limertinib
Based on 2 publication(s) in Google Scholar
limertinib (ASK120067) is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.12%
- No. CAS: 1934259-00-3
- Fòrmula: C29H32ClN7O2
- Peso molecular:546.06
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) limertinib
MoreVer todos los productos específicos de isoformas EGFR
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Actividad biológica
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EGFRT790M 0.5 nM (IC50) |
EGFRL858R/T790M 0.3 nM (IC50) |
EGFR (WT) 6 nM (IC50) |
EGFRExon 19 deletion 0.5 nM (IC50) |
In the in vitro kinase assay limertinib potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of limertinib against wild-type EGFR (EGFRWT) is 6 nM[1]. limertinib selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM[1]. limertinib (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFRL858R/T790M) even at low dosage (0.1-1 nM). Additionally, limertinib inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM[1].
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:BALB/cA nude mice[1]
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Dosage:5-20 mg/kg
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Administration:Oral gavage; 5-20 mg/kg; once daily; 21 days
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Result:Were well tolerated in animals without observed body weight lossDemonstrated profound and selective antitumor efficacy and decreased TGI rate.Significantly inhibited the phosphorylation of EGFR L858R/T790M and AKT in tumor tissue.
Chemical Information
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No. CAS 1934259-00-3
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Appearance Solid
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Peso molecular 546.06
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Fòrmula C29H32ClN7O2
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Color White to yellow
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SMILES
O=C(NC1=CC(NC2=NC=C(C(NC3=CC4=C(C=CC=C4)C=C3)=N2)Cl)=C(C=C1N(CCN(C)C)C)OC)C=C
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Synonyms
ASK120067
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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NPJ Precis Oncol
High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]2026 Apr 8;10(1):211. PMID: 41951768 -
J Med Chem
2025 Aug 28;68(16):17917-17932. PMID: 40801664
Solvente y solubilidad
DMSO : 100 mg/mL (183.13 mM; Need ultrasonic; 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, 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: ≥ 2.5 mg/mL (4.58 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.
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 mM | 1.8313 mL | 9.1565 mL | 18.3130 mL | 45.7825 mL |
| 5 mM | 0.3663 mL | 1.8313 mL | 3.6626 mL | 9.1565 mL | |
| 10 mM | 0.1831 mL | 0.9157 mL | 1.8313 mL | 4.5783 mL | |
| 15 mM | 0.1221 mL | 0.6104 mL | 1.2209 mL | 3.0522 mL | |
| 20 mM | 0.0916 mL | 0.4578 mL | 0.9157 mL | 2.2891 mL | |
| 25 mM | 0.0733 mL | 0.3663 mL | 0.7325 mL | 1.8313 mL | |
| 30 mM | 0.0610 mL | 0.3052 mL | 0.6104 mL | 1.5261 mL | |
| 40 mM | 0.0458 mL | 0.2289 mL | 0.4578 mL | 1.1446 mL | |
| 50 mM | 0.0366 mL | 0.1831 mL | 0.3663 mL | 0.9157 mL | |
| 60 mM | 0.0305 mL | 0.1526 mL | 0.3052 mL | 0.7630 mL | |
| 80 mM | 0.0229 mL | 0.1145 mL | 0.2289 mL | 0.5723 mL | |
| 100 mM | 0.0183 mL | 0.0916 mL | 0.1831 mL | 0.4578 mL |
limertinib Related Classifications
HY-138751 Related Classifications
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