| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
FIIN-2 (FIIN 2; FIIN2) is a novel irreversible/covalent pan-FGFR inhibitor with potential anticancer activity. It has IC50 values of 3.09 nM, 4.3 nM, 27 nM, and 45.3 nM, which indicate that it inhibits FGFR1/2/3/4. High anti-proliferative activity of FIIN-2 is seen in vitro against cells that are dependent on FGFR1 or FGFR2 gatekeeper mutants.
| Targets |
FGFR1 (IC50 = 3.1 nM); FGFR2 (IC50 = 4.3 nM); FGFR3 (IC50 = 27 nM); FGFR4 (IC50 = 45 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
A broad-coverage kinase binding assay platform based on TR-FRET is used to conduct biochemical experiments.
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| Cell Assay |
One day after being plated at a density of 1,500 cells per well in 96-well plates, NCI-H2077, NCI-H1581, H520, Kato III, AN3CA, RT112, A2780, 4T1, and SKOV-3 cells are treated with inhibitors. FGFR1 V561M is ectopically overexpressed in NCI-H2077 or NCI-H1581 cells through lentiviral transduction to create the gatekeeper mutation cell lines. Using the Cell-Titer-Glo reagent and the manufacturer's instructions, cell survival is measured 96 hours after the inhibitor is added. GraphPad Prism 5 is used to compute EC50 values. FGF or EGF ligand is also applied to SKOV-3 cells during treatment. A luminometer was used to measure proliferation after 96 hours. Relative values are used to display data. Comparing the luminescence of cells treated with the indicated inhibitor dose to untreated cells is done.
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| Animal Protocol |
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| References |
| Molecular Formula |
C35H38N8O4
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| Molecular Weight |
634.73
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| Exact Mass |
634.301
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| Elemental Analysis |
C, 66.23; H, 6.03; N, 17.65; O, 10.08
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| CAS # |
1633044-56-0
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| Related CAS # |
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| PubChem CID |
91825767
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.666
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| LogP |
1.82
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
47
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(C2C=C(C=C(C=2)OC)OC)CC2=CN=C(N=C2N1CC1C=CC(=CC=1)NC(C=C)=O)NC1C=CC(=CC=1)N1CCN(C)CC1
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| InChi Key |
DVBPRWJMHURKHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H38N8O4/c1-5-32(44)37-26-8-6-24(7-9-26)22-43-33-25(23-42(35(43)45)29-18-30(46-3)20-31(19-29)47-4)21-36-34(39-33)38-27-10-12-28(13-11-27)41-16-14-40(2)15-17-41/h5-13,18-21H,1,14-17,22-23H2,2-4H3,(H,37,44)(H,36,38,39)
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| Chemical Name |
N-[4-[[3-(3,5-dimethoxyphenyl)-7-[4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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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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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5755 mL | 7.8774 mL | 15.7547 mL | |
| 5 mM | 0.3151 mL | 1.5755 mL | 3.1509 mL | |
| 10 mM | 0.1575 mL | 0.7877 mL | 1.5755 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibition of FGFR-dependent signaling by BGJ398, FIIN-2, and FIIN-3 in Tel/FGFR2 V564M Ba/F3 cells. Cells were treated with a dose escalation of inhibitors for 6 h and then were lysed and subjected to Western blot for the indicated proteins or phosphoproteins. Proc Natl Acad Sci U S A. 2014 Nov 11; 111(45): E4869–E4877. |
Inhibition of FGFR-dependent signaling by BGJ398, FIIN-2, and FIIN-3 in H1581 (FGFR1 WT or V561M) cells. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77. |
Effects of FIIN-2, FIIN-3, and FRIN-3 on FGF- and EGF-induced dispersion of SKOV-3 cells in a 3D microfluidic device. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77. |
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