Tipifarnib (Synonyms: IND 58359; R115777)

Name: Tipifarnib
Brand: MedChemExpress
SKU: HY-10502
Rating: 5.0 (14 reviews)

Cat. No.: HY-10502 Purity: 99.72%: Data Sheet
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Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC₅₀ of 0.86 nM. Antineoplastic activity and antiparasitic activity.

For research use only. We do not sell to patients.

CAS No. : 192185-72-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Tipifarnib:

14 Publications Citing Use of MCE Tipifarnib

In Vivo Efficacy Study

In Vivo Imaging

RT-PCR

Histological Imaging/Staining

: Tipifarnib purchased from MedChemExpress. Usage Cited in: Circ Res. 2024 Jul 5;135(2):280-297. [Abstract]; Representative image of the western blotting analyses of protein extracted from mouse hearts to study the effect of Tipifarnib (10 mg/kg body weight/three times a week, IP injection) treatment on the expression of proteins involved in exosome biogenesis. GAPDH served as the loading control.

: Tipifarnib purchased from MedChemExpress. Usage Cited in: Circ Res. 2024 Jul 5;135(2):280-297. [Abstract]; Post TAC, heart-to-body weight ratio (HW/BW) and Heart weight (HW) to Tibia length (TL) (gm/cm) ratio at 8 weeks for sham, TAC and TAC+Tipifarnib (10 mg/kg body weight/three times a week, IP injection). Data are expressed as Mean ± SEM. Mean of the different groups was compared using one-way ANOVA followed by Tukey post-tests. with 95% confidence interval.

: Tipifarnib purchased from MedChemExpress. Usage Cited in: Circ Res. 2024 Jul 5;135(2):280-297. [Abstract]; Representative echocardiographic images (M-mode) from sham, TAC and Tipifarnib (10 mg/kg body weight/three times a week, IP injection) treated TAC mouse heart at 8 weeks.

: Tipifarnib purchased from MedChemExpress. Usage Cited in: Circ Res. 2024 Jul 5;135(2):280-297. [Abstract]; Tipifarnib (10 mg/kg body weight/three times a week, IP injection). Representative image of the immunofluorescence of myocardial sections stained with Alexa fluor 488-labeled wheat germ agglutinin (WGA) antibody, defining myocyte boundaries. Scale bar = 50 μm).

: Tipifarnib purchased from MedChemExpress. Usage Cited in: Circ Res. 2024 Jul 5;135(2):280-297. [Abstract]; Tipifarnib (10 mg/kg body weight/three times a week, IP injection). Quantitative Reverse Transcription Polymerase Chain Reaction (qRT PCR) of mice heart tissues for hypertrophy–related genes (ANP, BNP and MYH7) in each experimental group after 8 weeks post-TAC; n=7/group.

: Tipifarnib purchased from MedChemExpress. Usage Cited in: Circ Res. 2024 Jul 5;135(2):280-297. [Abstract]; Representative image for Masson’s trichrome staining in the heart tissues of sham, TAC and Tipifarnib (10 mg/kg body weight/three times a week, IP injection) treated TAC (TAC+Tipifarnib) Scale bar = 50 μm.

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Biological Activity
Purity & Documentation
References
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Description

Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC₅₀ of 0.86 nM. Antineoplastic activity and antiparasitic activity^[1].

IC₅₀ & Target

IC50: 0.86 nM (FTase)

