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159857-80-4
  • names:

    MC-Val-Cit-PAB

  • CAS號:

    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
MC-Val-Cit-PAB(159857-80-4)是一種ADC肽連接化合物,可用于ADC偶聯(lián)物的形成,在抗癌研究中具有重要意義。
貨品編碼 規(guī)格 純度 價格 (¥) 現(xiàn)價(¥) 特價(¥) 庫存描述 數(shù)量 總計 (¥)
YZM000948-1g 1g 99% ¥ 5600.00 ¥ 5600.00 2-3天
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YZM000948-250mg 250mg 99% ¥ 2260.00 ¥ 2260.00 2-3天
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中文別名 MC-Val-Cit-PAB(159857-80-4)
英文別名 MC-Val-Cit-PAB,159857-80-4
CAS號 159857-80-4
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
溶解度Solubility
性狀 白色至灰白色固體粉末
儲藏條件 Storage conditions 4°C,在氮氣下儲存

MC-Val-Cit-PAB(159857-80-4)實驗注意事項:
1.實驗前需戴好防護眼鏡,穿戴防護服和口罩,佩戴手套,避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生,必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲,并交于專業(yè)生物廢氣物處理公司處理,以免造成環(huán)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.

Tag:MC-Val-Cit-PAB(159857-80-4),MC-Val-Cit-PAB試劑,MC-Val-Cit-PAB抑制劑,MC-Val-Cit-PAB的純度,MC-Val-Cit-PAB的作用,MC-Val-Cit-PAB的合成路線,MC-Val-Cit-PAB的廠家,MC-Val-Cit-PAB的價格,MC-Val-Cit-PAB的外觀,MC-Val-Cit-PAB的MSDS,MC-Val-Cit-PAB的注意事項
產(chǎn)品說明 MC-Val-Cit-PAB(159857-80-4)是一種ADC肽連接化合物,可用于ADC偶聯(lián)物的形成,在抗癌研究中具有重要意義。
IntroductionMC-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

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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