MMAE (Monomethyl auristatin E)

別名: SGD-1010 中文名稱：一甲基澳瑞他汀E

目錄號：S7721 Purity: 99.99%

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

CAS: 474645-27-7

規(guī)格	價格	庫存
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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產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

MMAE (Monomethyl auristatin E)相關(guān)產(chǎn)品

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相關(guān)化合物庫	激酶抑制劑庫血管生成相關(guān)化合物庫 TGF-beta/Smad信號通路庫細胞骨架信號通路化合物庫抗心血管疾病化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

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，MMAE在CD30⁺細胞中表現(xiàn)出選擇性細胞毒性，并通過誘導(dǎo)細胞凋亡，引起G2/M期生長阻滯和細胞死亡。^[1] 在體外，與抗-CD79b抗體耦合時，抗-CD79b-vcMMAE對一大組NHL細胞系具有非常有效且廣泛的活性。^[2] 與抗-HER2抗體耦合時，hertuzumab-vc-MMAE能夠被充分吸收，并有效殺死HER2過表達的腫瘤細胞。^[3]
細胞實驗	細胞系	CD30⁺ Karpas 299細胞
	濃度	~1000 ng/mL
	孵育時間	96小時
	方法	細胞毒性使用Alamar Blue染料還原試驗根據(jù)制造商指示測量。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小時后，Alamar Blue加入到細胞中，構(gòu)成10%的培養(yǎng)體積。細胞培養(yǎng)4小時，染料的減少在Fusion HT熒光分析儀(Packard儀器，Meriden，CT)上測量。

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)不會產(chǎn)生可檢測的抗腫瘤活性。^[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]

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)不會產(chǎn)生可檢測的抗腫瘤活性。^[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
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
[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

參考文獻

[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

化學(xué)信息&溶解度

分子量	717.98	分子式	C₃₉H₆₇N₅O₇
CAS號	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
儲存條件(自收到貨起)	-20℃ 粉末三年	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	-20℃ 粉末三年	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

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

Ethanol : 100 mg/mL (139.27 mM)

Water : Insoluble

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

Ethanol : 100 mg/mL (139.27 mM)

Water : Insoluble

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

Ethanol : 100 mg/mL (139.27 mM)

Water : Insoluble

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

Ethanol : 100 mg/mL (139.27 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

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

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(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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MMAE (Monomethyl auristatin E)

產(chǎn)品質(zhì)控

MMAE (Monomethyl auristatin E)相關(guān)產(chǎn)品

細胞實驗數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實驗計算

技術(shù)支持