Olafertinib
Based on 1 Customer Validation
Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.51%
- CAS No.: 1660963-42-7
- Formule: C29H28F2N6O2
- Masse moléculaire:530.57
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
GI50: 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19), 689 nM (EGFR WT)[1].
In Vitro
Olafertinib (Compound CK-101) (72 h) selectively inhibits cell proliferation of cell lines expressing both the activating (e.g. HCC827, IC50 < 0.015 μM) and resistance mutations (NCI-H1975, IC50 < 0.005 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Olafertinib inhibits tumor growth by up to 90% in a xenograft study of PC-9 cells in SCID/Beige mice[2].
Olafertinib inhibits tumor growth by up to 95% in a xenograft study of NCI-H1975 cells in BALB/c nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1660963-42-7
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Appearance Solid
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Masse moléculaire 530.57
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Formule C29H28F2N6O2
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Color Light yellow to yellow
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SMILES
OCCN1CCN(C2=C(F)C(F)=C(NC3=NC=C4C(C(C5=CC(NC(C=C)=O)=CC=C5)=CC=C4)=N3)C=C2)CC1
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Synonyms
CK-101; RX518
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (235.60 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (3.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (272 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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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8848 mL | 9.4238 mL | 18.8477 mL | 47.1191 mL |
| 5 mM | 0.3770 mL | 1.8848 mL | 3.7695 mL | 9.4238 mL | |
| 10 mM | 0.1885 mL | 0.9424 mL | 1.8848 mL | 4.7119 mL | |
| 15 mM | 0.1257 mL | 0.6283 mL | 1.2565 mL | 3.1413 mL | |
| 20 mM | 0.0942 mL | 0.4712 mL | 0.9424 mL | 2.3560 mL | |
| 25 mM | 0.0754 mL | 0.3770 mL | 0.7539 mL | 1.8848 mL | |
| 30 mM | 0.0628 mL | 0.3141 mL | 0.6283 mL | 1.5706 mL | |
| 40 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1780 mL | |
| 50 mM | 0.0377 mL | 0.1885 mL | 0.3770 mL | 0.9424 mL | |
| 60 mM | 0.0314 mL | 0.1571 mL | 0.3141 mL | 0.7853 mL | |
| 80 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5890 mL | |
| 100 mM | 0.0188 mL | 0.0942 mL | 0.1885 mL | 0.4712 mL |
Olafertinib Related Classifications
HY-19815 Related Classifications
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