AXL-IN-13
Based on 1 Customer Validation
AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.79%
- No. CAS: 2376928-82-2
- Fòrmula: C34H41FN6O5
- Peso molecular:632.72
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Axl |
PDGFRβ 2.3 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
4.7 nM
Compound: 6li
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Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 36358010] |
In Vitro
AXL-IN-13 (compound 6li) inhibits Ba/F3-TEL-AXL cell proliferation with an IC50 of 4.7 nM (determined by ELISA)[1].
AXL-IN-13 also shopws binding affinities against CSF1R, FLT1/3/4, KLT, PDGFRB, TIE2[1].
AXL-IN-13 (0-500 nM, 6 h) inhibits the phosphorylation of AXL in MDA-MB-231 and 4T1 cells[1].
AXL-IN-13 (0-3 μM, 3 days) blocks EMT induced by TGF-β1 (10 ng/mL) in MDA-MB-231 cells[1].
AXL-IN-13 (0-3 μM, 24 h) suppresses MDA-MB-231 cell migration and invasion induced by TGF-β1 (10 ng/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 0.11, 0.33, 1, 3 μM.
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Incubation Time:3 days
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Result:Restored the protein levels of E-cadherin and N-cadherin to control levels.
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Cell Line:MDA-MB-231 cell
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Concentration:0, 0.11, 0.33, 1, 3 μM.
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Incubation Time:24 h
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Result:Inhibited cell migration at 1 and 3 μM.
Inhibited the invasion of MDA-MB-231 cells by 22.6, 34.8, 56.5, and 70.4% at the concentrations of 0.11, 0.33, 1.0, and 3.0 μM, respectively.
In Vivo
AXL-IN-13 (25 mg/kg, p.o.) displays reasonable PK profiles with an AUC of 8410.21 ng/mL•h, a T1/2 value of 4.22 h, and an oral bioavailability (F) of 14.4%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft model derived from highly metastatic 4T1 cells.[1]
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Dosage:50 or 100 mg/kg
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Administration:Oral administration (p.o.)
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Result:Suppressed 4T1 tumor growth with a tumor growth inhibition (TGI) of 78.0 and 95.9% at 50 and 100 mg/kg, respectively.
Inhibited the phosphorylation of AXL.
Showed that liver is one of the most common sites of breast cancer metastasis.
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Animal Model:Rats[1]
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Dosage:5 mg/kg (i.v.), 25 mg/kg (p.o.)
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Administration:Intravenous injection (i.v.), oral administration (p.o.)
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Result:Pharmacokinetic parameters of AXL-IN-13 (Compound 6li).
parameters T1/2 (h) Cmax (ng/mL) AUClast F (%) 5 mg/kg (i.v.) 3.31 12280.44 11684.24 25 mg/kg (p.o.) 4.22 887.75 8410.21 14.4
Chemical Information
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No. CAS 2376928-82-2
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Appearance Solid
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Peso molecular 632.72
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Fòrmula C34H41FN6O5
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Color Off-white to light yellow
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SMILES
COC1=C(C=C(C2=C1)N=CC=C2OC3=C(C=C(C=C3)NC4=NN(C=C4C(NC5CCCCC5)=O)C)F)OCCCN6CCOCC6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (158.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.95 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.95 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Scratch/Wound-Healing Migration Assay
The scratch/wound-healing migration assay measures collective migration of adherent cells into an experimentally created cell-free gap in a confluent monolayer. The readout is generated by imaging the gap immediately after scratching and at later time points, then quantifying reduction in wound area, wound width, or percentage closure as cells move into the denuded region. Gap closure reflects cell migration but may also include cell proliferation, so interpretation should distinguish migration-focused conditions from proliferation-driven closure when possible, such as by using short assay windows, serum-controlled conditions, cell counting, or proliferation controls reported in published protocols.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Chemotaxis Gradient Chamber Assay 1
The chemotaxis gradient chamber assay is based on the principle of observing directional cell migration in response to a stable, linear or quasi-linear concentration gradient of a chemoattractant formed between two fluid reservoirs separated by a narrow observation chamber. Cells placed within the chamber respond to the gradient by polarized movement toward higher chemoattractant concentrations, allowing quantification of chemotactic behavior in real time under microscopy. The classic Zigmond chamber design enables simultaneous visualization of gradient formation and individual cell trajectories, making it suitable for studying leukocyte chemotaxis and other motile cell types in vitro.
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Under-Agarose Cell Migration Assay
The under-agarose cell migration assay is a classical in vitro chemotaxis method designed to evaluate directed cell movement through a semi-solid agarose matrix toward soluble chemoattractant gradients, enabling visualization and quantification of leukocyte or motile cell migration in a confined 2D-like environment. In this system, cells and chemoattractants are placed in separate wells cut into an agarose gel, allowing diffusion-driven gradient formation that guides directional migration, which is typically assessed by measuring migration distance, cell morphology changes, and accumulation toward the chemoattractant source. This assay has been widely used to study neutrophil and leukocyte chemotaxis as a simple alternative to filter-based migration systems and allows direct microscopic observation of migrating cells under near-physiological confinement conditions.
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Neural Crest/Neuronal Cell Migration Explant Assay
Neural crest (NC) and neuronal cell migration explant assays are in vitro systems in which neural tube-derived tissues are cultured to allow premigratory or newly emigrated neural crest cells to undergo epithelial-to-mesenchymal transition (EMT), migrate away from the explant, and form a measurable radial outgrowth that reflects migratory capacity and environmental responsiveness. These assays typically quantify migration by measuring the expansion of cell outgrowth from neural tube or neural plate border explants over time, often comparing early and later timepoints to derive a migration index such as a radius ratio, which reflects net cell dispersal from the explant core. Neural tube explant cultures preserve key aspects of neural crest behavior, including EMT, migration, and early differentiation, making them suitable for assessing intrinsic migratory ability and extrinsic cue dependence. However, studies emphasize that migratory outgrowth from neural tube explants may include non-n
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Transwell/Boyden Chamber Migration Assay
The Transwell/Boyden chamber migration assay measures cell movement through a porous membrane separating an upper and lower chamber, usually after a chemoattractant gradient is established by placing cells in the upper chamber and chemoattractant-containing medium in the lower chamber. The readout is generated by quantifying cells that traverse the membrane and appear on the lower membrane surface or in the lower chamber, depending on whether the cell type is adherent or non-adherent. This assay reflects chemotactic or haptotactic migration rather than matrix invasion unless an extracellular-matrix barrier is added to the membrane.
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3D Collagen/Hydrogel Matrix Migration Assay
The 3D collagen/hydrogel matrix migration assay is based on embedding cells within or on top of a fibrillar collagen type I-rich three-dimensional matrix to model in vivo-like extracellular matrix (ECM) architecture, enabling analysis of cell migration through a physically and biochemically relevant scaffold. In contrast to 2D migration systems, cells in 3D matrices interact with fibrillar collagen networks, requiring coordinated adhesion remodeling and proteolytic or non-proteolytic deformation mechanisms to move through confined spaces, thereby providing a more physiologically relevant readout of invasive and migratory behavior in tissue-like environments. Cell movement in 3D collagen matrices is typically quantified by tracking single-cell trajectories, invasion depth, or matrix penetration over time, reflecting combined effects of cytoskeletal dynamics, cell-ECM adhesion turnover, and ECM remodeling. These systems are widely used to study tumor cell invasion and stromal cell motili
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Cell-Exclusion Zone Migration Assay
The Cell-Exclusion Zone (CEZ) migration assay is an in vitro 2D cell migration method in which a defined cell-free area is created using removable physical barriers such as silicone stoppers, allowing cells to be seeded around the barrier and subsequently migrate into the cleared zone after barrier removal. This approach enables quantification of collective cell migration by monitoring repopulation of the initially cell-free region over time using microscopy-based imaging. Compared with scratch-based wound healing assays, barrier-based exclusion methods are designed to avoid mechanical damage to the extracellular matrix and reduce injury-induced effects on boundary cells, thereby improving interpretability of migration behavior in vitro. The assay readout is typically the progressive reduction in the cell-free area or the number of cells invading the exclusion zone, reflecting coordinated cell motility relevant to physiological processes such as wound healing, epithelial repair, and ca
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Chemotaxis Gradient Chamber Assay 2
Chemotaxis gradient chamber assays measure directional cell migration in response to a soluble chemical gradient by imaging cells as they move across a defined observation region; the readout is generated from time-lapse cell trajectories, displacement toward the gradient, forward migration index, trajectory plots, rose/polar plots, and statistical tests of non-random directionality. The Dunn chamber is a direct-viewing glass chamber in which cells migrate across a bridge between control and chemoattractant wells, allowing observation of cells in a linear concentration gradient; related direct-viewing formats include the Insall chamber, which supports defined unidirectional gradients and high numerical-aperture microscopy, and the μ-Slide Chemotaxis chamber, which supports long-term live-cell imaging and gradient characterization with fluorescent dye.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5805 mL | 7.9024 mL | 15.8048 mL | 39.5120 mL |
| 5 mM | 0.3161 mL | 1.5805 mL | 3.1610 mL | 7.9024 mL | |
| 10 mM | 0.1580 mL | 0.7902 mL | 1.5805 mL | 3.9512 mL | |
| 15 mM | 0.1054 mL | 0.5268 mL | 1.0537 mL | 2.6341 mL | |
| 20 mM | 0.0790 mL | 0.3951 mL | 0.7902 mL | 1.9756 mL | |
| 25 mM | 0.0632 mL | 0.3161 mL | 0.6322 mL | 1.5805 mL | |
| 30 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL | 1.3171 mL | |
| 40 mM | 0.0395 mL | 0.1976 mL | 0.3951 mL | 0.9878 mL | |
| 50 mM | 0.0316 mL | 0.1580 mL | 0.3161 mL | 0.7902 mL | |
| 60 mM | 0.0263 mL | 0.1317 mL | 0.2634 mL | 0.6585 mL | |
| 80 mM | 0.0198 mL | 0.0988 mL | 0.1976 mL | 0.4939 mL | |
| 100 mM | 0.0158 mL | 0.0790 mL | 0.1580 mL | 0.3951 mL |
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