FIIN-1
Based on 1 Customer Validation
FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.
For research use only. We do not sell to patients.
- Purity: 99.04%
- CAS No.: 1256152-35-8
- Formula: C32H39Cl2N7O4
- Molecular Weight:656.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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FGFR1 2.8 nM (Kd) |
FGFR2 6.9 nM (Kd) |
FGFR3 5.4 nM (Kd) |
FGFR4 120 nM (Kd) |
FGFR1 9.2 nM (IC50) |
FGFR2 6.2 nM (IC50) |
FGFR3 11.9 nM (IC50) |
FGFR4 189 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H520 | IC50 |
121 nM
Compound: 1; FIIN-1
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Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay
Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay
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[PMID: 28521156] |
| SW780 | IC50 |
277 nM
Compound: 1; FIIN-1
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Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay
Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay
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[PMID: 28521156] |
FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480 and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively[1].
FIIN-1 (14 nM-46 μM; 72 hours) inhibits proliferation of FGF signaling-sensitive cancer cell lines[1].
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Stomach KATO III, SNU-16 and FU97 cells; Bladder RT4 cells; Kidney G-401 and G-402 cells; Lung SBC-3 and H520 cells; Pancreas A2.1 cells; Ovary A2780 and PA-1 cells; Bone RD-ES cells
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Concentration:
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Incubation Time:72 hours
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Result:The EC50 of 70 nM for Bladder RT4 cell.
The EC50 of 230 nM for Pancreas A2.1 cell.
The EC50 of 2.3 μM for Bone RD-ES cell.
EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively.
EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively.
EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively.
EC50s of 0.014, 0.03 and 0.65 μM for Stomach KATO III, SNU-16, FU97 cells, respectively.
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Cell Line:Serum-starved MCF10A cells that stably express iFGFR1
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Concentration:20 nM
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Incubation Time:30 minutes
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Result:Blocked activation of iFGFR1 and phosphorylation of downstream effectors Erk1/2.
Chemical Information
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CAS No. 1256152-35-8
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Appearance Solid
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Molecular Weight 656.60
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Formula C32H39Cl2N7O4
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Color White to off-white
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SMILES
C=CC(NC1=CC=CC(CN(C2=NC(NCCCCN(CC)CC)=NC=C2CN3C4=C(Cl)C(OC)=CC(OC)=C4Cl)C3=O)=C1)=O
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Synonyms
FGFR irreversible inhibitor-1
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (152.30 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: ≥ 2.08 mg/mL (3.17 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.
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.
Purity & Documentation
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Data Sheet (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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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. 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 | 1.5230 mL | 7.6150 mL | 15.2300 mL | 38.0749 mL |
| 5 mM | 0.3046 mL | 1.5230 mL | 3.0460 mL | 7.6150 mL | |
| 10 mM | 0.1523 mL | 0.7615 mL | 1.5230 mL | 3.8075 mL | |
| 15 mM | 0.1015 mL | 0.5077 mL | 1.0153 mL | 2.5383 mL | |
| 20 mM | 0.0761 mL | 0.3807 mL | 0.7615 mL | 1.9037 mL | |
| 25 mM | 0.0609 mL | 0.3046 mL | 0.6092 mL | 1.5230 mL | |
| 30 mM | 0.0508 mL | 0.2538 mL | 0.5077 mL | 1.2692 mL | |
| 40 mM | 0.0381 mL | 0.1904 mL | 0.3807 mL | 0.9519 mL | |
| 50 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7615 mL | |
| 60 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6346 mL | |
| 80 mM | 0.0190 mL | 0.0952 mL | 0.1904 mL | 0.4759 mL | |
| 100 mM | 0.0152 mL | 0.0761 mL | 0.1523 mL | 0.3807 mL |
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