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MMAE (Monomethyl auristatin E)

別名: SGD-1010 中文名稱：一甲基澳瑞他汀E

MMAE (Monomethyl auristatin E)是合成的抗腫瘤藥。它也是一種能夠破壞微管的試劑。

MMAE (Monomethyl auristatin E) Chemical Structure

MMAE (Monomethyl auristatin E) Chemical Structure

CAS: 474645-27-7

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 2694.51 現(xiàn)貨
1mg 956.03 現(xiàn)貨
5mg 2264.09 現(xiàn)貨
25mg 6534.84 現(xiàn)貨
100mg 14496.3 現(xiàn)貨
1g 57248.1 現(xiàn)貨
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MMAE (Monomethyl auristatin E)相關(guān)產(chǎn)品

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
non-small cell lung cancer cells Cytotoxicity assay 0.5 to 1 nM 4 days Cytotoxicity against human non-small cell lung cancer cells at 0.5 to 1 nM after 4 days by XTT assay 23845743
HCT116 Function assay 0.5 mM 24 hrs Effect on mitochondrial respiration in human HCT116 cells expressing carbonic anhydrase 9 assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis 28895394
KB Antiproliferative assay 4 days Antiproliferative activity against human KB cells after 4 days by XTT assay, IC50=0.00019μM 23845743
A549 Antiproliferative assay 4 days Antiproliferative activity against human A549 cells after 4 days by XTT assay, IC50=0.00059μM 23845743
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay, GI50=0.000418μM 28211277
SF268 Growth inhibition assay 48 hrs Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay, GI50=0.000432μM 28211277
KM20L2 Growth inhibition assay 48 hrs Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay, GI50=0.000599μM 28211277
NCI-H460 Growth inhibition assay 48 hrs Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay, GI50=0.000683μM 28211277
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.000418μM 28895394
SF268 Growth inhibition assay 48 hrs Growth inhibition of human SF268 cells after 48 hrs by SRB assay, GI50=0.000432μM 28895394
KM20L2 Growth inhibition assay 48 hrs Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay, GI50=0.000599μM 28895394
NCI-H460 Growth inhibition assay 48 hrs Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay, GI50=0.000683μM 28895394
MCF7 Growth inhibition assay 48 hrs Growth inhibition of human MCF7 cells after 48 hrs by SRB assay, GI50=0.000404μM 28926240
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.000418μM 28926240
SF268 Growth inhibition assay 48 hrs Growth inhibition of human SF268 cells after 48 hrs by SRB assay, GI50=0.000432μM 28926240
KM20L2 Growth inhibition assay 48 hrs Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay, GI50=0.000599μM 28926240
NCI-H460 Growth inhibition assay 48 hrs Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay, GI50=0.000683μM 28926240
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, EC50=0.0005μM 28972755
SKOV3 Cytotoxicity assay 2 days Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.00066μM 29454703
A549 Cytotoxicity assay 2 days Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.0013μM 29454703
L1210 Cytotoxicity assay 2 days Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.0021μM 29454703
NCI-H524 Cytotoxicity assay 2 hrs Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay, IC50=0.0037μM 30735385
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 23845743
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 25431858
MDA-MB-361 Cytotoxicity assay Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay, GI50=0.00049μM 25431858
NCI-N87 Cytotoxicity assay Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay, GI50=0.00054μM 25431858
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 28211277
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 28972755
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生物活性

產(chǎn)品描述 MMAE (Monomethyl auristatin E)是合成的抗腫瘤藥。它也是一種能夠破壞微管的試劑。
體外研究(In Vitro)
體外研究活性

耦合到cAC10時(shí)，MMAE在CD30+細(xì)胞中表現(xiàn)出選擇性細(xì)胞毒性，并通過誘導(dǎo)細(xì)胞凋亡，引起G2/M期生長阻滯和細(xì)胞死亡。[1]

在體外，與抗-CD79b抗體耦合時(shí)，抗-CD79b-vcMMAE對(duì)一大組NHL細(xì)胞系具有非常有效且廣泛的活性。[2]

與抗-HER2抗體耦合時(shí)，hertuzumab-vc-MMAE能夠被充分吸收，并有效殺死HER2過表達(dá)的腫瘤細(xì)胞。[3]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 CD30+ Karpas 299細(xì)胞
濃度 ~1000 ng/mL
孵育時(shí)間 96小時(shí)
方法

細(xì)胞毒性使用Alamar Blue染料還原試驗(yàn)根據(jù)制造商指示測(cè)量。簡而言之，培養(yǎng)物加入之前，Alamar Blue 40% 的溶液(wt/vol)在完全培養(yǎng)基中新鮮制備。藥物暴露92小時(shí)后，Alamar Blue加入到細(xì)胞中，構(gòu)成10%的培養(yǎng)體積。細(xì)胞培養(yǎng)4小時(shí)，染料的減少在Fusion HT熒光分析儀(Packard儀器，Meriden，CT)上測(cè)量。
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

在Karpas 299 ALCL模型中，cAC10-vcMMAE (1 mg/kg, i.v.)誘導(dǎo)完全的，持久的腫瘤退化，而游離MMAE (0.36 mg/kg)不會(huì)產(chǎn)生可檢測(cè)的抗腫瘤活性。[1]

在NHL小鼠異種移植模型中，抗-CD79b-vcMMAE (7 mg/kg, p.o.)顯著導(dǎo)致持續(xù)完全的腫瘤消退。[2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06395103 Not yet recruiting
B-cell Acute Lymphoblastic Leukemia|Diffuse Large B-cell Lymphoma|Burkitt Lymphoma|Neuroblastoma|Ewing Sarcoma
Merck Sharp & Dohme LLC
 June 4 2024 Phase 1|Phase 2
NCT06227156 Recruiting
Castration-resistant Prostate Cancer
RemeGen Co. Ltd.
 April 8 2024 Phase 1
NCT06265727 Recruiting
Solid Tumor Adult
Corbus Pharmaceuticals Inc.|CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co. Ltd.
 April 1 2024 Phase 1|Phase 2
NCT06351020 Not yet recruiting
Locally Advanced or Metastatic GC and GCJ Adenocarcinoma
LaNova Medicines Zhejiang Co. Ltd.|LaNova Medicines Limited
 April 1 2024 Phase 3

化學(xué)信息&溶解度

分子量 717.98 分子式
C39H67N5O7
 
CAS號(hào) 474645-27-7 SDF Download MMAE (Monomethyl auristatin E) SDF
Smiles CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(C)C(C2=CC=CC=C2)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)NC
儲(chǔ)存條件(自收到貨起) -20℃ 粉末 三年

體外溶解度
批次：

DMSO : 100 mg/mL ( (139.27 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 100 mg/mL (139.27 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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