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Qiagen 凯杰 Biosharp Omega

首页酶、辅酶及抑制剂MCE>

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Monomethyl auristatin E 纯度:99.94% 10mg

价:
560.00
价:
¥560.00

号:HY-15162

牌:MCE

账期 货到付款

(预计4-5工作日到货(以MCE官网货期为准))

工作时间

周一至周五:9:00-18:00

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0771-3293894

在线咨询

客服 郭恒 蔡玉坤 曾宪飞 技术咨询

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Monomethyl auristatin E (MMAE) 是海兔毒素10的合成衍生物,通过抑制微管蛋白聚合而起到有效的有丝分裂抑制作用。 MMAE广泛用作细胞毒性成分制作抗体-药物偶联物 (ADCs) 以治疗癌症。

Description

Monomethyl auristatin E (MMAE) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

IC50 & Target

Microtubule[1]

In Vitro

Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells[1]. MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells[2].

In Vivo

Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolongs tumor regression in xenograft models[2].

Solvent & Solubility
In Vitro:  

DMSO : ≥ 48 mg/mL (66.85 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3928 mL 6.9640 mL 13.9280 mL
5 mM 0.2786 mL 1.3928 mL 2.7856 mL
10 mM 0.1393 mL 0.6964 mL 1.3928 mL
* Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. Thirty μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. Blots are developed by ECL.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

717.98

Formula

C₃₉H₆₇N₅O₇

CAS No.

474645-27-7

SMILES

CC(C)[C@H](NC)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@@H](CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C)[C@H](C2=CC=CC=C2)O)=O)=O)OC)C)=O)C(C)C)=O

Storage

4°C, stored under nitrogen

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.94%

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