Idactamab (INT-001) is an IgG1-κ antibody with in vivo activity across a spectrum of hematological malignancies. Idactamab can be used for prepare MEDI7247, a potent and specific ADC, targeting ASCT2 (SLC1A5)[1][2].
Idactamab 对不同血红素癌症细胞系具有抑制作用，IC50 为 0.05-65 ng/mL[1]。
ASCT2 (SLC1A5) 是一种多通道、Na+ 依赖的中性氨基酸转运体，介导肿瘤生长和进展所需氨基酸的摄取[1]。
Idactamab 能够提高 3 种播散性急性髓性白血病 (AML) 细胞系模型:TF1α (ASCT2 高表达)、MOLM-13 (ASCT2 低表达) 和 M.V.411 (ASCT2 高表达) 的生存率，对应的最低抑制浓度分别为 0.05 mg/kg，0.1 mg/kg，和 0.1 mg/kg[2]。
[1]. Pore N, et al. Discovery and development of MEDI7247, a novel pyrrolobenzodiazepine (PBD)-based antibody drug conjugate targeting ASCT2, for treating hematological cancers[J]. Blood, 2018, 132: 4071.
[2]. Monks N R, et al. Abstract LB-295: MEDI7247, a novel pyrrolobenzodiazepine ADC targeting ASCT2 with potent in vivo activity across a spectrum of hematological malignancies[J]. Cancer Research, 2018, 78(13_Supplement): LB-295-LB-295.