SML3228

Rimiducid

≥90% (HPLC)

• 別名: (S,2S,2′S)-((1R,1′R)-1,1′-(3,3′-(2,2′-(Ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy)bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl)) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate), 1,1′-{Ethylenebis[azanediyl(2-oxoethane-2,1-diyl)oxy-3,1-phenylene]}bis[(1R)-3(3,4-dimethoxyphenyl)propyl]bis{(2S)-1-[(2S)-2-(3,4,5trimethoxyphenyl)butanoyl]piperidine-2-carboxylate}, 2,2′-[1,2-Ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] bis[(2S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate], AP 1903, AP-1903, AP1903
• 実験式（ヒル表記法）: C₇₈H₉₈N₄O₂₀
• CAS番号: 195514-63-7
• 分子量: 1411.63
• MDL番号: MFCD25976784
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥90% (HPLC)
• フォーム: 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: N2([C@@H](CCCC2)C(=O)O[C@H](CCc8cc(c(cc8)OC)OC)c3cc(ccc3)OCC(=O)NCCNC(=O)COc4cc(ccc4)[C@H](OC(=O)[C@H]6N(CCCC6)C(=O)[C@@H](CC)c7cc(c(c(c7)OC)OC)OC)CCc5cc(c(cc5)OC)OC)C(=O)[C@@H](CC)c1cc(c(c(c1)OC)OC)OC
• InChI Key: GQLCLPLEEOUJQC-ZTQDTCGGSA-N

詳細

生物化学的／生理学的作用

Rimiducid (AP1903) is a homodimeric FKBP12 Phe36Val (F36V-FKBP, FKBP-F36V) mutant-selective cross-linker composed of two high-affinity ligands, each with 713-fold selectivity over endogenous FKBP (Kd = 94 pM/F36V- vs 67 nM/Wt-FKBP using 4′-AF-labeled rimiducid). Rimiducid activates signaling events via Chemical Induction of Dimerization (CID) by cross-linking FKBP12-F36 fusions (Chimeric Antigen Receptor or CAR) expressed in cells in cultures (apoptosis induction EC50 = 0.1 nM; HT1080 expressing FKBP(F36V)-Fas intracellular domain) and in animals in vivo (EC50 = 0.4 mg/kg i.v. in a murine model of conditional cell ablation).

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3