| MDL | MFCD25372036 |
|---|---|
| Molecular Weight | 1316.63 |
| Molecular Formula | C68H105N11O15 |
| 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 |
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
|
Auristatin |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
-20°C, sealed storage, away from moisture and light
* The compound is unstable in solutions, freshly prepared is recommended.
DMSO : ≥ 54 mg/mL ( 41.01 mM )
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
* "≥" means soluble, but saturation unknown.
| 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 |
VcMMAE is dissolved in DMSO and then diluted with 0.9% NaCl [3] .