| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
FGFR2 29 nM (IC50) FGFR1 389 nM (IC50) FGFR3 758 nM (IC50)
FGFR2 (primary target), FGFR1, FGFR3. FGFR2-IN-2 is a selective antagonist of FGFR2 with IC50s of 389 nM for FGFR1, 29 nM for FGFR2, and 758 nM for FGFR3, showing approximately 13-fold selectivity for FGFR2 over FGFR1. |
|---|---|
| ln Vitro |
FGFR2-IN-2 inhibits FGFR2 with an IC50 of 29 nM, FGFR1 with an IC50 of 389 nM, and FGFR3 with an IC50 of 758 nM. It demonstrates approximately 13-fold selectivity for FGFR2 over FGFR1. Its in vitro activity makes it a useful tool for exploring FGFR2-specific pathways.
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| ln Vivo |
No specific in vivo activity data are reported for FGFR2-IN-2. As a selective FGFR2 inhibitor, it is expected to have anti-tumor activity in FGFR2-driven cancer models, such as gastric cancer (SNU-16) or endometrial cancer. Its selectivity for FGFR2 makes it valuable for studying FGFR2-specific biology without off-target FGFR1/3 effects.
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| Enzyme Assay |
Cell-free FGFR1, FGFR2, and FGFR3 kinase assays are performed using recombinant human enzymes. The compound is incubated with the enzyme and a peptide substrate in the presence of ATP for 30-60 minutes. Kinase activity is measured using a luminescence-based ADP detection kit. IC50 values of 389 nM (FGFR1), 29 nM (FGFR2), and 758 nM (FGFR3) are calculated from dose-response curves.
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| Cell Assay |
FGFR2-dependent cancer cell lines (e.g., SNU-16 gastric cancer cells) are seeded in 96-well plates and treated with increasing concentrations of FGFR2-IN-2 for 72 hours. Cell viability is assessed using the CellTiter-Glo reagent. The effect on FGFR2 phosphorylation and downstream signaling (p-FRS2, p-ERK) is measured by Western blotting. IC50 for cell proliferation is determined.
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| Animal Protocol |
For in vivo studies, FGFR2-IN-2 would be administered orally to mice bearing FGFR2-driven tumor xenografts. Dosing regimens are not specified but typically range from 10-100 mg/kg daily. Tumor volumes are measured with calipers. At termination, tumors are excised for analysis of FGFR2 phosphorylation and downstream signaling. No published studies are available.
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| ADME/Pharmacokinetics |
No specific PK data are reported for FGFR2-IN-2. The molecular weight is 432.43 (C20H17F3N4O2S). CAS 2677709-81-6. The compound is soluble in DMSO (10-50 mg/mL). For in vivo studies, it would typically be formulated in 0.5% methylcellulose. Oral bioavailability and half-life have not been characterized.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for FGFR2-IN-2. As a selective FGFR2 inhibitor, potential on-target toxicities may include effects on FGFR2-dependent tissues, such as bone and mammary gland development. Comprehensive toxicological assessments have not been published. The compound is for research use only.
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| References | |
| Additional Infomation |
Other information: FGFR2-IN-2 (CAS 2677709-81-6) is a research compound and not FDA-approved. It is a selective FGFR2 inhibitor with IC50s of 29 nM (FGFR2), 389 nM (FGFR1), and 758 nM (FGFR3). It is valuable for studying FGFR2-specific signaling pathways in cancer and cardiovascular disease. For research use only.
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| Molecular Formula |
C23H22N4O
|
|---|---|
| Molecular Weight |
370.45
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| Exact Mass |
370.179
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| CAS # |
2677709-81-6
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| PubChem CID |
157049298
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
495
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(O)=CC=C(C2=CC3=C(C=C2)C(C2=CC=C(N4CCNCC4)C=C2)=NN3)C=C1
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| InChi Key |
OYKIIJTXTXJYKZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H22N4O/c28-20-8-3-16(4-9-20)18-5-10-21-22(15-18)25-26-23(21)17-1-6-19(7-2-17)27-13-11-24-12-14-27/h1-10,15,24,28H,11-14H2,(H,25,26)
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| Chemical Name |
4-[3-(4-piperazin-1-ylphenyl)-1H-indazol-6-yl]phenol
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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 |
| 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) |
DMSO: 62.5 mg/mL (168.71 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.61 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6994 mL | 13.4971 mL | 26.9942 mL | |
| 5 mM | 0.5399 mL | 2.6994 mL | 5.3988 mL | |
| 10 mM | 0.2699 mL | 1.3497 mL | 2.6994 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.
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