FIIN-2
Based on 1 Customer Validation
FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
For research use only. We do not sell to patients.
- Purity: 99.32%
- CAS No.: 1633044-56-0
- Formula: C35H38N8O4
- Molecular Weight:634.73
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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FGFR1 3.1 nM (IC50) |
FGFR2 4.3 nM (IC50) |
FGFR3 27 nM (IC50) |
FGFR4 45 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | EC50 |
1 nM
Compound: 21; FIIN-2
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Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR1 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR1 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
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[PMID: 34962782] |
| BaF3 | EC50 |
1 nM
Compound: 21; FIIN-2
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Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR2 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR2 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
|
[PMID: 34962782] |
| BaF3 | EC50 |
1 nM
Compound: 21; FIIN-2
|
Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR3 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR3 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
|
[PMID: 34962782] |
| BaF3 | EC50 |
1 nM
Compound: 21; FIIN-2
|
Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR4 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR4 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
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[PMID: 34962782] |
| BaF3 | EC50 |
58 nM
Compound: 21; FIIN-2
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Antiproliferative activity against mouse BaF3 cells harboring FGFR2 V564M mutant assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring FGFR2 V564M mutant assessed as reduction in cell proliferation measured after 72 hrs by MTS assay
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[PMID: 34962782] |
FIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F[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.
Chemical Information
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CAS No. 1633044-56-0
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Appearance Solid
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Molecular Weight 634.73
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Formula C35H38N8O4
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Color White to off-white
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SMILES
C=CC(NC1=CC=C(CN(C2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2CN5C6=CC(OC)=CC(OC)=C6)C5=O)C=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 100 mg/mL (157.55 mM; 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, 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)
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 (3.94 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.94 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 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.
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.
Protocol
TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of the compounds. After 72 h the cells are assessed by MTS tetrazolium assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (273 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)
- Portuguese - PT (393 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, 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 | 1.5755 mL | 7.8774 mL | 15.7547 mL | 39.3868 mL |
| 5 mM | 0.3151 mL | 1.5755 mL | 3.1509 mL | 7.8774 mL | |
| 10 mM | 0.1575 mL | 0.7877 mL | 1.5755 mL | 3.9387 mL | |
| 15 mM | 0.1050 mL | 0.5252 mL | 1.0503 mL | 2.6258 mL | |
| 20 mM | 0.0788 mL | 0.3939 mL | 0.7877 mL | 1.9693 mL | |
| 25 mM | 0.0630 mL | 0.3151 mL | 0.6302 mL | 1.5755 mL | |
| 30 mM | 0.0525 mL | 0.2626 mL | 0.5252 mL | 1.3129 mL | |
| 40 mM | 0.0394 mL | 0.1969 mL | 0.3939 mL | 0.9847 mL | |
| 50 mM | 0.0315 mL | 0.1575 mL | 0.3151 mL | 0.7877 mL | |
| 60 mM | 0.0263 mL | 0.1313 mL | 0.2626 mL | 0.6564 mL | |
| 80 mM | 0.0197 mL | 0.0985 mL | 0.1969 mL | 0.4923 mL | |
| 100 mM | 0.0158 mL | 0.0788 mL | 0.1575 mL | 0.3939 mL |
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