Tipifarnib
Based on 14 publication(s) in Google Scholar
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.
- Purity: 99.72%
- CAS No.: 192185-72-1
- Formula: C27H22Cl2N4O
- Molecular Weight:489.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Tipifarnib
More- Cancer Res. 2026 Feb 9. [Abstract]
- Circ Res. 2024 Jul 5;135(2):280-297. [Abstract]
- Mol Cell. 2021 Oct 7;81(19):4076-4090.e8. [Abstract]
- Mol Cell. 2021 Jul 1;81(13):2736-2751.e8. [Abstract]
- J Clin Invest. 2025 Jul 15;135(14):e189048. [Abstract]
- J Immunother Cancer. 2022 Apr;10(4):e004399. [Abstract]
- Br J Cancer. 2024 Apr;130(6):1059-1072. [Abstract]
- Plant Cell Environ. 2023 Jan;46(1):288-305. [Abstract]
- Biochem Pharmacol. 2025 Sep:239:117019. [Abstract]
- Mol Plant Pathol. 2019 Sep;20(9):1264-1278. [Abstract]
- iScience. 2025 Jan 21;28(2):111864. [Abstract]
- Mol Biol Rep. 2025 Jan 15;52(1):124. [Abstract]
- Extracell Vesicle. 2025 Jun.
- Patent. US20180263995A1.
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WB
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In Vivo Efficacy Study
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In Vivo Imaging
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IF
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RT-PCR
Biological Activity
IC50: 0.86 nM (FTase)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Capan-2 | IC50 |
16 nM
Compound: 59
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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
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[PMID: 33228976] |
| HCT-116 | EC50 |
24 nM
Compound: R115777
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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
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[PMID: 16222147] |
| HepG2 | CC50 |
30 μM
Compound: Tipifarnib
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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
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[PMID: 39051854] |
| HT1197 | IC50 |
1.7 nM
Compound: 59
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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
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[PMID: 33228976] |
| MCF7 | IC50 |
3.08 μM
Compound: R115777
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Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
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10.1039/C3MD00058C |
| NCI-H441 | IC50 |
36 nM
Compound: 59
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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
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[PMID: 33228976] |
| NIH3T3 | EC50 |
0.002 μM
Compound: 1, R-115777
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Effective concentration against Ha-RAS processing in NIH3T3 ras-transformed cells
Effective concentration against Ha-RAS processing in NIH3T3 ras-transformed cells
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[PMID: 12657284] |
| NIH3T3 | EC50 |
1.6 nM
Compound: 1
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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
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[PMID: 15911281] |
| NIH3T3 | EC50 |
1.6 nM
Compound: 1 (Tipifarnib)
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Inhibition of H-Ras transformed NIH-3T3-cell proliferation
Inhibition of H-Ras transformed NIH-3T3-cell proliferation
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[PMID: 15454229] |
| NIH3T3 | EC50 |
1.6 nM
Compound: Tipifarnib
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Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells
Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells
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[PMID: 15454228] |
| NIH3T3 | EC50 |
100 nM
Compound: 1
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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
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[PMID: 15911281] |
| NIH3T3 | EC50 |
3.7 nM
Compound: R115777
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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
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[PMID: 16222147] |
| NIH3T3 | EC50 |
4 nM
Compound: 1
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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
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[PMID: 20429511] |
| NIH3T3 | EC50 |
4 nM
Compound: 1
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Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells
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[PMID: 19875282] |
| NIH3T3 | IC50 |
1.7 nM
Compound: 1
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T24H-ras-transformed NIH3T3 cell proliferation
T24H-ras-transformed NIH3T3 cell proliferation
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[PMID: 14643327] |
| NIH3T3 | IC50 |
1.7 nM
Compound: 1, R-115777
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Inhibition of T24F1H-ras-transformation in NIH 3T3 cells
Inhibition of T24F1H-ras-transformation in NIH 3T3 cells
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[PMID: 12699751] |
| NIH3T3 | IC50 |
1.7 nM
Compound: R-11577
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In vitro inhibition of NIH3T3 cell proliferation
In vitro inhibition of NIH3T3 cell proliferation
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[PMID: 14643326] |
| Sf9 | IC50 |
0.7 nM
Compound: 1
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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
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[PMID: 19239254] |
| Sf9 | IC50 |
0.7 nM
Compound: 1
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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
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[PMID: 20429511] |
| SU.86.86 | IC50 |
9.5 nM
Compound: 59
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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
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[PMID: 33228976] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GalN/LPS challenge mouse[5]
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Dosage:10 mg/kg; while chanllenge with GalN (400 mg/kg; IP) and LPS (32 g/kg)
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Administration:IP; 60 min before challenge
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Result:Protected primary hepatocytes from GalN/tumor necrosis factor-induced cell death.
Inhibited caspase 3 activation and upregulating antiapoptotic proteins.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 192185-72-1
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Appearance Solid
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Molecular Weight 489.40
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Formula C27H22Cl2N4O
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Color White to light yellow
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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
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Synonyms
IND 58359; R115777
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (14)
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Journal Impact Factor
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Most Recent
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Cancer Res
The Farnesyl Transferase Inhibitor Darlifarnib (KO-2806) Resensitizes Relapsing Tumors to RAS Inhibition. [Abstract]2026 Feb 9. PMID: 41661652 -
Circ Res
2024 Jul 5;135(2):280-297. PMID: 38847080
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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Mol Cell
A proteomic and phosphoproteomic landscape of KRAS mutant cancers identifies combination therapies. [Abstract]2021 Oct 7;81(19):4076-4090.e8. PMID: 34375582 -
Mol Cell
The ZMYND8-regulated mevalonate pathway endows YAP-high intestinal cancer with metabolic vulnerability. [Abstract]2021 Jul 1;81(13):2736-2751.e8. PMID: 33932349 -
J Clin Invest
Cancer-associated SPOP mutations enlarge nuclear size and facilitate nuclear envelope rupture upon farnesyltransferase inhibitor treatment. [Abstract]2025 Jul 15;135(14):e189048. PMID: 40662365 -
J Immunother Cancer
Small extracellular vesicles induce resistance to anti-GD2 immunotherapy unveiling tipifarnib as an adjunct to neuroblastoma immunotherapy. [Abstract]2022 Apr;10(4):e004399. PMID: 35483745 -
Br J Cancer
Farnesyl-transferase inhibitors show synergistic anticancer effects in combination with novel KRAS-G12C inhibitors. [Abstract]2024 Apr;130(6):1059-1072. PMID: 38278976 -
Plant Cell Environ
Isoprenylation modification is required for HIPP1-mediated powdery mildew resistance in wheat. [Abstract]2023 Jan;46(1):288-305. PMID: 36319595 -
Biochem Pharmacol
An updated review on the inhibition of exosome biogenesis, release, and uptake: a potential anticancer approach. [Abstract]2025 Sep:239:117019. PMID: 40499840 -
Mol Plant Pathol
The farnesyltransferase β-subunit RAM1 regulates localization of RAS proteins and appressorium-mediated infection in Magnaporthe oryzae. [Abstract]2019 Sep;20(9):1264-1278. PMID: 31250536 -
iScience
Functional-proteomics-based investigation of the cellular response to farnesyltransferase inhibition in lung cancer. [Abstract]2025 Jan 21;28(2):111864. PMID: 39995872 -
Mol Biol Rep
Role of Acorus calamus extract in reducing exosome secretion by targeting Rab27a and nSMase2: a therapeutic approach for breast cancer. [Abstract]2025 Jan 15;52(1):124. PMID: 39812915 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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
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 |