CRT0273750
Based on 1 Customer Validation
CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.87%
- CAS No.: 1979939-16-6
- Formule: C25H22ClF3N4O2
- Masse moléculaire:502.92
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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
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Activité biologique
IC50: 0.014 μM (plasma CRA)
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Cell Line
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Type | Value | Description | References |
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| 4T1 | EC50 |
0.025 μM
Compound: 9v; CRT0273750
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Inhibition of human recombinant ATX/LPC 18:1-mediated mouse 4T1 cell migration after overnight incubation by Transwell assay
Inhibition of human recombinant ATX/LPC 18:1-mediated mouse 4T1 cell migration after overnight incubation by Transwell assay
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[PMID: 27780639] |
CRT0273750 shows high potency in both the biochemical (IC50 = 0.01 μM) and plasma choline release assay(IC50 = 0.014 μM)[1].
CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CRT0273750 (10 mg/kg; oral administration) treatment shows the Cmax, AUC and t1/2 values of 3.8 μM, 3.2 μM.h and 1.4 h, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:1 mg/kg
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Administration:I.v.
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Result:Had a moderate blood clearance.
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Animal Model:Balb-c nu/nu mice[1]
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Dosage:10, 30 and 100 mg/kg
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Administration:Oral administration (Pharmacokinetic Analysis)
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Result:The Cmaxs were 3.8, 10.9 and 18.1 µM, respectively.
The AUCs were 3.2, 15.2 and 59.3 µM.h, respectively.
The t1/2s were 1.4, 0.9 and 1.3 h, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1979939-16-6
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Appearance Solid
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Masse moléculaire 502.92
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Formule C25H22ClF3N4O2
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Color White to off-white
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SMILES
FC(F)(OC1=CC=C(C=C1)CN2C(CCC(N[C@H](C3=CC=C(Cl)C=C3)C)=O)=NC4=CC=CN=C42)F
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Synonyms
IOA-289
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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
DMSO : 175 mg/mL (347.97 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 2.08 mg/mL (4.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9884 mL | 9.9419 mL | 19.8839 mL | 49.7097 mL |
| 5 mM | 0.3977 mL | 1.9884 mL | 3.9768 mL | 9.9419 mL | |
| 10 mM | 0.1988 mL | 0.9942 mL | 1.9884 mL | 4.9710 mL | |
| 15 mM | 0.1326 mL | 0.6628 mL | 1.3256 mL | 3.3140 mL | |
| 20 mM | 0.0994 mL | 0.4971 mL | 0.9942 mL | 2.4855 mL | |
| 25 mM | 0.0795 mL | 0.3977 mL | 0.7954 mL | 1.9884 mL | |
| 30 mM | 0.0663 mL | 0.3314 mL | 0.6628 mL | 1.6570 mL | |
| 40 mM | 0.0497 mL | 0.2485 mL | 0.4971 mL | 1.2427 mL | |
| 50 mM | 0.0398 mL | 0.1988 mL | 0.3977 mL | 0.9942 mL | |
| 60 mM | 0.0331 mL | 0.1657 mL | 0.3314 mL | 0.8285 mL | |
| 80 mM | 0.0249 mL | 0.1243 mL | 0.2485 mL | 0.6214 mL | |
| 100 mM | 0.0199 mL | 0.0994 mL | 0.1988 mL | 0.4971 mL |
CRT0273750 Related Classifications
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