MMAE (Monomethyl auristatin E)

別名:SGD-1010

MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent.

MMAE (Monomethyl auristatin E)化学構造

CAS No. 474645-27-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 49300 国内在庫あり
JPY 29500 国内在庫あり
JPY 41500 国内在庫あり
JPY 119500 国内在庫なし(納期7~10日)
JPY 265500 国内在庫なし(納期7~10日)
JPY 595500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(8)

製品安全説明書

現在のバッチを見る: 純度: 99.99%
99.99

MMAE (Monomethyl auristatin E)関連製品

ADC Cytotoxin阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent.
In Vitro
In vitro

When coupled to cAC10, MMAE shows selective cytotoxicity in CD30+ cells, and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. [1]

When coupled to anti-CD79b antibody, anti–CD79b-vcMMAE has very potent and broad activity across a large panel of NHL cell lines in vitro. [2]

When coupled to anti-HER2 antibody, hertuzumab-vc-MMAE can also be effectively internalized and potently kill HER2 over-expressing tumor cells. [3]

細胞実験 細胞株 CD30+ Karpas 299 cells
濃度 ~1000 ng/mL
反応時間 96 h
実験の流れ

Cytotoxicity is measured using Alamar Blue dye reduction assay according to the manufacturer's directions. Briefly, a 40% solution (wt/vol) of Alamar Blue is freshly prepared in complete media just before cultures are added. Ninety-two hours after drug exposure, Alamar Blue solution is added to cells to constitute 10% culture volume. Cells are incubated for 4 hours, and dye reduction is measured on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT).

In Vivo
In Vivo

In the Karpas 299 ALCL model, cAC10-vcMMAE (1 mg/kg, i.v.) induces complete, durable tumor regression, while free MMAE (0.36 mg/kg) doesn’t produce detectable antitumor activity. [1]

In mouse xenograft models of NHL, anti–CD79b-vcMMAE (7 mg/kg, p.o.) strikingly results in sustained complete tumor remission. [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

化学情報

分子量 717.98 化学式
C39H67N5O7
 
CAS No. 474645-27-7 SDF Download MMAE (Monomethyl auristatin E) SDFをダウンロードする
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
保管 -20℃ power 3 years

In vitro
Batch:

DMSO : 100 mg/mL ( (139.27 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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