F-1
Based on 1 Customer Validation
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively.
For research use only. We do not sell to patients.
- Purity: 98.03%
- CAS No.: 2244775-31-1
- Formula: C22H27ClN8O3S
- Molecular Weight:519.02
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>1 μM
Compound: F-1
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Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
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[PMID: 30223120] |
| BaF3 | IC50 |
0.03 μM
Compound: F-1
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Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay
Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay
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[PMID: 30223120] |
| HCC78 | IC50 |
0.043 μM
Compound: F-1
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Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay
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[PMID: 30223120] |
| KARPAS-299 | IC50 |
0.01 μM
Compound: F-1
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Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay
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[PMID: 30223120] |
| NCI-H2228 | IC50 |
0.012 μM
Compound: F-1
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Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay
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[PMID: 30223120] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2244775-31-1
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Appearance Solid
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Molecular Weight 519.02
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Formula C22H27ClN8O3S
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Color White to off-white
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SMILES
O=S(NC1=C(NC2=NC(NC3=C(OC)N=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)C=CC=C1)(C)=O
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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)
Solvent & Solubility
DMSO : 125 mg/mL (240.84 mM; ultrasonic and warming and heat to 65°C; 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: ≥ 2.08 mg/mL (4.01 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.01 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (271 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 | 1.9267 mL | 9.6335 mL | 19.2671 mL | 48.1677 mL |
| 5 mM | 0.3853 mL | 1.9267 mL | 3.8534 mL | 9.6335 mL | |
| 10 mM | 0.1927 mL | 0.9634 mL | 1.9267 mL | 4.8168 mL | |
| 15 mM | 0.1284 mL | 0.6422 mL | 1.2845 mL | 3.2112 mL | |
| 20 mM | 0.0963 mL | 0.4817 mL | 0.9634 mL | 2.4084 mL | |
| 25 mM | 0.0771 mL | 0.3853 mL | 0.7707 mL | 1.9267 mL | |
| 30 mM | 0.0642 mL | 0.3211 mL | 0.6422 mL | 1.6056 mL | |
| 40 mM | 0.0482 mL | 0.2408 mL | 0.4817 mL | 1.2042 mL | |
| 50 mM | 0.0385 mL | 0.1927 mL | 0.3853 mL | 0.9634 mL | |
| 60 mM | 0.0321 mL | 0.1606 mL | 0.3211 mL | 0.8028 mL | |
| 80 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.6021 mL | |
| 100 mM | 0.0193 mL | 0.0963 mL | 0.1927 mL | 0.4817 mL |
F-1 Related Classifications
HY-112801 Related Classifications
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