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 19 Publications

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

PubMed: 31378681 ( 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 )

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

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	Activity Description	PMID
Sf9 cells	M3X2TmZ2dmO2aX;uJIF{e2G7	MV3Jcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N	Mlv1NlA1Ojl3MUG=
NIH3T3 cells	MlT3SpVv[3Srb36gZZN{[Xl?	NUjwPZNQUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1?	NWXWV5lQOTV7MUGyPFE>
human RPMI-6666 cell	M4XFZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NEP4[GNKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtOlY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTdwNEGgcm0>	NYLhO445W0GQR1XS
human ML-2 cell	NWS5[3RtT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M3zOS2lvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUGzMlY1KG6P	M2D0OHNCVkeHUh?=
human SIG-M5 cell	MknDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{HFU2lvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTdibl2=	NGfNe\|RUSU6JRWK=
human QIMR-WIL cell	MkXkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M3zxPWlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5\|MTDuUS=>	NWrX[G82W0GQR1XS
human A4-Fuk cell	NGjwc\|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3myUmlvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlAvPTlibl2=	MmPGV2FPT0WU
human ETK-1 cell	MnTMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NFnR[2lKdmirYnn0bY9vKG:oIHj1cYFvKEWWSz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTJibl2=	NYTDZXJUW0GQR1XS
human MEL-JUSO cell	NEjXWXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3\VVGlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVrVV28h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOy52NDDuUS=>	NFS3UodUSU6JRWK=
human NALM-6 cell	MlvhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MVnJcohq[mm2aX;uJI9nKGi3bXHuJG5CVE1vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUO2MlIyKG6P	Mne2V2FPT0WU
human IA-LM cell	MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MYnJcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NEeuOVIhdk1?	MWDTRW5ITVJ?
human Daoy cell	M3izNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NVHFRnl1UW6qaXLpeIlwdiCxZjDoeY1idiCGYX;5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVcvPTNibl2=	MmL5V2FPT0WU
human REH cell	NWfDT\|dnT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MYTJcohq[mm2aX;uJI9nKGi3bXHuJHJGUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTV7LkKgcm0>	MWXTRW5ITVJ?
human KU812 cell	MonWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{mxNmlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{4xPiCwTR?=	M1mzOHNCVkeHUh?=
human KM12 cell	M3nhZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NGO2coxKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=>	M3jGT3NCVkeHUh?=
human LCLC-103H cell	MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	Ml;uTY5pcWKrdHnvckBw\iCqdX3hckBNS0yFLUGwN2gh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF{OUCyJO69VQ>?	NILuemJUSU6JRWK=
human BC-1 cell	MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MoDMTY5pcWKrdHnvckBw\iCqdX3hckBDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6xNlk6PiEQvF2=	M1G0W3NCVkeHUh?=
human CMK cell	NFjGRmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwMUWxOFUh\|ryP	Mn3zV2FPT0WU
human MCF7 cell	NEHEPGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MlG1TY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6xOlY{KM7:TR?=	M3fwSnNCVkeHUh?=
human Calu-1 cell	NVnBeoVlT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M1PNeWlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDF\|NDFOwG0>	M2SzbXNCVkeHUh?=
human SK-LMS-1 cell	NGO2[4VIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MofQTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTh2MEmg{txO	MWjTRW5ITVJ?
human HH cell	MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NUDSOVY3UW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNVkxQDlizszN	MUTTRW5ITVJ?
human NCI-H2122 cell	MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NF;0SHpKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwMUmxOFUh\|ryP	M{PHdnNCVkeHUh?=
human SNG-M cell	NIrlR2hIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M2fTV2lvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxOzV2IN88US=>	MWnTRW5ITVJ?
human IGROV-1 cell	MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NWjkU2g1UW6qaXLpeIlwdiCxZjDoeY1idiCLR2LPWk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MEiyN{DPxE1?	NG\TWHBUSU6JRWK=
human KYSE-270 cell	Mn\yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NITGdYFKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1?	MVjTRW5ITVJ?
human NTERA-S-cl-D1 cell	M3\NXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MkL1TY5pcWKrdHnvckBw\iCqdX3hckBPXEWUQT3TMYNtNURzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6yN\|c1KM7:TR?=	NH;W[FRUSU6JRWK=
human LoVo cell	Mne1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NX3ac3dtUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDB7MTFOwG0>	NVPqd\|B2W0GQR1XS
human MOLT-16 cell	Mo\XS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4j4UWlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO	M17ETHNCVkeHUh?=
human P30-OHK cell	MmPlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M1HOdmlvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjZ\|OEig{txO	M{LPb3NCVkeHUh?=
human HUTU-80 cell	MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1u1VGlvcGmkaYTpc44hd2ZiaIXtZY4hUFWWVT24NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjh3MEKg{txO	Ml7MV2FPT0WU
human MIA-PaCa-2 cell	MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NGPtTGhKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh\|ryP	NFLkSHFUSU6JRWK=
