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Monomethyl auristatin E (MMAE) 是海兔毒素 10 的合成衍生物,是一种抗有丝分裂剂,通过阻断微管蛋白的聚合来抑制细胞分裂,并且还具有抑制抗体-药物偶联物的活性。
Monomethyl auristatin E (MMAE) 是海兔毒素 10 的合成衍生物,是一种抗有丝分裂剂,通过阻断微管蛋白的聚合来抑制细胞分裂,并且还具有抑制抗体-药物偶联物的活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥ 291 | 现货 | |
25 mg | ¥ 397 | 现货 | |
50 mg | ¥ 552 | 现货 |
产品描述 | Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity. |
体外活性 | 当与cAC10结合时,Monomethyl auristatin E在CD30+细胞中表现出选择性的细胞毒性,并通过诱导凋亡来引起G2/M期生长停滞和细胞死亡。[1] 当与抗CD79b抗体结合时,抗CD79b-vcMonomethyl auristatin E对体外的大量NHL细胞系具有非常强大和广泛的活性。[2] 当与抗HER2抗体结合时,hertuzumab-vc-Monomethyl auristatin E也能有效地被内化,并强力地杀死过表达HER2的肿瘤细胞。[3] |
体内活性 | 在Karpas 299 ALCL模型中,cAC10-vcMonomethyl auristatin E(1 mg/kg,i.v.)引起完全且持久的肿瘤消退,而自由Monomethyl auristatin E(0.36 mg/kg)未显示出可检测的抗肿瘤活性。[1] 在NHL小鼠异种移植模型中,anti–CD79b-vcMonomethyl auristatin E(7 mg/kg,p.o.)显著导致持续的完全肿瘤缓解。[2] |
细胞实验 | Cytotoxicity is measured using Alamar Blue dye reduction assay according to the manufacturer's directions. Briefly, a 40% solution (wt/vol) of Alamar Blue is freshly prepared in complete media just before cultures are added. Ninety-two hours after drug exposure, Alamar Blue solution is added to cells to constitute 10% culture volume. Cells are incubated for 4 hours, and dye reduction is measured on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT). (Only for Reference) |
别名 | 一甲基澳瑞他汀E, Vedotin, MMAE |
分子量 | 717.98 |
分子式 | C39H67N5O7 |
CAS No. | 474645-27-7 |
Smiles | CC[C@H](C)C([C@@H](CC(=O)N1CCC[C@H]1C(OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)[C@@H](C(C)C)C(=O)NC(=O)[C@@H](NC)C(C)C |
密度 | 1.088 g/cm3 (Predicted) |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 71.8 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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