Refametinib
Synonym(s):(10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H.8,4-(metheno)pyrazolo[4,3.h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile;PF-06463922;PF-6463922
- CAS NO.：923032-37-5
- Empirical Formula: C19H20F3IN2O5S
- Molecular Weight: 572.34
- MDL number: MFCD18633256
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 23:02:33
What is Refametinib ?
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].
The Uses of Refametinib
Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2. Potent MEK inhibitor.
What are the applications of Application
BAY 869766 is a non–ATP-competitive inhibitor of MEK-1 and MEK-2.
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.
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.
Properties of Refametinib
| 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 |
Safety information for Refametinib
Computed Descriptors for Refametinib
New Products
Tert-butyl bis(2-chloroethyl)carbamate 4-Methylphenylacetic acid N-Boc-D-alaninol N-BOC-D/L-ALANINOL N-octanoyl benzotriazole 3-Morpholino-1-(4-nitrophenyl)-5,6-dihydropyridin- 2(1H)-one Furan-2,5-Dicarboxylic Acid DIETHYL AMINOMALONATE HYDROCHLORIDE 1,1’-CARBONYLDIIMIDAZOLE R-2-BENZYLOXY PROPIONIC ACID 1,1’-CARBONYLDI (1,2-4 TRIAZOLE) N-METHYL INDAZOLE-3-CARBOXYLIC ACID (2-Hydroxyphenyl)acetonitrile 4-Bromopyrazole 5-BROMO-2CYANO PYRIDINE 5,6-Dimethoxyindanone 5-broMo-2-chloro-N-cyclopentylpyriMidin-4-aMine 2-(Cyanocyclohexyl)acetic acid 4-methoxy-3,5-dinitropyridine 1-(4-(aminomethyl)benzyl)urea hydrochloride 2-aminopropyl benzoate hydrochloride diethyl 2-(2-((tertbutoxycarbonyl)amino) ethyl)malonate tert-butyl 4- (ureidomethyl)benzylcarbamate Ethyl-2-chloro((4-methoxyphenyl)hydrazono)acetateRelated products of tetrahydrofuran
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