AM-9022
Based on 1 Customer Validation
AM-9022 is an orally active, potent, selective KIF18A inhibitor that can be used for research on cancer.
For research use only. We do not sell to patients.
- Purity: 99.53%
- CAS No.: 2446872-46-2
- Formula: C27H36F2N6O4S
- Molecular Weight:578.67
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Storage:Powder -20°C, 3 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
AM-9022 (10-5-6 μM, 96 h) suppresses KIF18A-inhibitor sensitive cells growth with mean EC50value of 0.045 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KIF18A-inhibitor sensitive (BT-549, HCC-1937, HCC-1806, MDA-MB-157, OVCAR-3), KIF18A-inhibitor insensitive (CAL-51, MCF-7, MDA-MB-453, ZR-75-1, OVCAR-5)
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Concentration:10-5-6 μM
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Incubation Time:96 h
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Result:BT-549, HCC-1937, HCC-1806, MDA-MB-157, OVCAR-3 were sensitive to the compound with mean half-maximum effective concentration (EC50) value of 0.045 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice were injected with OVCAR-3 cells (5 x 106) subcutaneously in the right flank. Femal CB.17 SCID mice were injected with JIMT-1 cells (1.0 × 107) subcutaneously in the right flank) (6-8 weeks)[1]
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Dosage:30 mg/kg (OVCAR-3 CDX tumors mice); 30, 100 mg/kg (JIMT-1 tumors mice)
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Administration:Oral gavage (p.o.); daily for 18 days or 21 days
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Result:Increased pH3 mitotic marker levels in OVCAR-3 tumors by 3.4-fold, with higher compound exposure in tumors relative to plasma in OVCAR-3 CDX tumors mice.
Inhibited tumor growth, with evidence of tumor regression (TR) (95% TR, six of ten tumor-free mice) and no body weight loss in OVCAR-3 CDX tumors mice.
Inhibited tumor growth with evidence of TR (16% and 94% TR, respectively) at well-tolerated doses in JIMT-1 tumors mice.
The plasma AUC value at 30 mg/kg was 3.7-fold higher in the JIMT-1 model relative to the OVCAR-3 model.
Chemical Information
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CAS No. 2446872-46-2
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Appearance Solid
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Molecular Weight 578.67
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Formula C27H36F2N6O4S
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Color White to off-white
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SMILES
O=C(C1=CC=C(NS([C@H](C)CO)(=O)=O)C=C1N2CCC3(CC3)CC2)NC4=CC(C)=NC(N5CCC(F)(F)CC5)=N4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (86.41 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: ≥ 1.25 mg/mL (2.16 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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 | 1.7281 mL | 8.6405 mL | 17.2810 mL | 43.2025 mL |
| 5 mM | 0.3456 mL | 1.7281 mL | 3.4562 mL | 8.6405 mL | |
| 10 mM | 0.1728 mL | 0.8641 mL | 1.7281 mL | 4.3203 mL | |
| 15 mM | 0.1152 mL | 0.5760 mL | 1.1521 mL | 2.8802 mL | |
| 20 mM | 0.0864 mL | 0.4320 mL | 0.8641 mL | 2.1601 mL | |
| 25 mM | 0.0691 mL | 0.3456 mL | 0.6912 mL | 1.7281 mL | |
| 30 mM | 0.0576 mL | 0.2880 mL | 0.5760 mL | 1.4401 mL | |
| 40 mM | 0.0432 mL | 0.2160 mL | 0.4320 mL | 1.0801 mL | |
| 50 mM | 0.0346 mL | 0.1728 mL | 0.3456 mL | 0.8641 mL | |
| 60 mM | 0.0288 mL | 0.1440 mL | 0.2880 mL | 0.7200 mL | |
| 80 mM | 0.0216 mL | 0.1080 mL | 0.2160 mL | 0.5400 mL |
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