2. Metabolic Enzyme/Protease
  3. Farnesyl Transferase
  4. Tipifarnib

Tipifarnib  (Synonyms: IND 58359; R115777)

Cat. No.: HY-10502 Purity: 99.78%
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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.

Tipifarnib Chemical Structure

Tipifarnib Chemical Structure

CAS No. : 192185-72-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 109 In-stock
Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 99 In-stock
10 mg USD 176 In-stock
25 mg USD 337 In-stock
50 mg USD 540 In-stock
100 mg USD 864 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Tipifarnib:

Tipifarnib Related Antibodies

Top Publications Citing Use of Products

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  • Purity & Documentation

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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)
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.

Tipifarnib Related Antibodies
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.
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
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.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

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)

g

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%

COA (255 KB) HNMR (174 KB) NP-HPLC (714 KB) LCMS (429 KB) Elemental Analysis Report (112 KB)

Handling Instructions (2659 KB)
References

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.

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
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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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