Cellular Effect

Cell Line	Type	Value	Description	References
Capan-2	IC₅₀	16 nM Compound: 59	Antiproliferative activity against human Capan-2 cells harboring KRAS 12 mutation assessed as inhibition of cell growth incubated for 4 to 7 days Antiproliferative activity against human Capan-2 cells harboring KRAS 12 mutation assessed as inhibition of cell growth incubated for 4 to 7 days	[PMID: 33228976]
HCT-116	EC₅₀	24 nM Compound: R115777	Inhibition of anchorage-independent growth in human HCT-116 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% FBS by imaging based soft agar colony formation assay Inhibition of anchorage-independent growth in human HCT-116 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% FBS by imaging based soft agar colony formation assay	[PMID: 16222147]
HT1197	IC₅₀	1.7 nM Compound: 59	Antiproliferative activity against human HT1197 cells harboring HRAS 61 mutation assessed as inhibition of cell growth incubated for 4 to 7 days Antiproliferative activity against human HT1197 cells harboring HRAS 61 mutation assessed as inhibition of cell growth incubated for 4 to 7 days	[PMID: 33228976]
HepG2	CC₅₀	30 μM Compound: Tipifarnib	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by resazurin dye based spectraMax M5 microplate reader analysis Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by resazurin dye based spectraMax M5 microplate reader analysis	[PMID: 39051854]
MCF7	IC₅₀	3.08 μM Compound: R115777	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	10.1039/C3MD00058C
NCI-H441	IC₅₀	36 nM Compound: 59	Antiproliferative activity against human NCI-H441 cells harboring KRAS 12 mutation assessed as inhibition of cell growth incubated for 4 to 7 days Antiproliferative activity against human NCI-H441 cells harboring KRAS 12 mutation assessed as inhibition of cell growth incubated for 4 to 7 days	[PMID: 33228976]
NIH3T3	EC₅₀	0.002 μM Compound: 1, R-115777	Effective concentration against Ha-RAS processing in NIH3T3 ras-transformed cells Effective concentration against Ha-RAS processing in NIH3T3 ras-transformed cells	[PMID: 12657284]
NIH3T3	EC₅₀	1.6 nM Compound: 1	Inhibition of Ras processing in H-ras transformed NIH3T3 cells in presence of Tipifarnib Inhibition of Ras processing in H-ras transformed NIH3T3 cells in presence of Tipifarnib	[PMID: 15911281]
NIH3T3	EC₅₀	1.6 nM Compound: 1 (Tipifarnib)	Inhibition of H-Ras transformed NIH-3T3-cell proliferation Inhibition of H-Ras transformed NIH-3T3-cell proliferation	[PMID: 15454229]
NIH3T3	EC₅₀	1.6 nM Compound: Tipifarnib	Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells	[PMID: 15454228]
NIH3T3	EC₅₀	100 nM Compound: 1	Inhibition of Ras processing in H-ras transformed NIH3T3 cells in presence of Lonafarnib Inhibition of Ras processing in H-ras transformed NIH3T3 cells in presence of Lonafarnib	[PMID: 15911281]
NIH3T3	EC₅₀	3.7 nM Compound: R115777	Inhibition of anchorage-independent growth in H-Ras transformed mouse NIH3T3 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% bovine serum by imaging based soft agar colony formation assay Inhibition of anchorage-independent growth in H-Ras transformed mouse NIH3T3 cells assessed as inhibition of colony formation incubated for 14 days in presence of 10% bovine serum by imaging based soft agar colony formation assay	[PMID: 16222147]
NIH3T3	EC₅₀	4 nM Compound: 1	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells	[PMID: 19875282]
NIH3T3	EC₅₀	4 nM Compound: 1	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 7 days by alamar blue assay Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 7 days by alamar blue assay	[PMID: 20429511]
NIH3T3	IC₅₀	1.7 nM Compound: 1	T24H-ras-transformed NIH3T3 cell proliferation T24H-ras-transformed NIH3T3 cell proliferation	[PMID: 14643327]
NIH3T3	IC₅₀	1.7 nM Compound: 1, R-115777	Inhibition of T24F1H-ras-transformation in NIH 3T3 cells Inhibition of T24F1H-ras-transformation in NIH 3T3 cells	[PMID: 12699751]
NIH3T3	IC₅₀	1.7 nM Compound: R-11577	In vitro inhibition of NIH3T3 cell proliferation In vitro inhibition of NIH3T3 cell proliferation	[PMID: 14643326]
SU.86.86	IC₅₀	9.5 nM Compound: 59	Antiproliferative activity against human SU-86-86 cells harboring KRAS 12 mutation assessed as inhibition of cell growth incubated for 4 to 7 days Antiproliferative activity against human SU-86-86 cells harboring KRAS 12 mutation assessed as inhibition of cell growth incubated for 4 to 7 days	[PMID: 33228976]
Sf9	IC₅₀	0.7 nM Compound: 1	Inhibition of rat recombinant protein farnesyltransferase expressed in Sf9 cells by [3H]-scintillation proximity assay Inhibition of rat recombinant protein farnesyltransferase expressed in Sf9 cells by [3H]-scintillation proximity assay	[PMID: 19239254]
Sf9	IC₅₀	0.7 nM Compound: 1	Inhibition of rat recombinant PFT expressed in insect Sf9 cells by scintillation proximity assay Inhibition of rat recombinant PFT expressed in insect Sf9 cells by scintillation proximity assay	[PMID: 20429511]

