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 22 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 )

NPJ Aging Mech Dis, 2016, 2:16026

PubMed: 28721276 ( 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	Mn63SpVv[3Srb36gZZN{[Xl?	MV\Jcohq[mm2aX;uJI9nKHKjdDDy[YNwdWKrbnHueEBRTlRiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC55IH7N	NIjMdGczODR{OUWxNS=>
NIH3T3 cells	NH3MPXVHfW6ldHnvckBie3OjeR?=	NV3WPVZrUW6qaXLpeIlwdiCxZjDSZZMheHKxY3Xzd4lv\yCrbjDIMZJieyC2cnHud4Zwem2nZDDOTWg{XDNiY3XscJMhcW5icILld4Vv[2Vib3[gWIlxcW[jcn7pZkwhTUN3ME2xMlYhdk1?	MmHjNVU6OTF{OEG=
human RPMI-6666 cell	MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3PjZ2lvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py52MTDuUS=>	M{DvZnNCVkeHUh?=
human ML-2 cell	M{C0[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NX7aTJJ6UW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvPjRibl2=	MoHDV2FPT0WU
human SIG-M5 cell	M2TQSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NUjhNYVCUW6qaXLpeIlwdiCxZjDoeY1idiCVSVetUVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53NzDuUS=>	NWS0NWtQW0GQR1XS
human QIMR-WIL cell	NEixNplIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MkT6TY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjNzIH7N	MnjoV2FPT0WU
human A4-Fuk cell	NWTs[mx3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVLJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUKwMlU6KG6P	MVvTRW5ITVJ?
human ETK-1 cell	NGXwdmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MWDJcohq[mm2aX;uJI9nKGi3bXHuJGVVUy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MkGuOVIhdk1?	M3vM[XNCVkeHUh?=
human MEL-JUSO cell	NUnGc4hCT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M4ewOGlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVrVV28h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOy52NDDuUS=>	M{DHeHNCVkeHUh?=
human NALM-6 cell	NGjURmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M4njcGlvcGmkaYTpc44hd2ZiaIXtZY4hVkGOTT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N\|YvOjFibl2=	M3XnOHNCVkeHUh?=
human IA-LM cell	MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1THTWlvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20O{42OiCwTR?=	Mn3EV2FPT0WU
human Daoy cell	Mn7vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{CyZ2lvcGmkaYTpc44hd2ZiaIXtZY4hTGGxeTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUW3MlU{KG6P	NEjKT29USU6JRWK=
human REH cell	MonBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M3PRZWlvcGmkaYTpc44hd2ZiaIXtZY4hWkWKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NUmuNkBvVQ>?	NH;GOpJUSU6JRWK=
human KU812 cell	M1TkVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	Mm\pTY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUm3MlA3KG6P	MYrTRW5ITVJ?
human KM12 cell	M1LNU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NIT3VHlKdmirYnn0bY9vKG:oIHj1cYFvKEuPMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyPjh4IN88US=>	MlfJV2FPT0WU
human LCLC-103H cell	Ml\KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvMUCzTEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ7MEKg{txO	NWfx[2VpW0GQR1XS
human BC-1 cell	NHvIS2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3;DeGlvcGmkaYTpc44hd2ZiaIXtZY4hSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNVI6QTZizszN	NXXXV5VlW0GQR1XS
human CMK cell	NVG2UW9ET3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVzJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwMUWxOFUh\|ryP	NW\iXI81W0GQR1XS
human MCF7 cell	MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NH[3eIVKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE3PjNizszN	M2[zNHNCVkeHUh?=
human Calu-1 cell	NWnzV2k5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M4C1ZmlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDF\|NDFOwG0>	M2Wwb3NCVkeHUh?=
human SK-LMS-1 cell	NEfpfIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MYXJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yQDRyOTFOwG0>	MUXTRW5ITVJ?
human HH cell	NWPkSlFNT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVTJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zOUC4PUDPxE1?	M3XiSXNCVkeHUh?=
human NCI-H2122 cell	M2DQdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NXzOcXpzUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG5NVQ2KM7:TR?=	NYHlW44{W0GQR1XS
human SNG-M cell	NHvHXpRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NVLhTYw4UW6qaXLpeIlwdiCxZjDoeY1idiCVTletUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB\|NUSg{txO	NX3yRZQzW0GQR1XS
human IGROV-1 cell	NYXEW41MT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NGSyO4RKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJyOEKzJO69VQ>?	NFPKUJdUSU6JRWK=
human KYSE-270 cell	NYH4WZZpT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NWT6RZZvUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVI4OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwMkG2Olgh\|ryP	NUfUXoM6W0GQR1XS
human NTERA-S-cl-D1 cell	NFj5NYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NVq2UHk5UW6qaXLpeIlwdiCxZjDoeY1idiCQVFXSRU1UNWOuLVSxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOzd2IN88US=>	M1Wzc3NCVkeHUh?=
human LoVo cell	MoPXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MoHpTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6yOFA6OSEQvF2=	M4KzOnNCVkeHUh?=
human MOLT-16 cell	MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3m2VGlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjV6MkOg{txO	M3ftcXNCVkeHUh?=
human P30-OHK cell	NVezPFJGT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHA{OC2RSFugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI3Ozh6IN88US=>	M174XXNCVkeHUh?=
