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	NWTaPW5PTnWwY4Tpc44h[XO\|YYm=	NIe4WYxKdmirYnn0bY9vKG:oIILheEBz\WOxbXLpcoFvfCCSRmSg[ZhxemW\|c3XkJIlvKGmwc3XjeEBU\jliY3XscJMh[nlic3PpcpRqdGyjdHnvckBxem:6aX3peJkh[XO\|YYmsJGlEPTB;MD63JI5O	M3\hflIxPDJ7NUGx
NIH3T3 cells	M1PNfmZ2dmO2aX;uJIF{e2G7	MoPZTY5pcWKrdHnvckBw\iCUYYOgdJJw[2W\|c3nu[{BqdiCKLYLhd{B1emGwc3\vdo1m\CCQSVizWFMh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiVHnwbYZiem6rYjygSWM2OD1zLk[gcm0>	MlzJNVU6OTF{OEG=
human RPMI-6666 cell	Mo[5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4LO[mlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=>	MXTTRW5ITVJ?
human ML-2 cell	M3j5fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MWTJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz62OEBvVQ>?	MnHRV2FPT0WU
human SIG-M5 cell	M4Tmemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNKTy2PNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUG0MlU4KG6P	NIL3RVhUSU6JRWK=
human QIMR-WIL cell	NXvFRmV[T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NVLIUmVZUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTF4LkOxJI5O	MoLnV2FPT0WU
human A4-Fuk cell	NXLEbZRwT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M{fuO2lvcGmkaYTpc44hd2ZiaIXtZY4hSTRvRoXrJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlAvPTlibl2=	MVjTRW5ITVJ?
human ETK-1 cell	NF7xdmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NXHlb3I6UW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV{IH7N	M363[XNCVkeHUh?=
human MEL-JUSO cell	MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MorqTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSmXTU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjR2IH7N	NH73V2xUSU6JRWK=
human NALM-6 cell	NXvSNlVST3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MoW1TY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk4zOSCwTR?=	MUXTRW5ITVJ?
human IA-LM cell	NFjuN49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NXPuXlBUUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjV{IH7N	NXH5NIdUW0GQR1XS
human Daoy cell	NYHoTlBzT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MlzOTY5pcWKrdHnvckBw\iCqdX3hckBF[W:7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NUeuOVMhdk1?	MWrTRW5ITVJ?
human REH cell	NX60V5JmT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MkLDTY5pcWKrdHnvckBw\iCqdX3hckBTTUhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT6yJI5O	NYjVV4RrW0GQR1XS
human KU812 cell	MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NEHZUXlKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVcvODZibl2=	MW\TRW5ITVJ?
human KM12 cell	MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NXLzSZh1UW6qaXLpeIlwdiCxZjDoeY1idiCNTUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTZ6NjFOwG0>	M2DoeXNCVkeHUh?=
human LCLC-103H cell	M1f2fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NUPudXc6UW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVExO0hiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyPVAzKM7:TR?=	M{jqOnNCVkeHUh?=
human BC-1 cell	Mne5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHfDZYdKdmirYnn0bY9vKG:oIHj1cYFvKEKFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEzQTl4IN88US=>	MWrTRW5ITVJ?
human CMK cell	MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NUDGRpl2UW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2OTR3IN88US=>	M1L0OnNCVkeHUh?=
human MCF7 cell	MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	Ml31TY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6xOlY{KM7:TR?=	NGC1fXBUSU6JRWK=
human Calu-1 cell	NVXtV3FIT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NG\adoFKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOThzM{Sg{txO	NHjwUZpUSU6JRWK=
human SK-LMS-1 cell	M36xXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NIHvOoZKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOESwPUDPxE1?	MWTTRW5ITVJ?
human HH cell	MojPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4PTcmlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NFg6KM7:TR?=	MnvIV2FPT0WU
human NCI-H2122 cell	NFHqTXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NWnVdHk2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?=	MVLTRW5ITVJ?
human SNG-M cell	MoruS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M3W5fWlvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxOzV2IN88US=>	MXXTRW5ITVJ?
human IGROV-1 cell	MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NWGwUIo5UW6qaXLpeIlwdiCxZjDoeY1idiCLR2LPWk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MEiyN{DPxE1?	NIjWO3FUSU6JRWK=
human KYSE-270 cell	NInpUlJIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NH7UO4VKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[2PEDPxE1?	NF\DS5NUSU6JRWK=
human NTERA-S-cl-D1 cell	NF3JPW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M1fPOWlvcGmkaYTpc44hd2ZiaIXtZY4hVlSHUlGtV{1kdC2GMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNlM4PCEQvF2=	MlW1V2FPT0WU
human LoVo cell	MofnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M3HIdmlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNlQxQTFizszN	NGDnXo5USU6JRWK=
human MOLT-16 cell	M13WN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NFT0ZZNKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ3OEKzJO69VQ>?	MYnTRW5ITVJ?