In Vitro

Tipifarnib is a potent inhibitor of Trypanosoma Cruzi with the ED₅₀ of 4 nM^[1].
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^[2].
Tipifarnib shows inhibition of cell growth or angiogenesis, and induction of apoptosis in aggressive prostate cancer (PCa)^[3].
Tipifarnib (0.25 μM, 1 μM; 48 h) shows a significant decrease in the concentration of exosomes in C4-2B cells and PC-3 cells^[3].
Tipifarnib (1 μM) significantly inhibits the protein concentration of Alix, nSMase2, and Rab27a in C4-2B cells^[3].
Tipifarnib (0.25 μM) significantly inhibits the activation of p-ERK (downstream effector molecule of the Ras/Raf/ERK signaling pathway) but not total ERK in C4-2B and PC-3 cells^[3].
Tipifarnib (1.25-5 μM; 30 min) promotes endoplasmic reticulum stress in U937 cells, resulting in dysregulation of intracellular calcium homeostasis^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tipifarnib (10 mg/kg; ip; single dose) upregulated antiapoptotic protein, Bcl-xL in liver, and prevents mosue death induced by GalN/LPS^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	GalN/LPS challenge mouse^[5]
Dosage:	10 mg/kg; while chanllenge with GalN (400 mg/kg; IP) and LPS (32 g/kg)
Administration:	IP; 60 min before challenge
Result:	Protected primary hepatocytes from GalN/tumor necrosis factor-induced cell death. Inhibited caspase 3 activation and upregulating antiapoptotic proteins.

Clinical Trial

Molecular Weight

489.40

Formula

C₂₇H₂₂Cl₂N₄O

CAS No.

192185-72-1

Appearance

Solid

Color

White to light yellow

SMILES

O=C1N(C2=C(C(C3=CC=CC(Cl)=C3)=C1)C=C(C=C2)[C@@](N)(C4=CN=CN4C)C5=CC=C(C=C5)Cl)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (68.10 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0433 mL	10.2167 mL	20.4334 mL
5 mM	0.4087 mL	2.0433 mL	4.0867 mL
10 mM	0.2043 mL	1.0217 mL	2.0433 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 20% HP-β-CD/10 mM Citrate pH 2.0
Solubility: 10 mg/mL (20.43 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.89% ee.: 99.18%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (254 KB) HNMR (174 KB) NP-HPLC (714 KB) LCMS (429 KB) Elemental Analysis Report (112 KB)

Handling Instructions (2659 KB)

References

[1]. Devendra S Puntambekar, et al. Inhibition of farnesyltransferase: a rational approach to treat cancer? J Enzyme Inhib Med Chem. 2007 Apr;22(2):127-40. [Content Brief]

[2]. End DW, et al. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 2001 Jan 1;61(1):131-7 [Content Brief]

[3]. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0433 mL	10.2167 mL	20.4334 mL	51.0834 mL
	5 mM	0.4087 mL	2.0433 mL	4.0867 mL	10.2167 mL
	10 mM	0.2043 mL	1.0217 mL	2.0433 mL	5.1083 mL
	15 mM	0.1362 mL	0.6811 mL	1.3622 mL	3.4056 mL
	20 mM	0.1022 mL	0.5108 mL	1.0217 mL	2.5542 mL
	25 mM	0.0817 mL	0.4087 mL	0.8173 mL	2.0433 mL
	30 mM	0.0681 mL	0.3406 mL	0.6811 mL	1.7028 mL
	40 mM	0.0511 mL	0.2554 mL	0.5108 mL	1.2771 mL
	50 mM	0.0409 mL	0.2043 mL	0.4087 mL	1.0217 mL
	60 mM	0.0341 mL	0.1703 mL	0.3406 mL	0.8514 mL

Tipifarnib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tipifarnib192185-72-1IND 58359 R115777IND58359IND-58359R115777R 115777R-115777Farnesyl TransferaseFtaseInhibitorinhibitorinhibit

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Tipifarnib (Synonyms: IND 58359; R115777)

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Tipifarnib Related Antibodies

14 Publications Citing Use of MCE Tipifarnib

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Tipifarnib Related Antibodies

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Complete Stock Solution Preparation Table

Tipifarnib Related Classifications

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