VcMMAE 纯度:99.89% 1mg

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VcMMAE 纯度:99.89% 1mg

市场价：: 420.00

促销价：: ¥420.00

货号：HY-15575

品牌：MCE

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北京朝阳

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商品介绍
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VcMMAE是抗体药物复合体的一部分 (drug-linker conjugate for ADC)，具有抗癌活性，它由MMAE和Vc连接而成。

Description

VcMMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

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 sensitized 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 prolonged tumor regression in xenograft models^[2].

Solvent & Solubility

In Vitro:

DMSO : ≥ 54 mg/mL (41.01 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.7595 mL	3.7976 mL	7.5951 mL
5 mM	0.1519 mL	0.7595 mL	1.5190 mL
10 mM	0.0760 mL	0.3798 mL	0.7595 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

VcMMAE is dissolved in DMSO and then diluted with 0.9% NaCl^[3].

References

[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.

[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.

[3]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.

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. 30μg 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]	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	[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897. [2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87. [3]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.

Molecular Weight	1316.63
Formula	C₆₈H₁₀₅N₁₁O₁₅
CAS No.	646502-53-6
SMILES	CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(COC(N(C)[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N2[C@@]([C@H](OC)[C@@H](C)C(N[C@H](C)[C@@H](O)C3=CC=CC=C3)=O)([H])CCC2)=O)C)=O)=O)=O)C=C1)=O)=O)NC(CCCCCN4C(C=CC4=O)=O)=O
Storage	4°C, protect from light, stored under nitrogen
Shipping	Room temperature in continental US; may vary elsewhere