limertinib diTFA
Based on 2 publication(s) in Google Scholar
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFRT790M (IC50: 0.3 nM) with selectivity over EGFRWT (IC50: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- Purity: 98.96%
- Formula: C33H34ClF6N7O6
- Molecular Weight:774.11
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
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Publications Citing Use of MedChemExpress (MCE) limertinib diTFA
MoreAll EGFR Isoforms
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Biological Activity
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Molecular Weight 774.11
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Formula C33H34ClF6N7O6
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Color Light yellow to light brown
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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.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
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Synonyms
ASK120067 diTFA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
Solvent & Solubility
DMSO : 175 mg/mL (226.07 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 (protect from light). 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 (protect from light). 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: ≥ 5 mg/mL (6.46 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (6.46 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (276 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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Handling Instructions (2659 KB)
References
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 (protect from light). 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 | 1.2918 mL | 6.4590 mL | 12.9181 mL | 32.2952 mL |
| 5 mM | 0.2584 mL | 1.2918 mL | 2.5836 mL | 6.4590 mL | |
| 10 mM | 0.1292 mL | 0.6459 mL | 1.2918 mL | 3.2295 mL | |
| 15 mM | 0.0861 mL | 0.4306 mL | 0.8612 mL | 2.1530 mL | |
| 20 mM | 0.0646 mL | 0.3230 mL | 0.6459 mL | 1.6148 mL | |
| 25 mM | 0.0517 mL | 0.2584 mL | 0.5167 mL | 1.2918 mL | |
| 30 mM | 0.0431 mL | 0.2153 mL | 0.4306 mL | 1.0765 mL | |
| 40 mM | 0.0323 mL | 0.1615 mL | 0.3230 mL | 0.8074 mL | |
| 50 mM | 0.0258 mL | 0.1292 mL | 0.2584 mL | 0.6459 mL | |
| 60 mM | 0.0215 mL | 0.1077 mL | 0.2153 mL | 0.5383 mL | |
| 80 mM | 0.0161 mL | 0.0807 mL | 0.1615 mL | 0.4037 mL | |
| 100 mM | 0.0129 mL | 0.0646 mL | 0.1292 mL | 0.3230 mL |
limertinib diTFA Related Classifications
HY-138751A Related Classifications
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