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

Safety Information

HS Code 

2935909099

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.

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.

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