AMG 900
Based on 5 publication(s) in Google Scholar
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
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- Purity: 98.82%
- CAS No.: 945595-80-2
- 화학식: C28H21N7OS
- 분자량:503.58
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보관: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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AMG 900
MoreAll Aurora Kinase Isoforms
More
Biological Activity
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Aurora A 5 nM (IC50) |
Aurora B 4 nM (IC50) |
Aurora C 1 nM (IC50) |
AMG 900 inhibits the enzyme activity of all 3 aurora kinase family members with IC50 values of 5 nM or less. In HeLa cells, AMG 900 inhibits autophosphorylation of aurora-A and -B in a concentration-dependent manner. Treatment of HCT116 cells with 50 nM of AMG 900 for 48 hours resulted in polyploidy and suppresses the formation of colonies after cell replating. AMG 900 inhibits cell proliferation, with EC50 values ranging from 0.7 to 5.3 nM. Importantly, 4 of these AMG 900-sensitive cell lines (HCT-15, MES-SA-Dx5, 769P, and SNU449) are resistant to paclitaxel and other anticancer agents. AMG 900 inhibits p-histone H3 or induced polyploidy across all the cell lines tested irrespective of P-gp or BCRP status with uniform potency (IC50 or EC50 values ranging from 2 to 3 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 945595-80-2
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Appearance Solid
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분자량 503.58
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화학식 C28H21N7OS
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Color Light yellow to yellow
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SMILES
CC1=CSC(C2=NN=C(C3=C2C=CC=C3)NC4=CC=C(C=C4)OC5=C(C=CC=N5)C6=CC=NC(N)=N6)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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J Chem Inf Model
2017 Nov 27;57(11):2699-2706. PMID: 29035535 -
Oncotarget
Molecular-genetic profiling and high-throughput in vitro drug screening in NUT midline carcinoma-an aggressive and fatal disease. [Abstract]2017 Dec 2;8(68):112313-112329. PMID: 29348827
용액&용해도
DMSO : ≥ 50 mg/mL (99.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (9.93 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.93 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Protocol
Different tumor cell lines including NCI-H460, MDA-MB231, MES-SA, NCI-H460 PTX, MDA-MB-231 PTX, MES-SA Dx5, and HCT-15. are treated with AMG 900 (0.5, 5.0, 50 nM) for 48 hours, washed twice with complete media, and cells are replated at a density of 5000 cells per well in drug-free complete media. Cells are grown until the DMSO control wells are confluent. Cells are stained with crystal violet dye, washed with distilled water, and imaged using a digital scanner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Female athymic nude mice of approximately 14 weeks of age are used. Mice are injected subcutaneously with 2×106 COLO 205 cells in 100 μL of 50% matrigel. Mice with established tumors (approximately 200 mm3) are assigned into experimental groups (n=10 per group) and administered a single oral dose of vehicle or AMG 900 at 3.75, 7.5, and 15 mg/kg. Three hours after treatment tissue specimens (bone marrow, tumor, and skin) are collected from individual mice for pharmacodynamic and histological analysis. Blood plasma samples (50 μL) are collected from individual mice to determine the concentration of AMG 900 using quantitative methods. Excised tumors are divided in half for parallel flow and imaging based cytometric analyses.
Rats[3]
Effect of food intake on AMG 900 PK is evaluated in male rats and male dogs following a single oral dose of AMG 900 at 5 mg/kg (rats) or 2 mg/kg (dogs) in the oral formulation mentioned above. For the rats, food is removed ~16 h before dosing for the fasted group, although the fed group had free access to standard laboratory rodent chow throughout the study; food is returned to rats in the fasted group 2 h post-dose. All the dogs are fasted for ~16 h before dosing. Each dog in the fed group receive 350 g of moist food 1 h prior to dosing, and any remaining food is removed after 1 h. All the dogs are fed 2 h post-dose.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Payton M, et al. Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res, 2010, 70(23), 9846-9854. [Content Brief]
[2]. Juan G, et al. AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues. J Transl Med. 2014 Nov 4;12:307. [Content Brief]
[3]. Huang L, et al. In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases. Xenobiotica. 2011 May;41(5):400-8. [Content Brief]
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 | 1.9858 mL | 9.9289 mL | 19.8578 mL | 49.6445 mL |
| 5 mM | 0.3972 mL | 1.9858 mL | 3.9716 mL | 9.9289 mL | |
| 10 mM | 0.1986 mL | 0.9929 mL | 1.9858 mL | 4.9645 mL | |
| 15 mM | 0.1324 mL | 0.6619 mL | 1.3239 mL | 3.3096 mL | |
| 20 mM | 0.0993 mL | 0.4964 mL | 0.9929 mL | 2.4822 mL | |
| 25 mM | 0.0794 mL | 0.3972 mL | 0.7943 mL | 1.9858 mL | |
| 30 mM | 0.0662 mL | 0.3310 mL | 0.6619 mL | 1.6548 mL | |
| 40 mM | 0.0496 mL | 0.2482 mL | 0.4964 mL | 1.2411 mL | |
| 50 mM | 0.0397 mL | 0.1986 mL | 0.3972 mL | 0.9929 mL | |
| 60 mM | 0.0331 mL | 0.1655 mL | 0.3310 mL | 0.8274 mL | |
| 80 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6206 mL |
AMG 900 Related Classifications
HY-13253 Related Classifications
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