Tipifarnib

Catalog No.S1453 Synonyms: R115777

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.

Cited by 21 Publications

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

J Endocrinol Invest, 2019, 42(5):527-540

PubMed: 30191474 ( click the link to review the publication )

Nat Commun, 2018, 9(1):1524

PubMed: 29670091 ( click the link to review the publication )

Mol Oncol, 2018, 12(11):1895-1916

PubMed: 30009399 ( click the link to review the publication )

Exp Ther Med, 2018, 15(2):1314-1320

PubMed: 29434718 ( click the link to review the publication )

Acta Biol Hung, 2018, 69(4):395-410

PubMed: 30587022 ( click the link to review the publication )

Sci Rep, 2016, 6:34798

PubMed: 27739443 ( click the link to review the publication )

PLoS One, 2015, 10(12):e0143847

PubMed: 26630652 ( click the link to review the publication )

Stem Cells Transl Med, 2014, 3(4):510-9

PubMed: 24598781 ( click the link to review the publication )

Transl Res, 2014, 164(5):411-23

PubMed: 25016932 ( click the link to review the publication )

Shock, 2014, 42(6):570-7

PubMed: 25046541 ( click the link to review the publication )

Leuk Res, 2014, 38(11):1350-7

PubMed: 25262449 ( click the link to review the publication )

Universidade de Lisboa, 2014, Matias

PubMed: ( click the link to review the publication )

J Clin Endocrinol Metab, 2013, 98(6):2502-12

PubMed: 23559083 ( click the link to review the publication )

Phytochemistry, 2013, 98:190-6

PubMed: 24361288 ( click the link to review the publication )

Ann Clin Microbiol Antimicrob, 2013, 12(1):37

PubMed: 24314136 ( click the link to review the publication )

Cancer Chemoth Pharm, 2013, 72(3):683-97

PubMed: 23934261 ( click the link to review the publication )

University of Kentucky, 2013, Tamer Ahmed

PubMed: ( click the link to review the publication )

Clin Cancer Res, 2012, 18(13):3524-31

PubMed: 22529099 ( click the link to review the publication )

Pediatr Neurol, 2012, 46(4):203-11

PubMed: 22490764 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description

