Chemical Property of Selumetinib
Chemical Property:
- Appearance/Colour:White or pale white solid.
- PKA:14.20±0.10(Predicted)
- PSA：88.41000
- Density:1.692 g/cm3
- LogP:3.98950
- Storage Temp.:-20°
- Solubility.:Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 2 mg/ml)
- XLogP3:3.6
- Hydrogen Bond Donor Count:3
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:6
- Exact Mass:456.00001
- Heavy Atom Count:27
- Complexity:523
- Purity/Quality:
-
99% *data from raw suppliers
Selumetinib *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Genetic Disorder Agents, Antineoplastic Agents
- Canonical SMILES:CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO
- Recent ClinicalTrials:Selumetinib in Chinese Paediatric With Post-operative NF1-PNs, PhaseⅡ, Double-Blinded, Placebo-Controlled Study
- Recent EU Clinical Trials:A Phase I/II, Single-Arm, Open label Study to Evaluate the Pharmacokinetics, Safety/Tolerability and Efficacy of the Selumetinib Granule Formulation in Children Aged ≥ 1 to < 7 Years with Neurofibromatosis Type 1 (NF1) Related Symptomatic, Inoperable Plexiform Neurofibromas (PN) (SPRINKLE)
- Recent NIPH Clinical Trials:A Phase III, Multicentre, International Study With a Parallel, Randomised, Double-blind, Placebo-controlled, 2 Arm Design to Assess the Efficacy and Safety of Selumetinib in Adult Participants With NF1 Who Have Symptomatic, Inoperable Plexiform Neurofibromas
-
Description
Selumetinib (AZD6244; ARRY-142886) is an oral MEK inhibitor. In a randomized trial, NSCLC patients with wild-type KRAS were randomized to erlotinib
alone or combination therapy with selumetinib, while mutant KRAS patients were
randomized to selumetinib alone or combination therapy. The primary end points
were PFS for the KRAS wild-type cohort and objective response rate (ORR) for the
KRAS mutant cohort. Results were not impressive, with no PFS difference in the
KRAS wild-type arm (2.4 vs. 2.1?months) and no ORR difference in the KRASmutated subgroup (0% vs. 10%). A planned trial of selumetinib in combination
with the anti-PD-L1 antibody durvalumab has since been suspended (NCT03004105).
-
Uses
It is a tight-binding, uncompetitive inhibitor of mitogen-activated protein kinase kinases (MEK) 1 and 2 currently in clinical development. It is useful as biomarker in human lung cancer cell. Potent MEK inhibitor. It is a tight-binding, uncompetitive inhibitor of mitogen-activated protein kinase kinases (MEK) 1 and 2 currently in clinical development.
