SML3522

DT2216

≥90% (HPLC)

• 別名: (2S,4R)-1-((S)-2-(7-(4-((R)-3-((4-(N-(4-(4-((4′-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoyl)sulfamoyl)-2-((trifluoromethyl)sulfonyl)phenyl)amino)-4-(phenylthio)butyl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide, DT 2216, DT-2216
• 実験式（ヒル表記法）: C₇₇H₉₆ClF₃N₁₀O₁₀S₄
• CAS番号: 2365172-42-3
• 分子量: 1542.36
• UNSPSCコード: 12352200
• NACRES: NA.21

特性

• 品質水準: 100
• アッセイ: ≥90% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear (Warmed)
• 保管温度: -10 to -25°C
• SMILES記法: CC(C)(C1)CCC(C2=CC=C(C=C2)Cl)=C1CN3CCN(C4=CC=C(C=C4)C(NS(=O)(C5=CC(S(C(F)(F)F)(=O)=O)=C(C=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCCC(N[C@@H](C(C)(C)C)C(N8[C@@H](C[C@H](C8)O)C(N[C@H](C9=CC=C(C%10=C(N=CS%10)C)C=C9)C)=O)=O)=O)=O)=O)=O)CC3

詳細

生物化学的／生理学的作用

DT2216 is a selective BCL-XL, but not BCL-2 or BCL-W, degrader composed of a von Hippel-Lindau (VHL) E3 ligase-targeting ligand linked to a ABT-263 (navitoclax) derivative. DT2216 is more potent than ABT-263 against BCL-XL-dependent leukemia (MOLT-4 IC50 = 52 vs 191 nM) and cancer cells (MDA-MB-231 IC50 = 229 vs 707 nM). DT2216 effectively inhibits the growth of several xenograft tumors in vivo either alone (15 mg/kg/wk i.p.) or in combination with other chemotherapeutic agents (docetaxel or VDL), exhbiting improved efficacy and reduced thrombocytopenia when compared with ABT-263 as a result of greatly reduced platelet toxicity due to poor VHL expression in platelets.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable