APS6-45
Based on 1 Customer Validation
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 2188236-41-9
- Formula: C23H16F8N4O3
- Molecular Weight:548.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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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GPCR/G Protein Compound Library
HY-L006
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Immunology/Inflammation Compound Library
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Kinase Inhibitor Library
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MAPK Compound Library
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Biological Activity
APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay[1].
APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice[1].
APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 µM) and AUC0-24 (123.7 µM•h) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (6 weeks) are implanted with TT cells[1]
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Dosage:10 mg/kg
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Administration:P.o. daily for 30 days
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Result:Led to partial or complete responses in 75% and was well tolerated.
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Animal Model:Male ICR mice (6 weeks of age)[1]
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Dosage:20 mg/kg (Pharmacokinetic Analysis)
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Administration:A single p.o.
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Result:T1/2=5.6 h, Cmax=9.7 µM, AUC0-24=123.7 µM•h.
Chemical Information
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CAS No. 2188236-41-9
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Appearance Solid
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Molecular Weight 548.39
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Formula C23H16F8N4O3
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Color Off-white to light yellow
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SMILES
O=C(C1=NC=CC(OC2=CC=C(C=C2)NC(NC3=CC(C(F)(C(F)(F)F)C(F)(F)F)=CC=C3F)=O)=C1)NC
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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 2 years -20°C 1 year
Solvent & Solubility
DMSO : 250 mg/mL (455.88 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
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 (270 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8235 mL | 9.1176 mL | 18.2352 mL | 45.5880 mL |
| 5 mM | 0.3647 mL | 1.8235 mL | 3.6470 mL | 9.1176 mL | |
| 10 mM | 0.1824 mL | 0.9118 mL | 1.8235 mL | 4.5588 mL | |
| 15 mM | 0.1216 mL | 0.6078 mL | 1.2157 mL | 3.0392 mL | |
| 20 mM | 0.0912 mL | 0.4559 mL | 0.9118 mL | 2.2794 mL | |
| 25 mM | 0.0729 mL | 0.3647 mL | 0.7294 mL | 1.8235 mL | |
| 30 mM | 0.0608 mL | 0.3039 mL | 0.6078 mL | 1.5196 mL | |
| 40 mM | 0.0456 mL | 0.2279 mL | 0.4559 mL | 1.1397 mL | |
| 50 mM | 0.0365 mL | 0.1824 mL | 0.3647 mL | 0.9118 mL | |
| 60 mM | 0.0304 mL | 0.1520 mL | 0.3039 mL | 0.7598 mL | |
| 80 mM | 0.0228 mL | 0.1140 mL | 0.2279 mL | 0.5698 mL | |
| 100 mM | 0.0182 mL | 0.0912 mL | 0.1824 mL | 0.4559 mL |
APS6-45 Related Classifications
HY-124944 Related Classifications
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