AMG-458
Based on 1 Customer Validation
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.
For research use only. We do not sell to patients.
- Purity: 98.41%
- CAS No.: 913376-83-7
- Formula: C30H29N5O5
- Molecular Weight:539.58
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Storage: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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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
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VEGDR2 4100 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | IC50 |
120 nM
Compound: 17
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Inhibition of HGF-mediated c-Met phosphorylation in mouse CT26 cells
Inhibition of HGF-mediated c-Met phosphorylation in mouse CT26 cells
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[PMID: 18553959] |
| HUVEC | IC50 |
690 nM
Compound: 17
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Inhibition VEGFR2-mediated survival of HUVEC
Inhibition VEGFR2-mediated survival of HUVEC
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[PMID: 18553959] |
| NIH3T3 | ED50 |
12 mg/kg
Compound: 17
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Antitumor activity in TPR-Met expressing human NIH3T3 cells xenografted in po dosed mouse assessed as tumor growth inhibition after 24 hrs
Antitumor activity in TPR-Met expressing human NIH3T3 cells xenografted in po dosed mouse assessed as tumor growth inhibition after 24 hrs
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[PMID: 18553959] |
| PC-3 | IC50 |
60 nM
Compound: 17
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Inhibition of HGF-mediated c-Met phosphorylation in human PC3 cells
Inhibition of HGF-mediated c-Met phosphorylation in human PC3 cells
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[PMID: 18553959] |
| PC-3 | IC50 |
60.1 nM
Compound: 59e, AMG-458
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Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
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[PMID: 22320327] |
| U-87MG ATCC | ED50 |
16 mg/kg
Compound: 17
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Antitumor activity in human U87MG cells xenografted orally dosed CD1 NU/NU mouse assessed as tumor growth inhibition after 14 days
Antitumor activity in human U87MG cells xenografted orally dosed CD1 NU/NU mouse assessed as tumor growth inhibition after 14 days
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[PMID: 18553959] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model[1].
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Dosage:10, 30, 100 mg/kg.
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Administration:Orally q.d. or b.i.d.
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Result:With an ED50 of ∼12 mg/kg and an ED90 of ∼ 34 mg/kg in NIH-3T3/TPR-Met model.
With an ED50 of ∼16 mg/kg and an ED90 of ∼ 59 mg/kg in U-87 MG human glioblastoma xenograft model.
Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight.
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Animal Model:Balb/c mouse and SD rat[1].
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Dosage:1 mg/kg (Pharmacokinetic Analysis).
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Administration:IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid).
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Result:Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, Vss (L/kg) values of 0.31 and 0.62, t1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.
Chemical Information
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CAS No. 913376-83-7
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Appearance Solid
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Molecular Weight 539.58
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Formula C30H29N5O5
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Color Off-white to pink
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SMILES
O=C(C1=C(C)N(CC(C)(O)C)N(C2=CC=CC=C2)C1=O)NC3=NC=C(OC4=CC=NC5=CC(OC)=CC=C45)C=C3
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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 (92.66 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)
Purity & Documentation
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Data Sheet (275 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
[1]. Longbin Liu, et al. Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem. 2008 Jul 10;51(13):3688-91. [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, 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 | 1.8533 mL | 9.2665 mL | 18.5329 mL | 46.3323 mL |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7066 mL | 9.2665 mL | |
| 10 mM | 0.1853 mL | 0.9266 mL | 1.8533 mL | 4.6332 mL | |
| 15 mM | 0.1236 mL | 0.6178 mL | 1.2355 mL | 3.0888 mL | |
| 20 mM | 0.0927 mL | 0.4633 mL | 0.9266 mL | 2.3166 mL | |
| 25 mM | 0.0741 mL | 0.3707 mL | 0.7413 mL | 1.8533 mL | |
| 30 mM | 0.0618 mL | 0.3089 mL | 0.6178 mL | 1.5444 mL | |
| 40 mM | 0.0463 mL | 0.2317 mL | 0.4633 mL | 1.1583 mL | |
| 50 mM | 0.0371 mL | 0.1853 mL | 0.3707 mL | 0.9266 mL | |
| 60 mM | 0.0309 mL | 0.1544 mL | 0.3089 mL | 0.7722 mL | |
| 80 mM | 0.0232 mL | 0.1158 mL | 0.2317 mL | 0.5792 mL |
AMG-458 Related Classifications
HY-14723 Related Classifications
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