Refametinib
Refametinib Basic information
- Product Name:
- Refametinib
- 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
- Product Categories:
-
- Inhibitors
- Mol File:
- 923032-37-5.mol
Refametinib 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)
- color
- White to yellow
Refametinib 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.
in vivo
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, highly selective inhibitor of MEK1/2, which is active in human tumor xenograft models and is well tolerated within the therapeutic exposure range in animals[1].
target
MEK1
IC 50
MEK1: 19 nM (IC50); MEK2: 47 nM (IC50)
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.
Refametinib Supplier
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