L-778123 hydrochloride
Based on 5 publication(s) in Google Scholar
L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC50 values of 2 nM and 98 nM respectively.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 253863-00-2
- Formula: C22H21Cl2N5O
- Molecular Weight:442.34
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) L-778123 hydrochloride
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Biological Activity
L-778123 hydrochloride alone does not have obvious cytotoxicity on HT-29 and A549 cell lines (IC50: >100 μM), but can generate synergistic effects with Doxorubicin (HY-15142A), with the decreased IC50s of 1.72 and 1.52 μM respectively[2].
L-778123 hydrochloride inhibits myeloid leukemia cell proliferation with IC50 values of 0.2 μM-1.8 μM for cell lines, and 0.1 μM-161.8 μM in primary samples[3].
L-778123 (0-1 μM, 12 h; or 5 μM, 6 h) hydrochloride inhibits H-RAS prenylation in HL-60 cells, and inhibits phosphorylated MEK-1/2 level (5 μM, 24 h)[3].
L-778123 (0-100 μM, 72 h) hydrochloride inhibits lymphocyte activation (marker: CD71 or CD25) and function in human PBMCs[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.
Chemical Information
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CAS No. 253863-00-2
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Appearance Solid
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Molecular Weight 442.34
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Formula C22H21Cl2N5O
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Color White to off-white
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SMILES
N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jan 8;189(1):23-33.e16. PMID: 41289993 -
Immunity
2024 May 14;57(5):1056-1070.e5. PMID: 38614091 -
ACS Nano
M-Sec Overexpressed Stem Cells Growing Abundant Tunneling Nanotubes for Diverse Active Transferring. [Abstract]2025 Aug 12;19(31):28644-28659. PMID: 40743507 -
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bioRxiv
2023 Feb 8:2023.02.07.527548. PMID: 36798302
Solvent & Solubility
DMSO : ≥ 25 mg/mL (56.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (56.52 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.25 mg/mL (5.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: ≥ 2.25 mg/mL (5.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: PBS
Solubility: 100 mg/mL (226.07 mM); Suspended solution; Need ultrasonic and adjust pH to 5 with 1M HCl
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (281 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lobell RB, et al. Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther. 2002 Jul;1(9):747-758. [Content Brief]
[2]. Ghasemi S, et al. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines. Adv Pharm Bull. 2013;3(1):73-77. [Content Brief]
[4]. Si MS, et al. Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123. Invest New Drugs. 2005 Jan;23(1):21-9. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.2607 mL | 11.3035 mL | 22.6070 mL | 56.5176 mL |
| 5 mM | 0.4521 mL | 2.2607 mL | 4.5214 mL | 11.3035 mL | |
| 10 mM | 0.2261 mL | 1.1304 mL | 2.2607 mL | 5.6518 mL | |
| 15 mM | 0.1507 mL | 0.7536 mL | 1.5071 mL | 3.7678 mL | |
| 20 mM | 0.1130 mL | 0.5652 mL | 1.1304 mL | 2.8259 mL | |
| 25 mM | 0.0904 mL | 0.4521 mL | 0.9043 mL | 2.2607 mL | |
| 30 mM | 0.0754 mL | 0.3768 mL | 0.7536 mL | 1.8839 mL | |
| 40 mM | 0.0565 mL | 0.2826 mL | 0.5652 mL | 1.4129 mL | |
| 50 mM | 0.0452 mL | 0.2261 mL | 0.4521 mL | 1.1304 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.