MMAE (Monomethyl auristatin E)
别名: SGD-1010 中文名称：一甲基澳瑞他汀E
MMAE (Monomethyl auristatin E)是合成的抗肿瘤药。它也是一种能够破坏微管的试剂。
MMAE (Monomethyl auristatin E) Chemical Structure
CAS: 474645-27-7
客户使用Selleck的发表文献7篇
产品质控
MMAE (Monomethyl auristatin E)相关产品
ADC Cytotoxin抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | MMAE (Monomethyl auristatin E)是合成的抗肿瘤药。它也是一种能够破坏微管的试剂。 |
|---|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 耦合到cAC10时，MMAE在CD30+细胞中表现出选择性细胞毒性，并通过诱导细胞凋亡，引起G2/M期生长阻滞和细胞死亡。[1] 在体外，与抗-CD79b抗体耦合时，抗-CD79b-vcMMAE对一大组NHL细胞系具有非常有效且广泛的活性。[2] 与抗-HER2抗体耦合时，hertuzumab-vc-MMAE能够被充分吸收，并有效杀死HER2过表达的肿瘤细胞。[3] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | CD30+ Karpas 299细胞 | ||
| 浓度 | ~1000 ng/mL | |||
| 孵育时间 | 96小时 | |||
| 方法 | 细胞毒性使用Alamar Blue染料还原试验根据制造商指示测量。简而言之，培养物加入之前，Alamar Blue 40% 的溶液(wt/vol)在完全培养基中新鲜制备。药物暴露92小时后，Alamar Blue加入到细胞中，构成10%的培养体积。细胞培养4小时，染料的减少在Fusion HT荧光分析仪(Packard仪器，Meriden，CT)上测量。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 |
在Karpas 299 ALCL模型中，cAC10-vcMMAE (1 mg/kg, i.v.)诱导完全的，持久的肿瘤退化，而游离MMAE (0.36 mg/kg)不会产生可检测的抗肿瘤活性。[1] 在NHL小鼠异种移植模型中，抗-CD79b-vcMMAE (7 mg/kg, p.o.)显著导致持续完全的肿瘤消退。[2] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06181994 | Recruiting | Chronic Subdural Hematoma |
Montefiore Medical Center |
December 5 2023 | -- |
| NCT05514158 | Recruiting | Gastric Cancer |
RemeGen Co. Ltd. |
September 28 2022 | Phase 1 |
| NCT05773937 | Recruiting | Advanced Malignant Solid Tumors |
Mabwell (Shanghai) Bioscience Co. Ltd. |
June 21 2022 | Phase 1 |
| NCT05216965 | Recruiting | Solid Tumors |
Mabwell (Shanghai) Bioscience Co. Ltd. |
June 11 2022 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 717.98 | 分子式 | C39H67N5O7
|
| CAS号 | 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 | ||
| 储存条件(自收到货起) | -20℃ 粉末 三年 | ||
|
体外溶解度 |
DMSO : 100 mg/mL ( (139.27 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (139.27 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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