AF38469 |
Katalog-Nr.GC19023
One-Click Copy Product Info
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AF38469 ist ein selektiver, oral bioverfÜgbarer Sortilin-Inhibitor mit einem IC50-Wert von 330 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1531634-31-7
Sample solution is provided at 25 µL, 10mM.
AF38469 is an orally active Sortilin (SORT1; IC₅₀=330nM) receptor inhibitor[1-2]. AF38469 possesses antioxidant functions. AF38469 can be used in research related to neurodegenerative diseases and cancer[3-4].
In vitro, pancreatic cancer cells (PANC-1, MIA PaCa-2, PaCa-44) were treated with AF38469 (10μM) for 6-24 hours. AF38469 inhibited cell adhesion and invasion, reduced cell migration capacity, and decreased the phosphorylation of focal adhesion kinase (FAK) at Tyr925[5]. Human primary Müller cells and rat Müller cells (rMC-1) cultured under 25mM high glucose conditions were treated with AF38469 (20μM) for 24 hours. AF38469 significantly reduced the protein levels of sortilin, NOD-like receptor protein 3 (NLRP3), tumor necrosis factor α (TNFα), P75 neurotrophin receptor (P75NTR), lysosomal-associated membrane protein 2 (LAMP2), and cleaved caspase 3[6].
In vivo, mice bearing MDA-MB 231-luc xenografts and receiving repetitive GRN A injections were treated with AF38469 (5-10μg/day/mouse) via drinking water for 3 weeks. AF38469 significantly reduced GRN A-induced lung metastasis and prevented cancer cell infiltration of the skin[7]. Male C57BL/6J mice on a Western diet starting at 12 weeks of age for 8 weeks were treated with AF38469 (approximately 4mg/kg/day, orally mixed in feed). AF38469 significantly lowered plasma cholesterol levels and reduced hepatic VLDL secretion and pro-inflammatory cytokine expression[8].
References:
[1] Pearson AC, Miller JS, Jensen HJ, et al. Neurotensin Regulates Primate Ovulation Via Multiple Neurotensin Receptors. Endocrinology. 2025 Mar 24;166(5):bqaf041.
[2] Li C, Jiang N, Liu Y, et al. Toxoplasma sortilin interacts with secretory proteins and it is critical for parasite proliferation. Parasit Vectors. 2024 Mar 4;17(1):105.
[3] Yang W, Wu PF, Ma JX, et al. Sortilin promotes glioblastoma invasion and mesenchymal transition through GSK-3β/β-catenin/twist pathway. Cell Death Dis. 2019 Feb 27;10(3):208.
[4] Schrøder TJ, Christensen S, Lindberg S, et al. The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorg Med Chem Lett. 2014 Jan 1;24(1):177-80.
[5] Gao F, Griffin N, Faulkner S, et al. The Membrane Protein Sortilin Can Be Targeted to Inhibit Pancreatic Cancer Cell Invasion. Am J Pathol. 2020 Sep;190(9):1931-1942.
[6] Liu L, Jiang Y, Steinle JJ. Inhibition of sortilin reduces neuronal and vascular damage after ischemia/reperfusion through reduced inflammatory and autophagy actions in retinal Müller cells. Mol Vis. 2025 Oct 3;31:359-366.
[7] Rhost S, Hughes É, Harrison H, et al. Sortilin inhibition limits secretion-induced progranulin-dependent breast cancer progression and cancer stem cell expansion. Breast Cancer Res. 2018 Nov 20;20(1):137.
[8] Chen C, Li J, Matye DJ, et al. Hepatocyte sortilin 1 knockout and treatment with a sortilin 1 inhibitor reduced plasma cholesterol in Western diet-fed mice. J Lipid Res. 2019 Mar;60(3):539-549.
| Cell experiment [1]: | |
Cell lines | Pancreatic adenocarcinoma cell lines (PANC-1, MIA PaCa-2, PaCa-44) |
Preparation Method | Cancer cell lines were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% (v/v) fetal bovine serum and 1% (v/v) GlutaMAX Supplement in a humidified incubator at 37°C with 5% (v/v) CO₂. Cells were treated with the AF38469 (10μM) for 24 hours. |
Reaction Conditions | 10μM; 24 hours. |
Applications | AF38469 strongly reduced the adhesion and invasion of pancreatic cancer cells without affecting cell survival and viability. AF38469 also decreased the phosphorylation of focal adhesion kinase (FAK) at Tyr925. |
| Animal experiment [2]: | |
Animal models | NOD SCID gamma mice with MDA-MB 231-luc xenografts |
Preparation Method | MDA-MB 231-luc cells were injected subcutaneously into mice. Mice were given AF38469 (5-10μg/day/mouse) in their drinking water in parallel to repetitive injections of the active progranulin domain GRN A for 3 weeks. |
Dosage form | 5-10μg/day/mouse; in drinking water; daily for 3 weeks. |
Applications | AF38469 significantly reduced GRN A-induced lung metastasis and completely prevented cancer cell infiltration of the skin. |
References: | |
| Cas No. | 1531634-31-7 | SDF | |
| Canonical SMILES | O=C(NC1=CC=CC(C)=N1)C2=CC=C(C(F)(F)F)C=C2C(O)=O | ||
| Formula | C15H11F3N2O3 | M.Wt | 324.25 |
| Löslichkeit | DMSO : ≥ 43 mg/mL (132.61 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.084 mL | 15.4202 mL | 30.8404 mL |
| 5 mM | 616.8 μL | 3.084 mL | 6.1681 mL |
| 10 mM | 308.4 μL | 1.542 mL | 3.084 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)