Molecular Formula | C68H105N11O15 |
Molar Mass | 1316.63 |
Density | 1.196±0.06 g/cm3(Predicted) |
Boling Point | 1347.6±65.0 °C(Predicted) |
Solubility | DMSO: ≥ 54 mg/mL |
pKa | 13.29±0.70(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Physical and Chemical Properties | Bioactive VcMMAE (mc-vc-PAB-MMAE), an MMAE derivative with a valine-citrulline (Vc) linker, is a antibody-drug conjugate (ADC) with antitumor activity. MMAE is a synthetic anti-tumor drug, which can be effectively released from VcMMAE in vitro and exert cytotoxic activity. |
Use | Product Description VcMMAE (mc-vc-PAB-MMAE) is a biochemical reagent, which is part of the antibody drug complex (drug-linker conjugate for ADC) and has anti-cancer activity. It is formed by connecting MMAE (a tubulin inhibitor) and Vc. |
In vitro study | 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. 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. |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.76 ml | 3.798 ml | 7.595 ml |
5 mM | 0.152 ml | 0.76 ml | 1.519 ml |
10 mM | 0.076 ml | 0.38 ml | 0.76 ml |
5 mM | 0.015 ml | 0.076 ml | 0.152 ml |
application
VcMMAE(mc-vc-PAB-MMAE) is the drug linkers conjugate of ADC, through the use of the anti-mitotic agent monomethyl auristatin E(MMAE, tubulin inhibitor), a dipeptide cleavable by lysosomes, valine-citrulline (vc).
in vitro action
Monomethylotatin E(MMAE) can be effectively released from SGN-35 in CD30 cancer cells, and due to its membrane permeability, it can exert cytotoxic activity on bystander cells. MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose-dependent manner associated with mitotic block. Radiosensitization was demonstrated by decreased clonal formation survival and increased DNA double-strand breaks after radiotherapy.
in vivo action
The combination of monomethylatorvastatin E(MMAE) and IR will cause tumor growth delay. In xenograft models, ACPP-cRGD-MMAE targeting tumors with IR will produce more stable and significantly prolonged tumor regression.
application
VcMMAE(mc-vc-PAB-MMAE) is the drug linker conjugate of ADC, through the use of the anti-mitotic agent monomethyl auristatin E(MMAE, tubulin inhibitor), a dipeptide cleavable by lysosomes, valine-citrulline (vc).
in vitro action
Monomethylotatin E(MMAE) can be effectively released from SGN-35 in CD30 cancer cells, and due to its membrane permeability, it can exert cytotoxic activity on bystander cells. MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose-dependent manner associated with mitotic block. Radiosensitization was demonstrated by decreased clonal formation survival and increased DNA double-strand breaks after radiotherapy.
in vivo action
The combination of monomethylatorvastatin E(MMAE) and IR will cause tumor growth delay. In xenograft models, ACPP-cRGD-MMAE targeting tumors with IR will produce more stable and significantly prolonged tumor regression.