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SPDB-DM4 Sale

目录号 : GC32982

SPDB-DM4是ADC的一部分,由maytansinebasedpayload(DM4)和SPDB连接而成,具有高效的抗肿瘤活性。

SPDB-DM4 Chemical Structure

Cas No.:1626359-62-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥14,661.00
现货
1mg
¥3,124.00
现货
5mg
¥8,479.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via a SPDB linker, exhibiting potent anti-tumor activity.

[1]. Puja Sapra, et al. Investigational antibody drug conjugates for solid tumors. Journal Expert Opinion on Investigational Drugs Volume 20, 2011-Issue 8.

Chemical Properties

Cas No. 1626359-62-3 SDF
Canonical SMILES C[C@]1([C@H](CC(N(C(C=C2C=C3OC)=C3Cl)C)=O)OC([C@H](C)N(C)C(CCC(C)(C)SSCCCC(ON(C4=O)C(CC4)=O)=O)=O)=O)[C@H]([C@@H]([C@](OC5=O)([H])C[C@]([C@](/C=C/C=C(C)/C2)([H])OC)(N5)O)C)O1
分子式 C46H63ClN4O14S2 分子量 995.59
溶解度 Soluble in DMSO 储存条件 -80°C, protect from light, stored under nitrogen
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.0044 mL 5.0221 mL 10.0443 mL
5 mM 0.2009 mL 1.0044 mL 2.0089 mL
10 mM 0.1004 mL 0.5022 mL 1.0044 mL
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Research Update

Sensitive ELISA Method for the Measurement of Catabolites of Antibody-Drug Conjugates (ADCs) in Target Cancer Cells

Mol Pharm 2015 Jun 1;12(6):1752-61.PMID:25738394DOI:10.1021/acs.molpharmaceut.5b00028.

A new, sensitive ELISA method has been developed which measures catabolites in cells and media upon processing of antibody-drug conjugates (ADCs) by target cancer cells. This ELISA method, exemplified for maytansinoid ADCs, uses competitive inhibition by a maytansinoid analyte of the binding of biotinylated antimaytansine antibody to an immobilized BSA-maytansinoid conjugate. Synthetic standards of several maytansinoid catabolites derived from ADCs with different linkers were tested and showed similar inhibition curves, with an EC50 of about 0.1 nM (0.03 pmol in an assay volume of 0.25 mL). This high sensitivity allowed quantification of catabolites from a methanolic cell extract and from the medium, generated from an ADC in 1 day using only about 1 million cells. The processing of anti-EpCAM and anti-CanAg ADCs with noncleavable linker (SMCC-DM1), disulfide linker (SPDB-DM4), and charged sulfonate-bearing disulfide linker (sulfo-SPDB-DM4), each containing an average of about four maytansinoid molecules per antibody, were compared in colon cancer cell lines (COLO 205 and HT-29). An 8-10-fold higher total level of catabolite was observed for anti-CanAg ADCs than for anti-EpCAM ADCs upon processing by COLO 205 cells, consistent with a higher cell-surface expression of CanAg. In a multidrug resistant HCT-15 colon cancer cell line, the anti-EpCAM-SPDB-DM4 linker conjugate was not cytotoxic and showed a significantly lower level of catabolite within cells compared to that in medium, presumably due to Pgp-mediated efflux of the nonpolar DM4 catabolite. In contrast, sulfo-SPDB-DM4 and SMCC-DM1 linker conjugates were cytotoxic, which correlated with higher amounts of catabolites found within the HCT-15 cells relative to amounts in medium. In a nonmultidrug resistant HT-29 cell line, the anti-EpCAM-SPDB-DM4 linker conjugate was cytotoxic, with most of the catabolite found in cells and little in the medium. In conclusion, this highly sensitive ELISA method for measurement of ADC catabolite is convenient for screening multiple ADC parameters such as linkers and antibodies in a number of cell lines, does not require concentration of sample or extraction of media, and is complementary to other reported methods such as radiolabeling of ADCs or mass spectrometry.