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HomeProduct name listRefametinib

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

Refametinib  Structural

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

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