| Identification | Back Directory | [Name]
RDEA119 | [CAS]
923032-37-5 | [Synonyms]
RDEA119
CS-2434
Lorlatinib
BAY-869766
RefaMetinib
BAY 8697661
RDEA119 USP/EP/BP
REFAMETINIB(RDEA119)
RDEA-119 (BAY-869766)
RefaMetinib/BAY 8697661
BAY 869766; BAY 86-9766
Refametinib (BAY86-9766)
BAY 869766;BAY 86-97661;RDEA119
N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide
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
Cyclopropanesulfonamide, N-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]- | [Molecular Formula]
C19H20F3IN2O5S | [MDL Number]
MFCD18633256 | [MOL File]
923032-37-5.mol | [Molecular Weight]
572.34 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
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| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|