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	Activity Description	PMID
Sf9 cells	NV\Sd\|JoTnWwY4Tpc44h[XO\|YYm=	NYTte48zUW6qaXLpeIlwdiCxZjDyZZQhemWlb33ibY5idnRiUF\UJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGK7IIPjbY51cWyuYYTpc44heHKxeHntbZR6KGG\|c3H5MEBKSzVyPUCuO{BvVQ>?	NYLpUW9xOjB2Mkm1NVE>
NIH3T3 cells	MX3GeY5kfGmxbjDhd5NigQ>?	NYXEfmtiUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1?	NFP3c3cyPTlzMUK4NS=>
human RPMI-6666 cell	NEPXZXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3rsfGlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=>	Mn3xV2FPT0WU
human ML-2 cell	MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3jNdGlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUGzMlY1KG6P	NH72RplUSU6JRWK=
human SIG-M5 cell	M2rLNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MmXQTY5pcWKrdHnvckBw\iCqdX3hckBUUUdvTUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PyCwTR?=	NHnubVZUSU6JRWK=
human QIMR-WIL cell	MojES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHLw[FBKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwM{Ggcm0>	MVXTRW5ITVJ?
human A4-Fuk cell	NELBOGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NWDIbHBuUW6qaXLpeIlwdiCxZjDoeY1idiCDND3GeYsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOC53OTDuUS=>	MoDUV2FPT0WU
human ETK-1 cell	MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NEfQ[XdKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTJibl2=	MnG5V2FPT0WU
human MEL-JUSO cell	MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NEiycolKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3KWXNQKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwNESgcm0>	Mlq4V2FPT0WU
human NALM-6 cell	MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MkKwTY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk4zOSCwTR?=	M1:2cnNCVkeHUh?=
human IA-LM cell	M4ToTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NX3QRoNxUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjV{IH7N	M1O1SHNCVkeHUh?=
human Daoy cell	Mn[wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NWXW[WI6UW6qaXLpeIlwdiCxZjDoeY1idiCGYX;5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVcvPTNibl2=	NX\QeIEzW0GQR1XS
human REH cell	MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1;yW2lvcGmkaYTpc44hd2ZiaIXtZY4hWkWKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NUmuNkBvVQ>?	MofGV2FPT0WU
human KU812 cell	MnTTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NY\3WotrUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk4NjB4IH7N	NVfFUGFvW0GQR1XS
human KM12 cell	NH3YN4FIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NFG4OmFKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=>	NGPxcY5USU6JRWK=
human LCLC-103H cell	NFT4bWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MWfJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO	MVTTRW5ITVJ?
human BC-1 cell	M1jLNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NXLLbY81UW6qaXLpeIlwdiCxZjDoeY1idiCEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOjl7NjFOwG0>	MonkV2FPT0WU
human CMK cell	Mnn1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NXy0VFVuUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=>	NH\ObI1USU6JRWK=
human MCF7 cell	MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NEX6eHRKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE3PjNizszN	MlHSV2FPT0WU
human Calu-1 cell	MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NGH1N3FKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOThzM{Sg{txO	MmjUV2FPT0WU
human SK-LMS-1 cell	NIPTco5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NHLi[plKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOESwPUDPxE1?	NEflUYFUSU6JRWK=
human HH cell	MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MljxTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwMUmwPFkh\|ryP	NWDCbZdoW0GQR1XS
human NCI-H2122 cell	MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NVPXWm1KUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?=	NXfFcY1EW0GQR1XS
human SNG-M cell	NHy3O2ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MnvUTY5pcWKrdHnvckBw\iCqdX3hckBUVkdvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNlA{PTRizszN	NX7IU3FDW0GQR1XS
human IGROV-1 cell	MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MULJcohq[mm2aX;uJI9nKGi3bXHuJGlIWk:YLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxQDJ\|IN88US=>	NWXST4VXW0GQR1XS
human KYSE-270 cell	M1TNe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NIewbnpKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1?	NWraRYhTW0GQR1XS
human NTERA-S-cl-D1 cell	MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NGTTN4FKdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{PzRizszN	M2\PXXNCVkeHUh?=
human LoVo cell	NYDY[2NkT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M3z2OWlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNlQxQTFizszN	MnLCV2FPT0WU
human MOLT-16 cell	NVP5OFNST3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M{nZTmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO	MkGxV2FPT0WU
human P30-OHK cell	MmrQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MYHJcohq[mm2aX;uJI9nKGi3bXHuJHA{OC2RSFugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3Ozh6IN88US=>	Mn;JV2FPT0WU
human HUTU-80 cell	MoS3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MmHTTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQDVyMjFOwG0>	Mmm0V2FPT0WU
human MIA-PaCa-2 cell	MlHXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NUi0T\|l6UW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6zNlA1KM7:TR?=	MVLTRW5ITVJ?
human HCC2157 cell	NH7SUYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MXTJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOzF4IN88US=>	MnvFV2FPT0WU
human HCT-15 cell	MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MoLYTY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=>	MWLTRW5ITVJ?
human 786-0 cell	NHe4[41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NHrKTnNKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjF5MzFOwG0>	NXr1N\|FxW0GQR1XS
human GDM-1 cell	MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MUnJcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6zOVI{QSEQvF2=	NFvVR5VUSU6JRWK=
human NCI-H2009 cell	NH3DR3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NXrDXG5lUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxODliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO2N\|M3KM7:TR?=	M2WzeHNCVkeHUh?=
