D8-MMAE - CAS 2070009-72-0

D8-MMAE - CAS 2070009-72-0 Catalog number: BADC-00635

* Please be kindly noted products are not for therapeutic use. We do not sell to patients.

D8-MMAE is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.

General Information

ADCs Cytotoxin
Product Name
Catalog Number
Molecular Formula
Molecular Weight

Chemical Structure

  • D8-MMAE
D8-Monomethyl auristatin E; (2S)-2,3,4,4,4-pentadeuterio-N-[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]-3-(trideuteriomethyl)butanamide
Room temperature
Canonical SMILES
InChI Key
1.Intracellular Released Payload Influences Potency and Bystander-Killing Effects of Antibody-Drug Conjugates in Preclinical Models
Li F, Emmerton KK, Jonas M, Zhang X, Miyamoto JB, Setter JR, Nicholas ND, Okeley NM, Lyon RP, Benjamin DR, Law CL
Antibody-drug conjugates (ADC) comprise targeting antibodies armed with potent small-molecule payloads. ADCs demonstrate specific cell killing in clinic, but the basis of their antitumor activity is not fully understood. In this study, we investigated the degree to which payload release predicts ADC activity in vitro and in vivo ADCs were generated to target different receptors on the anaplastic large cell lymphoma line L-82, but delivered the same cytotoxic payload (monomethyl auristatin E, MMAE), and we found that the intracellular concentration of released MMAE correlated with in vitro ADC-mediated cytotoxicity independent of target expression or drug:antibody ratios. Intratumoral MMAE concentrations consistently correlated with the extent of tumor growth inhibition in tumor xenograft models. In addition, we developed a robust admixed tumor model consisting of CD30(+) and CD30(-) cancer cells to study how heterogeneity of target antigen expression, a phenomenon often observed in cancer specimens, affects the treatment response. CD30-targeting ADC delivering membrane permeable MMAE or pyrrolobenzodiazepine dimers demonstrated potent bystander killing of neighboring CD30(-) cells. In contrast, a less membrane permeable payload, MMAF, failed to mediate bystander killing in vivo, suggesting local diffusion and distribution of released payloads represents a potential mechanism of ADC-mediated bystander killing. Collectively, our findings establish that the biophysical properties and amount of released payloads are chief factors determining the overall ADC potency and bystander killing. Cancer Res; 76(9); 2710-9.

View All ADCs Cytotoxin Sort Specific Products

View All ADCs Cytotoxin with Linkers Sort Specific Products

View All ADCs Linker Sort Specific Products

Related Products

Get in Touch

Verification code
Historical Records: D8-MMAF hydrochloride | Val-cit-PAB-OH | 2,5-Dioxopyrrolidin-1-yl 3-((2-Fluorobenzyl)oxy)propanoate | DBCO-SS-aldehyde | Apaziquone | Val-Cit-PAB-MMAE | Mal-PEG2-NHS | t-Boc-N-amido-PEG1-NHS ester | Benzoylheteratisine hydrochloride | Aceclidine Salicylic Acid | D8-MMAE
Inquiry Basket