human P30-OHK cell	NHnYdXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MlXpTY5pcWKrdHnvckBw\iCqdX3hckBROzBvT1jLJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPjN6ODFOwG0>	MVHTRW5ITVJ?
human HUTU-80 cell	M1zWOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	Ml\XTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zQDVyMjFOwG0>	MnrKV2FPT0WU
human MIA-PaCa-2 cell	NF7ld5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NH;NXmRKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkOyNFQh\|ryP	Ml7jV2FPT0WU
human HCC2157 cell	NEX1dFRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3\1UmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkG1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ\|MU[g{txO	MWnTRW5ITVJ?
human HCT-15 cell	NHjJRZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NVnSTpN[UW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN{N{C1JO69VQ>?	NV[zc3F7W0GQR1XS
human 786-0 cell	MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MoHiTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuN\|IyPzNizszN	MV3TRW5ITVJ?
human GDM-1 cell	NX24WZFiT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6zOVI{QSEQvF2=	M2XPcXNCVkeHUh?=
human NCI-H2009 cell	MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MUjJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ\|M{[g{txO	M1WzRnNCVkeHUh?=
human TE-15 cell	MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NVrrR5BxUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzZ2NkKg{txO	NXPsW2EzW0GQR1XS
human NCI-H2342 cell	NVHTN4NOT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M33MfGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN\|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|N{m4N{DPxE1?	MkHyV2FPT0WU
human RT-112 cell	M4PBfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NH;ZVHZKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzhzN{[g{rxu	NHmybHRUSU6JRWK=
human HCC2998 cell	Mn7KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MYnJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM5PDN4IN88US=>	NWnhem5ZW0GQR1XS
human HEL cell	M1yyeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M4m1[mlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6zPVQ1QSEQvF2=	MWfTRW5ITVJ?
human NMC-G1 cell	MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MoT3TY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQzPTB3IN88US=>	M2LIVHNCVkeHUh?=
human 8505C cell	M1v3OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NESzbVZKdmirYnn0bY9vKG:oIHj1cYFvKDh3MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OzFyOTFOwG0>	NF:ydphUSU6JRWK=
human HLE cell	NV3oWXNLT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MmnTTY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFEyKM7:TR?=	NWH4bYZkW0GQR1XS
human KGN cell	NF:yTZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3\FZmlvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD60OVI1QSEQvF2=	MlHPV2FPT0WU
human EW-18 cell	MmnYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{P6RWlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ2PzlzIN88US=>	NVrVWYw3W0GQR1XS
human OCUB-M cell	NVzxPIEyT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NIfsU5lKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDdzNkSg{txO	MorjV2FPT0WU
human SW620 cell	Mlm2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{iyN2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=>	Ml3WV2FPT0WU
human SK-MEL-2 cell	M4L4Omdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NFTKdm9KdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OEO3N{DPxE1?	M4fNW3NCVkeHUh?=
human G-401 cell	MoT6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4Dm[mlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUxOjZzIN88US=>	M1\6[XNCVkeHUh?=
human HT-29 cell	Mnz1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4PoWWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU1PjdizszN	NFS1WFlUSU6JRWK=
human A427 cell	MnnjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MXvJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?=	NHPiZYRUSU6JRWK=
human A375 cell	MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NHT2NY1KdmirYnn0bY9vKG:oIHj1cYFvKEF\|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYyPjR6IN88US=>	MmnhV2FPT0WU
SNU-449 cell	NUHifJROT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M37ZOGlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUS0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjJ{OUSg{txO	M4[1[nNCVkeHUh?=
human A431 cell	NXnpU3BwT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M37nW2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR\|MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOlU2OzZizszN	NHn6RmRUSU6JRWK=
human NCI-H1299 cell	NYjnUJQ3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NW\Mem0zUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFEzQTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[5N\|A5KM7:TR?=	MXTTRW5ITVJ?
human SNU-423 cell	MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MnO5TY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0>	NF63ZVdUSU6JRWK=
human SW1710 cell	MnPmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NVO5bohlUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd{NUWg{txO	MY\TRW5ITVJ?
human KYSE-450 cell	M3TVb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MnPJTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ6OEWg{txO	NXznZoNqW0GQR1XS

... 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)