DS-1205b free base
Based on 1 Customer Validation
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 1855860-24-0
- Formula: C41H42FN5O7
- Molecular Weight:735.80
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
|
Axl |
Mer |
AXL 1.3 nM (IC50) |
MER 63 nM (IC50) |
TrkA 407 nM (IC50) |
Met 104 nM (IC50) |
DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM)[1].
DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NIH3T3-AXL cells
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Concentration:1, 10, 100, 1000, 10000 μM
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Incubation Time:2, 24 hours
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Result:Completely inhibited the phosphorylation of AXL at concentrations above 10 nM.
Slightly inhibited the phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks[1]
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Dosage:3.1, 6.3, 13, 25, 50 mg/kg
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Administration:P.o. twice daily for 5 days
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Result:Inhibited tumor growth by 39-94%.
Reduced the phosphorylation of both AXL and AKT in tumors.
Chemical Information
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CAS No. 1855860-24-0
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Appearance Solid
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Molecular Weight 735.80
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Formula C41H42FN5O7
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Color Off-white to yellow
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SMILES
O=C(C1=CN(CC2CCOCC2)C=C(C3=NC=C(C)C=C3)C1=O)NC4=CC=C(C5=CC(C6=CC=C(OC[C@@H]7OCCOC7)C(OC)=C6)=CN=C5N)C(F)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (67.95 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)
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 (3.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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.
Purity & Documentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
References
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 | 1.3591 mL | 6.7953 mL | 13.5906 mL | 33.9766 mL |
| 5 mM | 0.2718 mL | 1.3591 mL | 2.7181 mL | 6.7953 mL | |
| 10 mM | 0.1359 mL | 0.6795 mL | 1.3591 mL | 3.3977 mL | |
| 15 mM | 0.0906 mL | 0.4530 mL | 0.9060 mL | 2.2651 mL | |
| 20 mM | 0.0680 mL | 0.3398 mL | 0.6795 mL | 1.6988 mL | |
| 25 mM | 0.0544 mL | 0.2718 mL | 0.5436 mL | 1.3591 mL | |
| 30 mM | 0.0453 mL | 0.2265 mL | 0.4530 mL | 1.1326 mL | |
| 40 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8494 mL | |
| 50 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6795 mL | |
| 60 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL |
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