO3NCVkeHUh?=
human QIMR-WIL cell NEewRXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVHFZ5loUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkOxJI5O NEfUe5hUSU6JRWK=
human A4-Fuk cell NVy5enlmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlU6KG6P MojaV2FPT0WU
human ETK-1 cell M{PZVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4POPGlvcGmkaYTpc44hd2ZiaIXtZY4hTVSNLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU42OiCwTR?= MnvWV2FPT0WU
human MEL-JUSO cell NHrkbnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlGwTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSmXTU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjR2IH7N NELKclhUSU6JRWK=
human NALM-6 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2HHZ2lvcGmkaYTpc44hd2ZiaIXtZY4hVkGOTT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|YvOjFibl2= NFHpUHNUSU6JRWK=
human IA-LM cell MmK0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4DuXmlvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20O{42OiCwTR?= NVz3UGZQW0GQR1XS
human Daoy cell NVvNUHc{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIHr[HJKdmirYnn0bY9vKG:oIHj1cYFvKESjb4mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21O{42OyCwTR?= MojXV2FPT0WU
human REH cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUDJcohq[mm2aX;uJI9nKGi3bXHuJHJGUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV7LkKgcm0> NInOXXVUSU6JRWK=
human KU812 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1j4cmlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{4xPiCwTR?= MoDtV2FPT0WU
human KM12 cell M{L3Z2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MonHTY5pcWKrdHnvckBw\iCqdX3hckBMVTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVY5PiEQvF2= NWDiRWZFW0GQR1XS
human LCLC-103H cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MliyTY5pcWKrdHnvckBw\iCqdX3hckBNS0yFLUGwN2gh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF{OUCyJO69VQ>? M3jmOXNCVkeHUh?=
human BC-1 cell NU\zR|V[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGJENTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyPVk3KM7:TR?= MYfTRW5ITVJ?
human CMK cell NGH3fpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3fBbGlvcGmkaYTpc44hd2ZiaIXtZY4hS02NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOVE1PSEQvF2= MoPRV2FPT0WU
human MCF7 cell M1rNeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1\JSWlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVY3OyEQvF2= M3TuZ3NCVkeHUh?=
human Calu-1 cell NVvDRZRzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3XKe2lvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDF|NDFOwG0> MXTTRW5ITVJ?
human SK-LMS-1 cell NYLlZ4hDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MofPTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTh2MEmg{txO M1zC[nNCVkeHUh?=
human HH cell M1vZeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYO4N4lLUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVkxQDlizszN NYriPXlpW0GQR1XS
human NCI-H2122 cell NUmyO5A3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TxcWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOUG0OUDPxE1? MmO3V2FPT0WU
human SNG-M cell M2PCfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHvGOnpKdmirYnn0bY9vKG:oIHj1cYFvKFOQRz3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODN3NDFOwG0> NFjr[mFUSU6JRWK=
human IGROV-1 cell M2fxbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHixOYpKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>? NYH0RVd{W0GQR1XS
human KYSE-270 cell NVT1OoM2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{fTSGlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2yO|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJzNk[4JO69VQ>? NGHHXGtUSU6JRWK=
human NTERA-S-cl-D1 cell NI\wTmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkDNTY5pcWKrdHnvckBw\iCqdX3hckBPXEWUQT3TMYNtNURzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yN|c1KM7:TR?= NHn5bJZUSU6JRWK=
human LoVo cell MonDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnq3TY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFA6OSEQvF2= M4fvbXNCVkeHUh?=
human MOLT-16 cell NVz1cGNoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{\ER2lvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO MlS4V2FPT0WU
human P30-OHK cell M3m3UWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2na[2lvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjZ|OEig{txO NID4dmNUSU6JRWK=
human HUTU-80 cell NUjhTZNyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX[5VJBtUW6qaXLpeIlwdiCxZjDoeY1idiCKVWTVMVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{OEWwNkDPxE1? NVX0OJhOW0GQR1XS
human MIA-PaCa-2 cell NIfMZ5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHjtOFdKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh|ryP NF3K[HVUSU6JRWK=
human HCC2157 cell NEDtS3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUnJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOzF4IN88US=> MULTRW5ITVJ?
human HCT-15 cell M3;MNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmH4TY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=> M4rp[3NCVkeHUh?=
human 786-0 cell NVTI[mhxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml\hTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN MV3TRW5ITVJ?
human GDM-1 cell M4SxNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1;UT2lvcGmkaYTpc44hd2ZiaIXtZY4hT0SPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2OjN7IN88US=> M4SwZXNCVkeHUh?=
human NCI-H2009 cell MmO4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MorwTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN4M{O2JO69VQ>? NXzD[XhJW0GQR1XS
human TE-15 cell NIi1NZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWPHTJlVUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO MU\TRW5ITVJ?
human NCI-H2342 cell NH:zdYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIDab|JKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlM1OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{e5PFMh|ryP MYrTRW5ITVJ?
human RT-112 cell MlSzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEHGO4lKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzhzN{[g{rxu NVfTV3hWW0GQR1XS
human HCC2998 cell M3zId2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFH5TJVKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6NEO2JO69VQ>? M4fSfHNCVkeHUh?=
human HEL cell MoLqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M17JbmlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zPVQ1QSEQvF2= Ml7YV2FPT0WU
human NMC-G1 cell NVTKeJVpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFI2ODVizszN NV3hWJVUW0GQR1XS
human 8505C cell NF6ydpRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4L5[mlvcGmkaYTpc44hd2ZiaIXtZY4hQDVyNVOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ{OTB7IN88US=> MkThV2FPT0WU
human HLE cell MlHIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYDJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNES4NVEh|ryP MkfVV2FPT0WU
human KGN cell NYfifZdsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rINGlvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OVI1QSEQvF2= NEPGN4dUSU6JRWK=
human EW-18 cell M{LzfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUnk[YVWUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDV5OUGg{txO M3vPZXNCVkeHUh?=
human OCUB-M cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mk\ETY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4OTZ2IN88US=> MUfTRW5ITVJ?
human SW620 cell MlLrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjJyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PFIzPCEQvF2= M1vv[HNCVkeHUh?=
human SK-MEL-2 cell MofvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkTkTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDh|N{Og{txO NV7kNnI2W0GQR1XS
human G-401 cell MmnJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFy3XIJKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42ODJ4MTFOwG0> M{nUeHNCVkeHUh?=
human HT-29 cell NVz3VlNvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUj5RY5YUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2yPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTR4NzFOwG0> M{DTPHNCVkeHUh?=
human A427 cell MoXMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEfXcHJKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU4QTF5IN88US=> MWnTRW5ITVJ?
human A375 cell MnzuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFvWSm5KdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=> NEWxcI9USU6JRWK=
SNU-449 cell Mn7TS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2XLVGlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUS0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjJ{OUSg{txO NH7vco5USU6JRWK=
human A431 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV\JNmFWUW6qaXLpeIlwdiCxZjDoeY1idiCDNEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43PTV|NjFOwG0> MVzTRW5ITVJ?
human NCI-H1299 cell MkP4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUTpXodDUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFEzQTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[5N|A5KM7:TR?= NHKzcnpUSU6JRWK=
human SNU-423 cell NHe2VoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{n5U2lvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzB2Nk[g{txO NVzZS2Z3W0GQR1XS
human SW1710 cell M3nMcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkPVTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlczPTVizszN MVHTRW5ITVJ?
human KYSE-450 cell NU[zN4NsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXT0RXNiUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{K4PFUh|ryP NFTH[IlUSU6JRWK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Caspase-12 / PARP1; 

