646502-53-6
646502-53-6 structure
- Name: VcMMAE
- Chemical Name: vc-mmae
- CAS Number: 646502-53-6
- Molecular Formula: C68H105N11O15
- Molecular Weight: 1316.626
- Catalog: Signaling Pathways Antibody-drug Conjugate Drug-Linker Conjugates for ADC
- Create Date: 2017-05-26 02:31:44
- Modify Date: 2024-01-02 22:49:14
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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).
| Name | vc-mmae |
|---|---|
| Synonyms |
L-Ornithinamide, N-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]-L-valyl-N-(aminocarbonyl)-N-[4-[(5S,8S,11S,12R)-12-[2-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1 -methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-oxoethyl]-4,10-dimethyl-5,8-bis(1-methylethyl)-11-[(1S)-1-methylpropyl]-3,6,9-trioxo-2,13-dioxa-4,7,10-triazatetradec-1-yl]phenyl]-
N-[6-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl]-L-valyl-N-{4-[(5S,8S,11S,12R)-11-[(2S)-2-butanyl]-12-(2-{(2S)-2-[(1R,2R)-3-{[(1S,2R)-1-hydroxy-1-phenyl-2-propanyl]amino}-1-methoxy-2-methyl-3-oxop ;ropyl]-1-pyrrolidinyl}-2-oxoethyl)-5,8-diisopropyl-4,10-dimethyl-3,6,9-trioxo-2,13-dioxa-4,7,10-triazatetradec-1-yl]phenyl}-N-carbamoyl-L-ornithinamide Vedotin Maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl-monomethyl auristatin E VcMMAE |
| 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). |
|---|---|
| Related Catalog | |
| 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]. |
| Cell Assay | 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. |
| Animal Admin | 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. |
| References |
[3]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1. |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 1347.6±65.0 °C at 760 mmHg |
| Molecular Formula | C68H105N11O15 |
| Molecular Weight | 1316.626 |
| Flash Point | 768.8±34.3 °C |
| Exact Mass | 1315.779175 |
| LogP | 6.04 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.556 |
| Storage condition | 2-8℃ |