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Monomethyl auristatin E (GMP) refers to the GMP grade reagents of Monomethyl auristatin E. Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity.
Description | Monomethyl auristatin E (GMP) refers to the GMP grade reagents of Monomethyl auristatin E. Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity. |
In vitro | When coupled to cAC10, Monomethyl auristatin E shows selective cytotoxicity in CD30+ cells, and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. [1] When coupled to anti-CD79b antibody, anti–CD79b-vcMonomethyl auristatin E has very potent and broad activity across a large panel of NHL cell lines in vitro. [2] When coupled to anti-HER2 antibody, hertuzumab-vc-Monomethyl auristatin E can also be effectively internalized and potently kill HER2 over-expressing tumor cells. [3] |
In vivo | In the Karpas 299 ALCL model, cAC10-vcMonomethyl auristatin E (1 mg/kg, i.v.) induces complete, durable tumor regression, while free Monomethyl auristatin E (0.36 mg/kg) doesn't produce detectable antitumor activity. [1] In mouse xenograft models of NHL, anti–CD79b-vcMonomethyl auristatin E (7 mg/kg, p.o.) strikingly RESULTS in sustained complete tumor remission. [2] |
Molecular Weight | 717.98 |
Formula | C39H67N5O7 |
Cas No. | 474645-27-7 |
Relative Density. | 1.088 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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