PubMed: 21378206     


Western blot analysis of protein extracts from U937 cells incubated in normal media (Control) or media containing tipifarnib at the indicated concentrations. Extracts were probed using antibodies directed against cleaved caspase-12, PARP1 (full-length and cleaved), and β-actin, with the latter used as a lane loading reference. 

Rheb / p-mTOR / mTOR / p-P70S6K / P70 S6K / p-S6 / S6 ; 

PubMed: 23996484     


After U937 cells were treated for 24 h with the indicated tipifarnib concentration, whole cell lysates were subjected to immunoblotting with antibodies that recognize the indicated antigens. GAPDH served as a loading control. In this and subsequent figures, gray arrow indicates farnesylated antigen and black arrow indicates unfarnesylated antigen. 

Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Puma / Noxa / Bim / Lamin B; 

PubMed: 23996484     


After U937 cells were treated for 6 days with the indicated tipifarnib concentration, whole cell lysates were subjected to immunoblotting with antibodies that recognize the indicated polypeptides.

HDJ-2 / N-Ras / FKBP51 / p-AKT / AKT; 

PubMed: 23996484     


Whole cell lysates prepared from parental U937 cells treated for 48 h with diluent or 800 nM tipifarnib (lanes 2 and 3, respectively) or from tipifarnib-resistant cells growing in 800 nM tipifarnib (lane 1) were subjected to SDS-PAGE followed by immunoblotting with antibodies that recognize the indicated antigen.

p-c-Raf / c-Raf / p-MEK / MEK / p-ERK / ERK; 

PubMed: 21673341     


After Jurkat cells were treated for 72 hours with the indicated tipifarnib concentration in the presence of 5μM Q-VD-OPh, whole cell lysates were subjected to immunoblotting with antibodies that recognize the indicate polypeptides. Ribosomal protein S6 and Hsp90 served as loading controls. 

21378206 23996484 21673341
Growth inhibition assay
Cell viability; 

PubMed: 26630652     


NCI-H929, INA6, MM.1S, and RPMI-8226 MM cell lines were cultured with tipifarnib (0–20 μM), dabrafenib (0–20 μM), or AZD6244 (0–20 μM) for 72 h. In each case, cell viability was assessed with the MTT assay of triplicate cultures and expressed as the percentage of the untreated control. Data are the mean ± SD.

26630652
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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03719690 Not yet recruiting HRAS Gene Mutation|HNSCC Kura Oncology Inc. December 2018 Phase 2
NCT03719690 Not yet recruiting HRAS Gene Mutation|HNSCC Kura Oncology Inc. December 2018 Phase 2
NCT03496766 Recruiting Non Small Cell Lung Cancer Spanish Lung Cancer Group May 7 2018 Phase 2
NCT03496766 Recruiting Non Small Cell Lung Cancer Spanish Lung Cancer Group May 7 2018 Phase 2
NCT02807272 Recruiting Leukemia Myelomonocytic Chronic Kura Oncology Inc. October 2016 Phase 2
NCT02807272 Recruiting Leukemia Myelomonocytic Chronic Kura Oncology Inc. October 2016 Phase 2

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID