159857-80-4|MC-Val-Cit-PAB|MC-Val-Cit-PAB|MFCD26142966-范德生物科技公司

MC-Val-Cit-PAB

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names：
MC-Val-Cit-PAB
CAS号：
159857-80-4
MDL Number： MFCD26142966
MF(分子式)： C28H40N6O7 MW(分子量)： 572.65
EINECS: Reaxys Number:
Pubchem ID:57544445 Brand:BIOFOUNT

MC-Val-Cit-PAB(159857-80-4)是一种ADC肽连接化合物，可用于ADC偶联物的形成，在抗癌研究中具有重要意义。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
YZM000948-1g	1g	99%	¥ 5600.00	¥ 5600.00		2-3天	- +	¥ 0.00
YZM000948-250mg	250mg	99%	¥ 2260.00	¥ 2260.00		2-3天	- +	¥ 0.00

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中文别名	MC-Val-Cit-PAB(159857-80-4)
英文别名	MC-Val-Cit-PAB,159857-80-4
CAS号	159857-80-4
SMILES	CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(CO)C=C1)=O)=O)NC(CCCCCN2C(C=CC2=O)=O)=O
Inchi	InChI=1S/C28H40N6O7/c1-18(2)25(33-22(36)8-4-3-5-16-34-23(37)13-14-24(34)38)27(40)32-21(7-6-15-30-28(29)41)26(39)31-20-11-9-19(17-35)10-12-20/h9-14,18,21,25,35H,3-8,15-17H2,1-2H3,(H,31,39)(H,32,40)(H,33,36)(H3,29,30,41)/t21-,25-/m0/s1
InchiKey	AMKBTTRWLGVRER-OFVILXPXSA-N
分子式 Formula	C28H40N6O7
分子量 Molecular Weight	572.65
闪点 FP	517.2±34.3 °C
熔点 Melting point	No data available
沸点 Boiling point	931.6±65.0 °C at 760 mmHg
Polarizability极化度	59.7±0.5 10-24cm3
密度 Density	1.3±0.1 g/cm3
蒸汽压 Vapor Pressure	0.0±0.3 mmHg at 25°C
溶解度Solubility
性状	白色至灰白色固体粉末
储藏条件 Storage conditions	4°C，在氮气下储存

MC-Val-Cit-PAB(159857-80-4)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染

MC-Val-Cit-PAB(159857-80-4) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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产品说明	MC-Val-Cit-PAB(159857-80-4)是一种ADC肽连接化合物，可用于ADC偶联物的形成，在抗癌研究中具有重要意义。
Introduction	MC-Val-Cit-PAB(159857-80-4), a kind of ADC peptide linker, could be used in the formation of ADC conjugate and be significant in anticancer studies.
Application1
Application2
Application3

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

1.A developed antibody-drug conjugate rituximab-vcMMAE shows a potent cytotoxic activity against CD20-positive cell line.
Abdollahpour-Alitappeh M;Hashemi Karouei SM;Lotfinia M;Amanzadeh A;Habibi-Anbouhi M Artif Cells Nanomed Biotechnol. 2018 Mar 9:1-8. doi: 10.1080/21691401.2018.1449119. [Epub ahead of print]
Rituximab is a chimeric monoclonal antibody directed against B-lymphocyte specific antigen CD20, which is used for the treatment of B-cell malignancies. However, the effectiveness of rituximab is limited partly due to treatment resistance. The aim of this study was to develop rituximab-based antibody drug conjugate (ADC) to enhance rituximab activity. In this study, monomethyl auristatin E (MMAE) was covalently conjugated to dithiothreitol -reduced rituximab via a valine-citrulline peptide linker (rituximab-vcMMAE). The conjugates were then characterized by using nonreducing sodium dodecyl sulfate-polyacrylamide electrophoresis (SDS-PAGE) and cell-based enzyme-linked immunosorbent assay (ELISA). The cytotoxic activity of the ADC was evaluated against Raji (human B-cell lymphoma; CD20-positive) and MOLT-4 (T lymphoblast; acute lymphoblastic leukemia; CD20-negative) cell lines. In addition, the colony formation assay was used to identify the propagation ability of ADC-treated cells in vitro. Results from nonreducing SDS-PAGE revealed various species of rituximab-MC-Val-Cit-PABC-MMAE (rituximab-vcMMAE), as compared with unconjugated rituximab. The binding capacity of rituximab-vcMMAE to the CD20-positive cell was similar to that of the parental rituximab.

2.An anti-HER2 antibody conjugated with monomethyl auristatin E is highly effective in HER2-positive human gastric cancer.
Li H;Yu C;Jiang J;Huang C;Yao X;Xu Q;Yu F;Lou L;Fang J Cancer Biol Ther. 2016 Apr 2;17(4):346-54. doi: 10.1080/15384047.2016.1139248. Epub 2016 Feb 6.
Antibody-drug conjugate (ADC) is a novel class of therapeutics for cancer target therapy. This study assessed antitumor activity of ADC with an antimitotic agent, monomethyl auristatin E (MMAE) and a humanized monoclonal anti-HER2 antibody, hertuzumab, in gastric cancer. The efficacy of hertuzumab-MC-Val-Cit-PAB-MMAE (hertuzumab-vcMMAE) on human epidermal growth factor receptor 2 (HER2) positive human gastric cancer cells, NCI-N87, was evaluated in vitro and in vivo. The cytotoxicity of hertuzumab was significantly enhanced after conjugation with MMAE. Compared to trastuzumab, hertuzumab had a higher affinity to HER2 and had more potent antibody-dependent cell-mediated cytotoxicity (ADCC) activity in vitro. After conjugation with MMAE, the binding specificity for HER2 was not affected. Furthermore, the internalization of hertuzumab-vcMMAE in HER2 positive gastric cancer cells was verified. Although the conjugation of hertuzumab and MMAE decreased the ADCC effect, the overall cytotoxicity was dramatically increased in HER2 positive gastric cancer cells. In vitro data on this hertuzumab-vcMMAE has exerted much stronger antitumor activity compared to trastuzumab-DM1 in HER2 positive gastric cancer cells.

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