human HUTU-80 cell	MlHHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MYTJcohq[mm2aX;uJI9nKGi3bXHuJGhWXFVvOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI5PTB{IN88US=>	M4n6XnNCVkeHUh?=
human MIA-PaCa-2 cell	NGj3NFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	Mk\oTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|MkC0JO69VQ>?	NWK3cXRJW0GQR1XS
human HCC2157 cell	NVrBcJJTT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M37xeWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkG1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJ\|MU[g{txO	M4\Gc3NCVkeHUh?=
human HCT-15 cell	Mn6yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MoT6TY5pcWKrdHnvckBw\iCqdX3hckBJS1RvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzPzB3IN88US=>	NVTGS4tlW0GQR1XS
human 786-0 cell	M{[wVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M1nSd2lvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd\|IN88US=>	MlrSV2FPT0WU
human GDM-1 cell	NUW5fo5ZT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M1LnT2lvcGmkaYTpc44hd2ZiaIXtZY4hT0SPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2OjN7IN88US=>	NHm0[oVUSU6JRWK=
human NCI-H2009 cell	Mk\KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M2TDfmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|NkOzOkDPxE1?	MWLTRW5ITVJ?
human TE-15 cell	NWDNWmhvT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MkHaTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuN\|Y1PjJizszN	M4XxSHNCVkeHUh?=
human NCI-H2342 cell	MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M4P6fWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN\|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|N{m4N{DPxE1?	MVzTRW5ITVJ?
human RT-112 cell	MlfQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NVHyUIo1UW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6MUe2JO6ddQ>?	MYjTRW5ITVJ?
human HCC2998 cell	NIXZfZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MlrJTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QDR\|NjFOwG0>	NFXwZ\|ZUSU6JRWK=
human HEL cell	MmXOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MYLJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwM{m0OFkh\|ryP	MonQV2FPT0WU
human NMC-G1 cell	Moq5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M1nITGlvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjVyNTFOwG0>	M1G4PHNCVkeHUh?=
human 8505C cell	M2PuU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NVzvOmV[UW6qaXLpeIlwdiCxZjDoeY1idiB6NUC1R{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDNzMEmg{txO	MXPTRW5ITVJ?
human HLE cell	MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MWTJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwNES4NVEh\|ryP	NFzlRnZUSU6JRWK=
human KGN cell	MnTlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHnPcGRKdmirYnn0bY9vKG:oIHj1cYFvKEuJTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOFUzPDlizszN	NWPoe\|cyW0GQR1XS
human EW-18 cell	NV;tTFFKT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NHfLRW1KdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PTd7MTFOwG0>	NWiyR457W0GQR1XS
human OCUB-M cell	NU\yeHBQT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	Mk\XTY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4OTZ2IN88US=>	MX7TRW5ITVJ?
human SW620 cell	Mon5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M1nMe2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ5OjJ2IN88US=>	NYXGfVF[W0GQR1XS
human SK-MEL-2 cell	Mn;1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDN5MzFOwG0>	NHzPNotUSU6JRWK=
human G-401 cell	M3nMXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MVfJcohq[mm2aX;uJI9nKGi3bXHuJGcuPDBzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD61NFI3OSEQvF2=	MkPJV2FPT0WU
human HT-29 cell	M4rqV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M3fPWWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU1PjdizszN	NUPkW3U5W0GQR1XS
human A427 cell	NYL6PJhLT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVHJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW3PVE4KM7:TR?=	MmjMV2FPT0WU
human A375 cell	MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MlPCTY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD62NVY1QCEQvF2=	MlrIV2FPT0WU
SNU-449 cell	MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MX7Jcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYzOjl2IN88US=>	M1;uS3NCVkeHUh?=
human A431 cell	MnToS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NGHBUnlKdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY2PTN4IN88US=>	M1TxfXNCVkeHUh?=
human NCI-H1299 cell	NIfWVldIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MkmzTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGyPVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ7M{C4JO69VQ>?	MVfTRW5ITVJ?
human SNU-423 cell	MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MljhTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44ODR4NjFOwG0>	Moe5V2FPT0WU
human SW1710 cell	NH32ZoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NEnBT\|JKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ3NTFOwG0>	MYXTRW5ITVJ?
human KYSE-450 cell	NGDqTXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NV;rVWFWUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwN{K4PFUh\|ryP	NILoVpJUSU6JRWK=

... 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]

- 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)

References

- Collapse

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

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Choose Your Country or Region

By Signaling Pathways

By product type

Tipifarnib

Cited by 22 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

Choose Your Country or Region

By Signaling Pathways

By product type

Tipifarnib

Cited by 22 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)