Naratuximab emtansine  (Synonyms: IMGN529; Debio 1562)

Naratuximab emtansine (IMGN529) is a CD37-targeted ADC consisting of a humanized IgG1 mAb coupled to the microtubule disruptor DM1. Naratuximab emtansine has high affinity and specificity for CD37, allowing ADC internalization, processing and intracellular release of DM1. Due to its ability to disrupt microtubule assembly, DM1 can subsequently induce cell cycle arrest and apoptosis^[1].

Naratuximab emtansine (IMGN529) (0.125 nM, 24 h) treatment alone induces activation of cystein 3/7 in DLBCL cell lines and this effect is significantly enhanced in the presence of rituximab (2 nM), which further induces an increase in cleaved PARP levels^[1].
Naratuximab emtansine (IMGN529) (0-3 ng/mL) shows dose-dependent antibody-dependent cell-mediated cytotoxicity (ADCC) activity against U-2932 and SU-DHL-4 cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Naratuximab emtansine (IMGN529) (10 mg/kg, a single bolus) monotherapy is inactive against U-2932 tumor and when combined with rituximab significantly enhances anti-tumor activity and no significant toxicity or weight loss is observed over the course of the study in female CB.17-SCID mice with U2932^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1607824-64-5

[Naratuximab emtansine]

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• [1]. Stuart W Hicks, et al. The Antitumor Activity of IMGN529, a CD37-Targeting Antibody-Drug Conjugate, Is Potentiated by Rituximab in Non-Hodgkin Lymphoma Models. Neoplasia. 2017 Sep;19(9):661-671.  [Content Brief]