human TE-15 cell	NYKwb5djT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NW\6UnFmUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO	M1LlWXNCVkeHUh?=
human NCI-H2342 cell	MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M{fSdWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN\|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|N{m4N{DPxE1?	M2e2[nNCVkeHUh?=
human RT-112 cell	MnnuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MVzJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuN\|gyPzZizqzt	MYnTRW5ITVJ?
human HCC2998 cell	Ml\VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4XKUmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzh2M{[g{txO	NXXkNmtqW0GQR1XS
human HEL cell	MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MYDJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwM{m0OFkh\|ryP	NYDZVZBtW0GQR1XS
human NMC-G1 cell	M{LMSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M3H2cGlvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjVyNTFOwG0>	NGDPSoNUSU6JRWK=
human 8505C cell	NIHtZVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NEjqNHJKdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0>	NWHWNFVqW0GQR1XS
human HLE cell	M3:2RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M3XLcmlvcGmkaYTpc44hd2ZiaIXtZY4hUEyHIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD60OFgyOSEQvF2=	MX3TRW5ITVJ?
human KGN cell	M17nUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M2OzT2lvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD60OVI1QSEQvF2=	Mn7aV2FPT0WU
human EW-18 cell	NH75bo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3HkUGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2PzlzIN88US=>	NF;4PGpUSU6JRWK=
human OCUB-M cell	M4PiT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NUTOO5dTUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2XCMW0h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR5MU[0JO69VQ>?	Mn;5V2FPT0WU
human SW620 cell	NVHZOnVUT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M1vKWGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=>	NX;YXId7W0GQR1XS
human SK-MEL-2 cell	Mk\vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NWTFNVFLUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwNEizO\|Mh\|ryP	NXz3cG06W0GQR1XS
human G-401 cell	MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1S5cmlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=>	M2[wOXNCVkeHUh?=
human HT-29 cell	NFzQbnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MUfJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD61OFY4KM7:TR?=	NEXHZYtUSU6JRWK=
human A427 cell	MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NVX5NnNvUW6qaXLpeIlwdiCxZjDoeY1idiCDNEK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42PzlzNzFOwG0>	NH\ZbYZUSU6JRWK=
human A375 cell	Ml30S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NF;oRVdKdmirYnn0bY9vKG:oIHj1cYFvKEF\|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=>	NXf6cWhrW0GQR1XS
SNU-449 cell	MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MoTmTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNES5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OjJ7NDFOwG0>	NVfnc4ppW0GQR1XS
human A431 cell	MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	Mon2TY5pcWKrdHnvckBw\iCqdX3hckBCPDNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD62OVU{PiEQvF2=	MY\TRW5ITVJ?
human NCI-H1299 cell	M{jnbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NEnt[3JKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVI6QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwNkmzNFgh\|ryP	NU\aZlc3W0GQR1XS
human SNU-423 cell	NI\OXVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MmHOTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0>	NFTlVGtUSU6JRWK=
human SW1710 cell	NETtSnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MUfJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuO\|I2PSEQvF2=	M3XhNXNCVkeHUh?=
human KYSE-450 cell	Mk[wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MnLOTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ6OEWg{txO	MlTSV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	Caspase-12 / PARP1; PubMed: 21378206 J Pharmacol Exp Ther 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 Haematologica 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 Haematologica 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 Haematologica 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 Blood 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 PLoS One 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]	- Collapse 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% CO_{2(Only for Reference)}
Animal Research:^[4]	- Collapse 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)

Cell Research:^[4]

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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% CO_{2(Only for Reference)}

Animal Research:^[4]

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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)

References

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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 Download Tipifarnib SDF

Molecular Weight	489.4
Formula	C₂₇H₂₂Cl₂N₄O
CAS No.	192185-72-1
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	R115777

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03496766	Recruiting	Drug: Tipifarnib	Non Small Cell Lung Cancer	Spanish Lung Cancer Group	May 7 2018	Phase 2
NCT02779777	Recruiting	Drug: Tipifarnib	Myelodysplastic Syndromes	Kura Oncology Inc.	May 2016	Phase 2
NCT00510939	Unknown status	Drug: Tipifarnib plus Bortezomib	Acute Myeloid Leukemia	University of Bologna\|Janssen-Cilag Ltd.	March 2007	Phase 2

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Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

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By Signaling Pathways

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Tipifarnib

Cited by 21 Publications

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Tipifarnib SDF

Bio Calculators

Molarity Calculator

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

Tech Support

Transferase Signaling Pathway Map

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)