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D8-MMAF Sale

(Synonyms: Monomethylauristatin F D8) 目录号 : GC35798

D8-MMAF是MMAF的氘代形式。

D8-MMAF Chemical Structure

规格 价格 库存 购买数量
1mg
¥9,900.00
现货
5mg
¥22,500.00
现货
10mg
¥42,300.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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产品描述

D8-MMAF is a deuterated form of MMAF, which is a microtubule disrupting agent. IC50: 119 nM (Cytotoxicity, Karpas 299 cell), 105 nM (Cytotoxicity, H3396 cell), 257 nM (Cytotoxicity, 786-O cell), 200 nM (Cytotoxicity, Caki-1, cell)[1]

MMAF shows in vitro cytotoxicity against a panel of cell lines. The IC50 values for Karpas 299, H3396, 786-O and Caki-1 are 119, 105, 257, and 200 nM, respectively. Targeted MMAF is much more potent than the free drug, and that cAC10 conjugates of MMAF display pronounced activities. On a molar basis, the cAC10-L1-MMAF4 is an average of over 2200-fold more potent than free MMAF and is active on all the CD30-positive cell lines tested[1].

The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (1 mg/kg). cAC10-L1-MMAF4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively[1].

[1]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.

Chemical Properties

Cas No. SDF
别名 Monomethylauristatin F D8
Canonical SMILES CC[C@H](C)[C@@H]([C@@H](CC(N1[C@@H](CCC1)[C@@H]([C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)OC)=O)OC)N(C([C@@](C([2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])([2H])NC([C@H](C(C)C)NC)=O)=O)C
分子式 C39H57D8N5O8 分子量 740.01
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.3513 mL 6.7567 mL 13.5133 mL
5 mM 0.2703 mL 1.3513 mL 2.7027 mL
10 mM 0.1351 mL 0.6757 mL 1.3513 mL
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