2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
HER1
In Vivo
Laprituximab emtansine (1-5 mg/kg, intravenous injection) leads to tumor regression in an EGFR-positive SCCHN xenograft model [4]. The compound demonstrated minimal efficacy at a dose of 1 mg/kg and showed highly active results at doses of 2.5 and 5 mg/kg.
In Vitro
Laprituximab emtansine exhibits anti-clonogenic and anti-proliferative activities against HNSCC cell lines, with IC50 values ranging from 0.003 nM to 1.74 nM [3]. Laprituximab emtansine also demonstrates cytotoxicity against NSCLC cell lines and EGFR-mutant HCC827 cell lines [2]. In a Cell Viability Assay [3], using PBMCs from humans, rhesus monkeys, and cynomolgus monkeys, the compound inhibited rCD154-induced proliferation of PBMCs with IC50 values of approximately 0.02 μg/mL, 0.03 μg/mL, and 0.01 μg/mL, respectively.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Moradi-Kalbolandi S, et al. Monoclonal antibody-based therapeutics, targeting the epidermal growth factor receptor family: from herceptin to Pan HER. J Pharm Pharmacol. 2018 Jul;70(7):841-854.
[2]. Yulius Y. et al. Abstract 4513: IMGN289, an EGFR-targeting antibody-drug conjugate, is effective against tumor cells that are resistant to EGFR tyrosine kinase inhibitors. Cancer Res 1 October 2014; 74 (19_Supplement): 4513.
[3]. Hyunseok Kang, et al. Antitumor effect of IMGN289, an anti-EGFR antibody-drug conjugate (ADC), in preclinical models of head and neck squamous cell carcinomas (HNSCC). Journal of Clinical Oncology. 2014. 32, no. 15_suppl.
[4]. Jose F. Ponte, et al. Abstract 5483: Preclinical evaluation of IMGN289, an anti-EGFR antibody-maytansinoid conjugate for the treatment of squamous cell carcinoma of the head and neck. Cancer Res (2013) 73 (8_Supplement): 5483.
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