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.
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- Pureté: 98.03%
- CAS No.: 2376928-82-2
- Formule: C34H41FN6O5
- Masse moléculaire:632.72
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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.
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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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CAS No. 2376928-82-2
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Appearance Solid
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Masse moléculaire 632.72
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 |
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| 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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