| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| Other Sizes |
| Targets |
FGFR3 3 nM (IC50) FGFR2 44 nM (IC50) FGFR1 289 nM (IC50)
FGFR3 (primary target), FGFR2, FGFR1. FGFR3-IN-5 is a selective FGFR3 inhibitor with IC50 values of 3 nM for FGFR3, 44 nM for FGFR2, and 289 nM for FGFR1, demonstrating approximately 15-fold selectivity for FGFR3 over FGFR2 and 96-fold over FGFR1. |
|---|---|
| ln Vitro |
FGFR phosphorylation is inhibited by FGFR3-IN-5 (compound 37; 5 mM; 1 h; HEK-293 cells), with IC50 values of 8 nM and 59 nM for FGFR3 and FGFR1, respectively [1].
FGFR3-IN-5 inhibits FGFR3 with an IC50 of 3 nM, FGFR2 with an IC50 of 44 nM, and FGFR1 with an IC50 of 289 nM. In HEK-293 cells (5 mM; 1 h), it inhibits FGFR phosphorylation with IC50 values of 8 nM (FGFR3) and 59 nM (FGFR1). Its selectivity makes it valuable for FGFR3-specific research. |
| ln Vivo |
No specific in vivo activity data are reported for FGFR3-IN-5. As a selective FGFR3 inhibitor, it is expected to have anti-tumor activity in FGFR3-driven cancer models, such as RT4 bladder cancer (FGFR3-TACC3 fusion) or multiple myeloma models. It can be used in cancer research to study FGFR3-dependent proliferation and survival pathways.
|
| 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 3 nM (FGFR3), 44 nM (FGFR2), and 289 nM (FGFR1) are calculated.
|
| Cell Assay |
HEK-293 cells are treated with FGFR3-IN-5 at 5 mM for 1 hour to assess FGFR phosphorylation. For proliferation assays, FGFR3-dependent cancer cell lines (e.g., RT4 bladder cancer cells) are seeded in 96-well plates and treated with increasing concentrations for 72 hours. Cell viability is assessed by MTT assay. The effect on FGFR3 phosphorylation is measured by Western blot.
|
| Animal Protocol |
For in vivo studies, FGFR3-IN-5 would be administered orally to mice bearing FGFR3-driven tumor xenografts (e.g., RT4). Dosing regimens are not specified but typically range from 10-50 mg/kg daily. Tumor volumes are measured with calipers. At termination, tumors are excised for analysis of FGFR3 phosphorylation and downstream signaling. No published studies are available.
|
| ADME/Pharmacokinetics |
No specific PK data are reported for FGFR3-IN-5. The molecular weight is 448.9 (C18H15Cl2N5O2S). CAS 2446664-72-6. It is soluble in DMSO (10-50 mg/mL). For in vivo studies, it would typically be formulated in 0.5% methylcellulose or a DMSO/PEG300/Tween-80/saline mixture. PK parameters have not been characterized.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are reported for FGFR3-IN-5. As a selective FGFR3 inhibitor, potential on-target toxicities may include effects on bone growth and development, given the role of FGFR3 in skeletal homeostasis. Comprehensive toxicological assessments have not been published. The compound is for research use only.
|
| References | |
| Additional Infomation |
Other information: FGFR3-IN-5 (CAS 2446664-72-6) is a research compound and not FDA-approved. It is a potent and selective FGFR3 inhibitor with an IC50 of 3 nM and demonstrates significant selectivity over FGFR2 and FGFR1. It is valuable for studying FGFR3-driven cancers, including bladder cancer and multiple myeloma. For research use only.
|
| Molecular Formula |
C24H24FN7O3
|
|---|---|
| Molecular Weight |
477.490867614746
|
| Exact Mass |
477.192
|
| CAS # |
2446664-72-6
|
| PubChem CID |
153619578
|
| Appearance |
White to off-white solid powder
|
| LogP |
0.7
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
35
|
| Complexity |
895
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C12=C(C#N)C=NN1C=C(C1=CN(C3CCN(C(C4(F)CN(C(=O)C=C)C4)=O)CC3)N=C1)C=C2OC
|
| InChi Key |
GUEZCEZQFMVREH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H24FN7O3/c1-3-21(33)30-14-24(25,15-30)23(34)29-6-4-19(5-7-29)31-13-18(11-27-31)16-8-20(35-2)22-17(9-26)10-28-32(22)12-16/h3,8,10-13,19H,1,4-7,14-15H2,2H3
|
| Chemical Name |
6-[1-[1-(3-fluoro-1-prop-2-enoylazetidine-3-carbonyl)piperidin-4-yl]pyrazol-4-yl]-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0943 mL | 10.4714 mL | 20.9428 mL | |
| 5 mM | 0.4189 mL | 2.0943 mL | 4.1886 mL | |
| 10 mM | 0.2094 mL | 1.0471 mL | 2.0943 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
