Laprituximab emtansine

Names

[ CAS No. ]:
1622327-37-0

[ Name ]:
Laprituximab emtansine

Biological Activity

[Description]:

Laprituximab emtansine (IMGN-289) is an immunotoxin targeting HER1. Laprituximab emtansine is an EGFR antibody-drug conjugate (ADC) consisting of the J2898A antibody, DM1 (anti-microtubule agent) and the SMCC thioether linker. Laprituximab emtansine can be used for cancer research[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

HER1


[In Vitro]

Laprituximab emtansine 显示出对 HNSCC 细胞系的抗克隆形成和抗增殖活性，IC50s 为 0.003 nM-1.74 nM[3]。 Laprituximab emtansine 对 NSCLC 细胞系和 EGFR 突变 HCC827 细胞系具有细胞毒性[2]。 Cell Viability Assay[3] Cell Line: PBMCs from humans, rhesus and cynomolgus animals Concentration: 0-1 μg/mL approximately Incubation Time: 3 days Result: Inhibited rCD154-induced proliferation of PBMCs with IC50s of 0.02, 0.03, and 0.01 μg/mL, respectively.

[In Vivo]

Laprituximab emtansine (1-5 mg/kg，静脉注射) 在 EGFR 阳性 SCCHN 异种移植模型中导致肿瘤消退[4]。 Animal Model: EGFR-positive SCCHN xenograft model[4] Dosage: 1, 2.5, 5 mg/kg Administration: i.v. Result: Resulted tumor regression with a minimally efficacious dose of 1 mg/kg, and highly active at 2.5 and 5 mg/kg.

[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.

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds