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

Tipifarnib  (Synonyms: IND 58359; R115777)

Cat. No.: HY-10502 Purity: 99.78%
COA Handling Instructions

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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 109 In-stock
Solid
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10 mg USD 176 In-stock
50 mg USD 616 In-stock
100 mg USD 1045 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Tipifarnib:

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  • Biological Activity

  • 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.

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 : 100 mg/mL (204.33 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0433 mL 10.2166 mL 20.4332 mL
5 mM 0.4087 mL 2.0433 mL 4.0866 mL
10 mM 0.2043 mL 1.0217 mL 2.0433 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.43 mg/mL (2.92 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.43 mg/mL (2.92 mM); Suspended solution; Need ultrasonic

  • 4.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.43 mg/mL (2.92 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.89% ee.: 99.18%

References
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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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Tipifarnib
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