SML3800

Selumetinib

≥98% (HPLC)

• 別名: 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
• 実験式（ヒル表記法）: C₁₇H₁₅BrClFN₄O₃
• CAS番号: 606143-52-6
• 分子量: 457.68
• MDL番号: MFCD11977472
• UNSPSCコード: 12352200
• NACRES: NA.21

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear (Warmed)
• 保管温度: 2-8°C
• SMILES記法: Fc1c2nc[n](c2cc(c1Nc3c(cc(cc3)Br)Cl)C(=O)NOCCO)C
• InChI: 1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)
• InChI Key: CYOHGALHFOKKQC-UHFFFAOYSA-N

詳細

生物化学的／生理学的作用

Orally active, potent and selective MEK1/2 inhibitor with anti-cancer efficacy in cultures and in vivo.

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).

安全性情報

• ピクトグラム: GHS08,GHS07
• シグナルワード: Warning
• 危険有害性情報: H302,H317,H361f,H373,H413
• 注意書き: P202 - P273 - P280 - P301 + P312 - P302 + P352 - P308 + P313
• 危険有害性の分類: Acute Tox. 4 Oral - Aquatic Chronic 4 - Repr. 2 - Skin Sens. 1 - STOT RE 2
• ターゲットの組織: Gastrointestinal tract,Eyes,Urinary tract
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable