| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
FGFR1 0.75 nM (IC50) FGFR2 0.5 nM (IC50) FGFR3 3.05 nM (IC50)
FGFR1, FGFR2, FGFR3 (with lower activity against FGFR4). CPL304110 is a selective FGFR1-3 inhibitor, with selectivity over KDR (VEGFR2), FLT3, Aurora A, and PDGFRbeta of >45-fold, >345-fold, >395-fold, and >680-fold, respectively. |
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| ln Vitro |
CPL304110 (0-0.6 μM) inhibits downstream signaling (p-ERK) and FGFR2 phosphorylation in a dose-dependent manner[1]. In the SNU-16 proliferation assay, CPL304110 (compound 56q) shows an IC50 of 85.64 nM[1]. In comparison to FGFR2, CPL304110 (compound 56q) exhibits a selectivity over KDR (VEGFR2), Flt3, Aura A, and PDGFRb that is more than 45-fold, 345-fold, 395-fold, and 680-fold, respectively. No discernible inhibitory effects were seen with other tyrosine kinases[1].
CPL304110 inhibits FGFR1 with an IC50 of 0.75 nM, FGFR2 with an IC50 of 0.5 nM, FGFR3 with an IC50 of 3.05 nM, and FGFR4 with an IC50 of 87.90 nM. In SNU-16 gastric cancer cells, it shows an IC50 of 85.64 nM. It efficiently decreases viability of A375 and RPMI7951 melanoma cells with IC50 below 1 uM. |
| ln Vivo |
Mice treated with CPL304110 (po, 40 mg/kg) show a t1/2 of 2 h and a Cmax of 3369 ng/mL[1]. In mice, CPL304110 (compound 56q, 2 X 20 mg/kg) dramatically suppresses tumor growth without causing toxicity or appreciable body loss. Tumor growth inhibition (TGI) at day 21 (D21, day of termination) is 64% when dosed twice daily at 20 mg/kg[1].
CPL304110 has shown high efficiency against the proliferation of A375 melanoma cells. It is orally bioavailable and is expected to have anti-tumor activity in FGFR-dependent cancer models. In vivo efficacy data in xenograft models have not been fully detailed, but its biochemical and cellular potencies support in vivo evaluation. |
| Enzyme Assay |
Cell-free FGFR1, FGFR2, FGFR3, and FGFR4 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 are calculated from dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: SNU-16 cell lines. Tested Tested Concentrations: 0-0.6 μM. Incubation Duration: 1 h. Experimental Results: Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK) Melanoma cell lines (A375, RPMI7951) or SNU-16 cells are seeded in 96-well plates and treated with increasing concentrations of CPL304110 for 72 hours. Cell viability is assessed using the MTT assay. The effect on FGFR phosphorylation and downstream signaling (p-FRS2, p-ERK) is measured by Western blotting. IC50 values (85.64 nM in SNU-16) are determined. |
| Animal Protocol |
Animal/Disease Models: Severe combined immunodeficient (SCID) mice implanted subcutaneously (sc) with SNU-16 (human)[1].
Doses: 20 mg/kg (X2). Route of Administration: Orally, twice (two times) daily for 21 days. Experimental Results: After 6 hrs (hours) of last dosing, concentration of 56q diminished in the plasma (9 %) but increased stepwise in the tumor cells (121%). For in vivo studies, CPL304110 would be administered orally to mice bearing FGFR-driven tumor xenografts (e.g., SNU-16). Dosing is typically once daily for 2-4 weeks. Tumor volumes are measured with calipers. At study termination, tumors are excised for pharmacodynamic analysis of FGFR phosphorylation and downstream signaling. |
| ADME/Pharmacokinetics |
CPL304110 is an orally bioavailable FGFR inhibitor. As a small molecule (MW 435.44, C24H21N7O), it is formulated for in vivo studies using standard vehicles such as 0.5% methylcellulose. Its high oral bioavailability and selectivity profile support once-daily dosing in preclinical models, but detailed PK parameters are not fully reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for CPL304110. As a selective FGFR1-3 inhibitor, potential on-target toxicities may include hyperphosphatemia, tissue calcification, and gastrointestinal effects, which are class-related. Comprehensive toxicological assessments have not been published. The compound is a research-grade chemical.
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| References | |
| Additional Infomation |
Other information: CPL304110 (CAS 1627826-19-0) is a research compound and not FDA-approved. It is a potent and selective FGFR1-3 inhibitor with single-digit nanomolar IC50 values. Its oral bioavailability makes it a valuable tool for in vivo studies of FGFR-driven cancers. Purity ≥98%. For research use only. Synonyms: CPL304110.
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| Molecular Formula |
C25H30N6O2
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|---|---|
| Molecular Weight |
446.544704914093
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| Exact Mass |
446.243
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| CAS # |
1627826-19-0
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| PubChem CID |
136387462
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| Appearance |
White to light yellow solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
606
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1NN=C(C2=NC3=CC=C(N4CCN(C)CC4)C=C3N2)C=1)CC1C=C(OC)C=C(OC)C=1
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| InChi Key |
QHCGPJPIPKDWAT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30N6O2/c1-30-8-10-31(11-9-30)19-6-7-22-23(15-19)27-25(26-22)24-14-18(28-29-24)5-4-17-12-20(32-2)16-21(13-17)33-3/h6-7,12-16H,4-5,8-11H2,1-3H3,(H,26,27)(H,28,29)
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| Chemical Name |
2-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-6-(4-methylpiperazin-1-yl)-1H-benzimidazole
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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: 100 mg/mL (223.94 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.60 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 (5.60 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 (5.60 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 | 2.2394 mL | 11.1972 mL | 22.3944 mL | |
| 5 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2394 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.
Link: https://clinicaltrials.gov/ct2/show/NCT04149691
Conditions:Gastric Cancer|Bladder Cancer|Squamous Non-small Cell Lung Cancer|Cholangiocarcinoma|Sarcoma|Endometrial Cancer|Other Solid TumoursProducts are for research use only; We do not sell to patients
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