human HCC2157 cell	M4PpVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MVvJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOzF4IN88US=>	MVPTRW5ITVJ?
human HCT-15 cell	MlfQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	Mn7kTY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=>	M135Z3NCVkeHUh?=
human 786-0 cell	NHXBeVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MnvYTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuN\|IyPzNizszN	MYXTRW5ITVJ?
human GDM-1 cell	MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NITCeYFKdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTJ\|OTFOwG0>	MVnTRW5ITVJ?
human NCI-H2009 cell	NVXnbmJtT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M1HZS2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|NkOzOkDPxE1?	MoTDV2FPT0WU
human TE-15 cell	Mnz4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MmT5TY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuN\|Y1PjJizszN	M33n[HNCVkeHUh?=
human NCI-H2342 cell	MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NXvFSnZyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO3PVg{KM7:TR?=	NYr0SJhkW0GQR1XS
human RT-112 cell	NGjFSItIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NYXldVhwUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6MUe2JO6ddQ>?	Mn3nV2FPT0WU
human HCC2998 cell	MofTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NWjGWldRUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|OESzOkDPxE1?	NYSwS4pHW0GQR1XS
human HEL cell	M{PtOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M4j3[GlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6zPVQ1QSEQvF2=	MU\TRW5ITVJ?
human NMC-G1 cell	M2\hZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NVzxe2RmUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS\|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUC1JO69VQ>?	NUj4RXZ4W0GQR1XS
human 8505C cell	MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3\YbWlvcGmkaYTpc44hd2ZiaIXtZY4hQDVyNVOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ{OTB7IN88US=>	M37aZnNCVkeHUh?=
human HLE cell	Mmj5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHTXO\|hKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOFQ5OTFizszN	NFjMRW1USU6JRWK=
human KGN cell	Mn;tS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NWTEdYRZUW6qaXLpeIlwdiCxZjDoeY1idiCNR16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2OjR7IN88US=>	NXy2T\|A6W0GQR1XS
human EW-18 cell	M3TTeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NU[3PFFZUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDV5OUGg{txO	MX\TRW5ITVJ?
human OCUB-M cell	MojWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NEXrSGlKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDdzNkSg{txO	M3zRVnNCVkeHUh?=
human SW620 cell	NUTi[GRYT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M3zXWGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=>	NHfCSINUSU6JRWK=
human SK-MEL-2 cell	MlHnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{nGOWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR6M{ezJO69VQ>?	MkTMV2FPT0WU
human G-401 cell	MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NHHsSYpKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42ODJ4MTFOwG0>	NH;SXnFUSU6JRWK=
human HT-29 cell	MknlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MkPoTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOVQ3PyEQvF2=	NU\5do01W0GQR1XS
human A427 cell	NXPhRXpIT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVzJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?=	MYTTRW5ITVJ?
human A375 cell	MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NIDuSINKdmirYnn0bY9vKG:oIHj1cYFvKEF\|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=>	Mkj0V2FPT0WU
SNU-449 cell	M2i3VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NUXSXHZPUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFQ6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkK5OEDPxE1?	M1PacXNCVkeHUh?=
human A431 cell	NX65PWNLT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M2XQSmlvcGmkaYTpc44hd2ZiaIXtZY4hSTR\|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOlU2OzZizszN	Mnn5V2FPT0WU
human NCI-H1299 cell	MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NVvETIJPUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFEzQTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[5N\|A5KM7:TR?=	MYnTRW5ITVJ?
human SNU-423 cell	MmGxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MoOwTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0>	NIrpPJRUSU6JRWK=
human SW1710 cell	MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M2TsVGlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjV3IN88US=>	MYnTRW5ITVJ?
human KYSE-450 cell	MoHaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NFHudIxKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtOFUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55Mki4OUDPxE1?	MYnTRW5ITVJ?

... 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]	+ 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% CO_{2(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)

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% CO_{2(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)

References

+ Expand

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 )

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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Chemical Information Download Tipifarnib SDF

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

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Cited by 19 Publications

Purity & Quality Control

Choose Selective Transferase Inhibitors

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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:

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

Tech Support

Transferase Signaling Pathway Map

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