MMAE (Monomethyl auristatin E)

別名：SGD-1010

製品コード：S7721 純度：99.99%

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

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
1mg	JPY 29500	国内在庫あり
5mg	JPY 41500	国内在庫あり
25mg	JPY 119500	国内在庫なし(納期7~10日)
100mg	JPY 265500	国内在庫なし(納期7~10日)
1g	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（7）

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

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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
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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]

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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考
[1] Francisco JA, et al. Blood. 2003, 102(4), 1458-1465. [2] Dornan D, et al. Blood. 2009, 114(13), 2721-2729. [3] Yao X, et al. Breast Cancer Res Treat. 2015, 153(1), 123-133. [4] Wang S, et al. Cancer Lett. 2017 Nov 28;409:125-136. + 展開

参考

[4] Wang S, et al. Cancer Lett. 2017 Nov 28;409:125-136.

+ 展開

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	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	-20℃ power 3 years	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):