Selumetinib sulfate

SKU: orb1908987

Description

Selumetinib sulfate (AZD6244 sulfate) is a potent, selective, and orally bioavailable MEK1/2 inhibitor. It is used in preclinical and clinical research for neurofibromatosis type 1, particularly for studying symptomatic, inoperable plexiform neurofibromas, based on in vitro and in vivo evidence.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 943332-08-9
• MW: 555.76
• Purity: 99.65% (May vary between batches)
• Formula: C₁₇H₁₇BrClFN₄O₇S
• SMILES: O=C(NOCCO)C1=CC2=C(N=CN2C)C(F)=C1NC3=CC=C(Br)C=C3Cl.O=S(=O)(O)O
• Target: MEK,Apoptosis
• Solubility: DMSO:40 mg/mL (71.97 mM);H2O:< 1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.6 mM)

Bioactivity

• Target IC50:
  purified MEK:12 nM
• In Vivo:
  In in vivo experiments, oral administration of 50 and 100 mg/kg Selumetinib sulfate dose-dependently reduced the growth rate of 4-1318 xenograft tumors; it also significantly inhibited the growth of 5-1318, 2-1318, 26-1004, and 29-1104 xenograft tumors at the 50 mg/kg dose. Oral administration of 10, 25, 50, or 100 mg/kg Selumetinib sulfate also inhibited ERK1/2 phosphorylation and reduced HT-29 xenograft tumor growth in nude mice. Meanwhile, tumor regression was observed in the BxPC3 xenograft model.
• In Vitro:
  Selumetinib sulfate (AZD6244) is a potent MEK inhibitor with an IC50 of 12 nM for purified MEK.Selumetinib sulfate is able to inhibit ERK1/2 phosphorylation in a variety of cancer cell lines with IC50s as low as 8 nM, both at basal and induced levels. In primary 2-1318 cells, Selumetinib sulfate induces growth arrest and apoptosis associated with ERK inactivation, resulting in reduced primary DNA synthesis and reduced cell viability over time and dose. In H-441 and H-1437 cells, Selumetinib sulfate (1 μM) exhibits antiproliferative effects by blocking the G0/G1 phase. In addition, Selumetinib sulfate inhibited the growth of various cell lines harboring B-Raf and Ras mutations, but had no significant effect on normal fibroblast cell lines.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ARRY-142886 sulfate, AZD6244 sulfate

Compound Identifiers

PubChem CID

16214875