Mc-MMAE 纯度:97.23% 5mg

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Mc-MMAE 纯度:97.23% 5mg

市场价：: 9114.00

促销价：: ¥9114.00

货号：HY-15741

品牌：MCE

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北京朝阳

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商品介绍
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Mc-MMAE 是保护基团 (马来酰亚氨基己酰) 共轭连接到单甲基 auristatin E (MMAE)。Mc-MMAE 是有效的微管蛋白抑制剂，是抗体偶联药物 (ADC) 中的毒性物质。

Description

Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate (ADC).

IC₅₀ & Target

Tubulin, Antibody-drug conjugates (ADC)^[1]

In Vitro

Synthesis of maleimidocaproyl-MMAE (mc-MMAE) requires the addition of maleimidocaproic acid to a solution of MMAE in dichloromethane followed by the addition of diethyl cyanophosphonate and diisopropylethylamine^[1].

Solvent & Solubility

In Vitro:

DMSO : ≥ 51 mg/mL (55.97 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0975 mL	5.4874 mL	10.9748 mL
5 mM	0.2195 mL	1.0975 mL	2.1950 mL
10 mM	0.1097 mL	0.5487 mL	1.0975 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[1]. Sanderson RJ, et al. In vivo drug-linker stability of an anti-CD30 dipeptide-linked auristatin immunoconjugate. Clin Cancer Res. 2005 Jan 15;11(2 Pt 1):843-52.

Kinase Assay ^[1]	Horseradish peroxidase (HRP) is thiolated with 2-iminothiolane and conjugated to mc-MMAE to generate the HRP-MMAE reporter enzyme-drug conjugate. Briefly, a thiolation reaction mixture containing 0.2 mM HRP (8 mg/mL) and 50 mM 2-iminothiolane in 25 mM sodium borate decahydrate (Na₂B₄O₇•10H₂O) buffer (pH 9.0) is incubated for 1 hour at 37°C. Unreacted 2-iminothiolane is removed by passage through a PD-10 desalting column equilibrated in PBS (pH 7.4). Peak fractions are pooled and mc-MMAE is coupled to thiolated HRP (HRP-SH) at a molar ratio of 3:1. The final conjugation reaction mixture contained 80 μM HRP-SH (3.2 mg/mL) in sodium borate buffer [50 mM H₃BO₃, 50 mM NaCl (pH 8.0); 80% v/v] and 240 μM mc-MMAE in ice-cold CH₃CN (20% v/v). After 30 minutes on ice, the reaction is terminated with a 20-fold molar excess of free cysteine (4.8 mM) before PD-10 chromatography. Peak fractions containing HRP-MMAE (exchanged into PBS) are pooled and evaluated for extent of modification using the thiol-reactive dye, Alexa Fluor 594 C₅ maleimide^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Sanderson RJ, et al. In vivo drug-linker stability of an anti-CD30 dipeptide-linked auristatin immunoconjugate. Clin Cancer Res. 2005 Jan 15;11(2 Pt 1):843-52.

Kinase Assay
^[1]

Horseradish peroxidase (HRP) is thiolated with 2-iminothiolane and conjugated to mc-MMAE to generate the HRP-MMAE reporter enzyme-drug conjugate. Briefly, a thiolation reaction mixture containing 0.2 mM HRP (8 mg/mL) and 50 mM 2-iminothiolane in 25 mM sodium borate decahydrate (Na₂B₄O₇•10H₂O) buffer (pH 9.0) is incubated for 1 hour at 37°C. Unreacted 2-iminothiolane is removed by passage through a PD-10 desalting column equilibrated in PBS (pH 7.4). Peak fractions are pooled and mc-MMAE is coupled to thiolated HRP (HRP-SH) at a molar ratio of 3:1. The final conjugation reaction mixture contained 80 μM HRP-SH (3.2 mg/mL) in sodium borate buffer [50 mM H₃BO₃, 50 mM NaCl (pH 8.0); 80% v/v] and 240 μM mc-MMAE in ice-cold CH₃CN (20% v/v). After 30 minutes on ice, the reaction is terminated with a 20-fold molar excess of free cysteine (4.8 mM) before PD-10 chromatography. Peak fractions containing HRP-MMAE (exchanged into PBS) are pooled and evaluated for extent of modification using the thiol-reactive dye, Alexa Fluor 594 C₅ maleimide^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Sanderson RJ, et al. In vivo drug-linker stability of an anti-CD30 dipeptide-linked auristatin immunoconjugate. Clin Cancer Res. 2005 Jan 15;11(2 Pt 1):843-52.

Molecular Weight	911.18
Formula	C₄₉H₇₈N₆O₁₀
CAS No.	863971-24-8
SMILES	O=C1N(CCCCCC(N(C)[C@H](C(N[C@@H](C(C)C)C(N([C@@H]([C@@H](C)CC)[C@@H](CC(N2[C@H]([C@H](OC)[C@H](C(N[C@@H]([C@H](C3=CC=CC=C3)O)C)=O)C)CCC2)=O)OC)C)=O)=O)C(C)C)=O)C(C=C1)=O
Storage	4°C, stored under nitrogen
Shipping	Room temperature in continental US; may vary elsewhere