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VcMMAE is a MMAE derivative with valine-citrulline (Vc) linker. 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. 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.
*The compound is unstable in solutions, freshly prepared is recommended
| Cell Experiment | |
|---|---|
| Cell lines | GIST-48B cells |
| Preparation method | KIT-negative GIST-48B cells was chosen as the negative control, and GIST-T1 and GIST-430/654 cells were chosen as positive cells. Results show that KIT-d-MMAE demonstrated notably lower IC50 values than VcMMAE and Lib-MMAE in GIST-T1 and GIST-430/654, but higher IC50 values in GIST-48B. |
| Concentrations | 0 - 10 nM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c nude mice |
| Formulation | DPBS |
| Dosages | 4 mg/kg |
| Administration | Tail vein injection |
| Molecular Weight | 1316.63 |
| Formula | C68H105N11O15 |
| CAS Number | 646502-53-6 |
| Solubility (25°C) | DMSO: ≥ 42 mg/mL |
| Storage | 4°C, protect from light, dry, sealed |
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