| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Trk (tropomyosin receptor kinase) family. GNF-8625 is a Trk inhibitor that effectively disrupts the signaling pathways associated with Trk receptors, which are implicated in neurotrophic signaling and oncogenesis.
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| ln Vitro |
Specific IC50 values for GNF-8625 are not published, as it is a chemical probe from a patent. However, as a Trk inhibitor, it is expected to block the phosphorylation of Trk receptors in a dose-dependent manner, leading to the inhibition of downstream signaling cascades such as RAS-MAPK and PI3K-AKT, which are involved in cell survival and proliferation.
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| ln Vivo |
No specific in vivo data are reported for GNF-8625. As a Trk inhibitor, it is predicted to have antitumor activity in preclinical models of NTRK-fusion-positive cancers. It is also used as a tool to investigate the role of Trk receptors in neuronal survival, differentiation, and nerve regeneration, making it a valuable tool for both oncology and neurobiology.
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| Enzyme Assay |
Cell-free Trk kinase assays are performed using recombinant TrkA, TrkB, or TrkC enzymes. The compound is incubated with the enzyme, a peptide substrate, and ATP for 30-60 minutes. Kinase activity is measured using a luminescence-based ADP detection kit. IC50 values are determined from a dose-response curve.
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| Cell Assay |
NTRK-fusion-positive cancer cell lines (e.g., KM-12 for TrkA) are seeded in 96-well plates. After an overnight incubation, cells are treated with increasing concentrations of GNF-8625. Following a 72-hour treatment, cell viability is assessed using the MTT assay. The effect on downstream signaling is evaluated by Western blotting for p-ERK and p-AKT.
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| Animal Protocol |
For an oncology study, nude mice are subcutaneously implanted with NTRK-fusion-positive tumor cells. When tumors are established, mice are treated daily with GNF-8625 by oral gavage. Tumor volumes are measured with calipers. For neurobiology studies, a sciatic nerve injury model in rats is used, and the compound is administered locally to assess nerve regeneration.
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| ADME/Pharmacokinetics |
No specific PK data are reported. The compound is formulated as a hydrochloride salt (C25H27ClFN7, MW 479.98) with CAS number 2412055-62-8. For research use, it is dissolved in DMSO to prepare a stock solution. It is predicted to be orally bioavailable, but this has not been confirmed.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported. As a Trk inhibitor, on-target toxicity may include peripheral neuropathy. This chemical is for research use only and is not intended for human consumption. It is not an FDA-approved drug.
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| References | |
| Additional Infomation |
Other information: GNF-8625 monopyridin-N-piperazine hydrochloride is from patent WO 2020038415 A1. It is a chemical probe for studying the Trk family of receptors. It is distinct from other Trk inhibitors like larotrectinib and entrectinib, making it a valuable tool for structure-activity relationship studies. For research use only.
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| Molecular Formula |
C25H27CLFN7
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|---|---|
| Molecular Weight |
479.980186700821
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| Exact Mass |
479.2
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| CAS # |
2412055-62-8
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| PubChem CID |
156767394
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
646
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| Defined Atom Stereocenter Count |
1
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| SMILES |
Cl.FC1=CC=CC(=C1)[C@H]1CCCN1C1C=CC2=NC=C(C3=CC=CC(=N3)N3CCNCC3)N2N=1
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| InChi Key |
XQABKTNVPTUVLG-ZMBIFBSDSA-N
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| InChi Code |
InChI=1S/C25H26FN7.ClH/c26-19-5-1-4-18(16-19)21-7-3-13-32(21)25-10-9-23-28-17-22(33(23)30-25)20-6-2-8-24(29-20)31-14-11-27-12-15-31;/h1-2,4-6,8-10,16-17,21,27H,3,7,11-15H2;1H/t21-;/m1./s1
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| Chemical Name |
6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]-3-(6-piperazin-1-ylpyridin-2-yl)imidazo[1,2-b]pyridazine;hydrochloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 6.67 mg/mL (13.90 mM)
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| 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 | 2.0834 mL | 10.4171 mL | 20.8342 mL | |
| 5 mM | 0.4167 mL | 2.0834 mL | 4.1668 mL | |
| 10 mM | 0.2083 mL | 1.0417 mL | 2.0834 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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