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| | RDEA119 Basic information |
| Product Name: | RDEA119 | | Synonyms: | RDEA119;BAY-869766;RefaMetinib;RDEA-119 (BAY-869766);BAY 8697661;RefaMetinib/BAY 8697661;N-[3,4-Difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropanesulfonamide;(S)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide | | CAS: | 923032-37-5 | | MF: | C19H20F3IN2O5S | | MW: | 572.34 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 923032-37-5.mol |  |
| | RDEA119 Chemical Properties |
| Boiling point | 566.9±60.0 °C(Predicted) | | density | 1.82±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; ≥151.8 mg/mL in DMSO; ≥90.2 mg/mL in EtOH | | form | Powder | | pka | 15.54±0.20(Predicted) |
| | RDEA119 Usage And Synthesis |
| Description | Lorlatinib (PF-06463922, Pfizer Oncology, Groton, CT, USA) is an oral TKI that
targets both ALK and ROS1 with high affinity and good CNS penetration [91]. | | Uses | Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2. Potent MEK inhibitor. | | Clinical Use | Lorlatinib is the sole third-generation ALK inhibitor at this time; it is approved for
ALK-positive NSCLC patients who progressed on at least two ALK inhibitors with
one being crizotinib or who progressed on alectinib or ceritinib if either is used in
the frontline setting. | | target | MEK1 | | references | [1] iverson c, larson g, lai c, et al. rdea119/bay 869766: a potent, selective, allosteric inhibitor of mek1/2 for the treatment of cancer. cancer research, 2009, 69(17): 6839-6847. |
| | RDEA119 Preparation Products And Raw materials |
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