L-778123
Based on 6 publication(s) in Google Scholar
L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 183499-57-2
- Formula: C22H20ClN5O
- Molecular Weight:405.88
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) L-778123
More
Customer Validation & Images
-
IF
-
WB
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.72 μM
Compound: 51; L-788,123
|
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
|
[PMID: 33228976] |
| A549 | IC50 |
100.72 μM
Compound: 51; L-788,123
|
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay
|
[PMID: 33228976] |
| Cancer cell lines | IC50 |
2280 nM
Compound: 51; L-788,123
|
Antiproliferative activity against human cancer cell lines harboring KRAS mutation assessed as reduction in cell viability
Antiproliferative activity against human cancer cell lines harboring KRAS mutation assessed as reduction in cell viability
|
[PMID: 33228976] |
| Cancer cell lines | IC50 |
70 nM
Compound: 51; L-788,123
|
Antiproliferative activity against human cancer cell lines harboring wild type RAS mutation assessed as reduction in cell viability
Antiproliferative activity against human cancer cell lines harboring wild type RAS mutation assessed as reduction in cell viability
|
[PMID: 33228976] |
| HT-29 | IC50 |
1.52 μM
Compound: 51; L-788,123
|
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
|
[PMID: 33228976] |
| HT-29 | IC50 |
125.78 μM
Compound: 51; L-788,123
|
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay
|
[PMID: 33228976] |
| PSN1 | EC50 |
6300 nM
Compound: 1
|
Effective dose required for half-maximal inhibition of prenylation in PSN-1 cells (Ki-Ras)
Effective dose required for half-maximal inhibition of prenylation in PSN-1 cells (Ki-Ras)
|
[PMID: 14741259] |
| PSN1 | EC50 |
6760 nM
Compound: 1
|
Effective dose required for half-maximal inhibition of geranylgeranylated protein (Rap1a) in PSN-1 cells
Effective dose required for half-maximal inhibition of geranylgeranylated protein (Rap1a) in PSN-1 cells
|
[PMID: 14741259] |
| PSN1 | EC50 |
92 nM
Compound: 1
|
Effective dose required for half-maximal inhibition of farnesylated protein (HDJ2) in PSN-1 cells
Effective dose required for half-maximal inhibition of farnesylated protein (HDJ2) in PSN-1 cells
|
[PMID: 14741259] |
| Rat1 | IC50 |
3 nM
Compound: 1
|
Concentration required to displace 50% of a radiolabeled farnesyltransferase inhibitor from FPTase in cultured Ha-Ras transformed RAT1 cells
Concentration required to displace 50% of a radiolabeled farnesyltransferase inhibitor from FPTase in cultured Ha-Ras transformed RAT1 cells
|
[PMID: 11378366] |
| Rat1 | IC50 |
3.6 nM
Compound: 1
|
Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.
Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.
|
[PMID: 14741259] |
| Rat1 | IC50 |
95 nM
Compound: 1
|
Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat1 cells.
Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat1 cells.
|
[PMID: 11965368] |
L-778123 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 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) 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) 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
-
CAS No. 183499-57-2
-
Appearance Solid
-
Molecular Weight 405.88
-
Formula C22H20ClN5O
-
Color White to off-white
-
SMILES
N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
-
Journal Impact Factor
-
Most Recent
-
Cell
2026 Jan 8;189(1):23-33.e16. PMID: 41289993 -
Immunity
2024 May 14;57(5):1056-1070.e5. PMID: 38614091
L-778123 purchased from MedChemExpress. Usage Cited in: Immunity. 2024 May 14;57(5):1056-1070.e5. [Abstract]
Confocal images of CFSE-labeled iIEMCs and CMT-93 cells cocultured in the presence of DMSO or 10 μM L-778123 and after 24 h, immunolabeled with DAPI, E-cadherin, and Mcpt1.
-
Nat Commun
HMGCS1 drives cholesterol-dependent membrane repair and shields tumor cells from lymphocyte attack. [Abstract]2026 Jun 5. PMID: 42248910 -
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 -
-
bioRxiv
2023 Feb 8:2023.02.07.527548. PMID: 36798302
L-778123 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 8:2023.02.07.527548. [Abstract]
Western blot detection of specific protein markers in samples after tandem enrichment. GW4869 and L778123 (10 μM 12 h) are small-molecule inhibitors of exosome biogenesis and tunneling nanotube formation, respectively.
Solvent & Solubility
1 M HCl : ≥ 100 mg/mL (246.38 mM)
DMSO : 20 mg/mL (49.28 mM; ultrasonic and adjust pH to 2 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Data Sheet (280 KB)
-
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)
-
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. 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 / 1 M HCl | 1 mM | 2.4638 mL | 12.3189 mL | 24.6378 mL | 61.5946 mL |
| 5 mM | 0.4928 mL | 2.4638 mL | 4.9276 mL | 12.3189 mL | |
| 10 mM | 0.2464 mL | 1.2319 mL | 2.4638 mL | 6.1595 mL | |
| 15 mM | 0.1643 mL | 0.8213 mL | 1.6425 mL | 4.1063 mL | |
| 20 mM | 0.1232 mL | 0.6159 mL | 1.2319 mL | 3.0797 mL | |
| 25 mM | 0.0986 mL | 0.4928 mL | 0.9855 mL | 2.4638 mL | |
| 30 mM | 0.0821 mL | 0.4106 mL | 0.8213 mL | 2.0532 mL | |
| 40 mM | 0.0616 mL | 0.3080 mL | 0.6159 mL | 1.5399 mL | |
| 1 M HCl | 50 mM | 0.0493 mL | 0.2464 mL | 0.4928 mL | 1.2319 mL |
| 60 mM | 0.0411 mL | 0.2053 mL | 0.4106 mL | 1.0266 mL | |
| 80 mM | 0.0308 mL | 0.1540 mL | 0.3080 mL | 0.7699 mL | |
| 100 mM | 0.0246 mL | 0.1232 mL | 0.2464 mL | 0.6159 mL |
L-778123 Related Classifications
HY-16273 Related Classifications
Powered by Bioz