SML3800

Selumetinib

≥98% (HPLC)

• Synonym(s): 5-((4-Bromo-2-chlorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide, 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, ARRY 142886, ARRY-142886, ARRY142886, AZD 6244, AZD-6244, AZD6244
• Empirical Formula (Hill Notation): C₁₇H₁₅BrClFN₄O₃
• CAS Number: 606143-52-6
• Molecular Weight: 457.68
• MDL number: MFCD11977472
• UNSPSC Code: 12352200
• NACRES: NA.21

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (Warmed)
• storage temp.: 2-8°C

Description

Biochem/physiol Actions

Selumetinib (ARRY-142886; AZD6244) is an orally active, potent and selective MEK1/2 inhibitor (MEK1 IC50 = 14 nM; <20% inhibition of >40 other kinases at 10 µM) that effectively downregulates cellular ERK1/2 phosphorylation levels (IC50 <40 nM post 1h incubation using 5 different cell lines). Selumetinib inhibits MEK1/2-dependent proliferations in cancer cultures (IC50 in nM = 59/Malme-3M, 93/SK-MEL-28, 175/HT-29, 200/SK-MEL-2, 473/MIA PaCa-2) and exhibits anti-tumor efficacy in mice in vivo (10-100 mg/kg p.o. b.i.d.; BxPC3 & HT-29 xenograft models).

Safety Information

• pictograms: GHS08,GHS07
• signalword: Warning
• hcodes: H302,H317,H361f,H373,H413
• pcodes: P202 - P273 - P280 - P301 + P312 - P302 + P352 - P308 + P313
• Hazard Classifications: Acute Tox. 4 Oral - Aquatic Chronic 4 - Repr. 2 - Skin Sens. 1 - STOT RE 2
• target_organs: Gastrointestinal tract,Eyes,Urinary tract
• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable