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AMG 208 (AMG-208) is a novel, highly potent and selective triazolopyridazine-based small molecule inhibitor of c-Met with potential antineoplastic activity. Its IC50 value for c-Met inhibition is 9 nM. Hepatocyte growth factor, the ligand for the oncogene MET, activates it. Numerous cancer types have been found to have a disrupted or dysregulated c-Met signaling pathway.
| Targets |
CYP3A4 (IC50 = 32 μM); c-Met (IC50 = 9 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
AMG-208, whose IC50 is 9.3 nM, is a strong small-molecule c-Met inhibitor.
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| Cell Assay |
AMG-208, whose IC50 is 9.3 nM, is a strong small-molecule c-Met inhibitor.AMG-208 exhibits a strong time-dependent inhibition of CYP3A4 metabolic activity with a 4.1 μM IC50 after 30 minutes of pre-incubation with human liver microsomes. This is an eight-fold reduction from the IC50 (32 μM) without preincubation.
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| Animal Protocol |
Male Sprague-Dawley rats
≤2 mg/kg Administered via i.v. and p.o. |
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| References |
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| Additional Infomation |
AMG-208 is a member of the class of quinolines that is 7-methoxyquinoline substituted at position 4 by a (6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy group. AMG exhibits antitumour activity, particularly in prostate cancer. It has a role as a c-Met tyrosine kinase inhibitor and an antineoplastic agent. It is a member of quinolines, an aromatic ether and a triazolopyridazine.
AMG-208 has been used in trials studying the treatment of Cancer, Tumors, Oncology, Prostate Cancer, and Oncology Patients, among others. c-Met Inhibitor AMG 208 is a selective small-molecule inhibitor of the proto-oncogene c-Met with potential antineoplastic activity. c-Met inhibitor AMG 208 inhibits the ligand-dependent and ligand-independent activation of c-Met, inhibiting its tyrosine kinase activity, which may result in cell growth inhibition in tumors that overexpress c-Met. C-Met encodes the hepatocyte growth factor receptor tyrosine kinase, plays an important role in epithelial cell proliferation and has been shown to be overexpressed in a variety of cancers. |
| Molecular Formula |
C22H17N5O2
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| Molecular Weight |
383.4
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| Exact Mass |
383.138
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| Elemental Analysis |
C, 68.92; H, 4.47; N, 18.27; O, 8.35
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| CAS # |
1002304-34-8
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| Related CAS # |
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| PubChem CID |
24864821
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.696
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| LogP |
4.02
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
531
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C2C(OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5)=CC=NC2=C1
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| InChi Key |
HEAIZQNMNCHNFD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H17N5O2/c1-28-16-7-8-17-19(13-16)23-12-11-20(17)29-14-22-25-24-21-10-9-18(26-27(21)22)15-5-3-2-4-6-15/h2-13H,14H2,1H3
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| Chemical Name |
7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline
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| Synonyms |
AMG 208; AMG-208; AMG208
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL | |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02420587 | Withdrawn | Drug: AMG 208 Behavioral: Questionnaire |
Prostate Cancer | M.D. Anderson Cancer Center | October 2014 | Phase 2 |
| NCT00813384 | Completed | Drug: AMG 208 | Cancer Leukemia Oncology |
Amgen | December 2008 | Phase 1 |
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