Tarlatamab  (Synonyms: 塔拉妥单抗; AMG-757)

Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the K_Ds of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the K_Ds of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research^[1].

(scFv-heavy-kappa)-(scFv-heavy-lambda)-scFc

Chimeric; Humanized

Tarlatamab (AMG-757; 0-10 nM; 48 小时) 在体外对表达 DLL3 的 SCLC 细胞系具有有效的特异性细胞毒活性^[1]。
Tarlatamab (0-10 nM; 4-72 小时) 随时间增加颗粒酶 B 水平和细胞毒性，在 48 小时观察到最大信号。T 细胞活化或炎症标志物 CD69、CD71、PD-1 和 PD-L1 (37-39) 被上调^[1]。

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

Tarlatamab (AMG-757; 3 mg/kg; 腹腔给药; 每周一次; 连续三周) 在 SCLC 小鼠模型中驱动肿瘤消退^[1]。
Tarlatamab (12 μg/kg; 腹腔给药; 单剂量) 在非人灵长类动物 (NHP) 的平均半衰期为 234 小时 (9.8 天)，平均清除率为 0.487 mL/hour/kg，稳态分布容积为 146 mL/kg^[1]。

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

2307488-83-9

液体

Colorless to light yellow

塔拉妥单抗

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

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  (scFv-heavy-kappa)-(scFv-heavy-lambda)-scFc

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  Flow cytometry analysis of DLL3 overexpression HEK293 cells labelling DLL3 with Tarlatamab at 142nM (Red). Goat anti human IgG Fc(Alexa Fluor488) was used as the secondary antibody at 1/400 dilution. Isotype control - human IgG (Blue). Unlabeled control - Unlabelled cells (Red).
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  Flow cytometry analysis of Jurkat cells labelling CD3 with Tarlatamab at 142nM (Red). Goat anti human IgG Fc (Alexa Fluor488) was used as the secondary antibody at 1/400 dilution. Isotype control - human IgG (Blue). Unlabeled control - Unlabelled cells (Gray).

• [1]. Michael J Giffin, et al. AMG 757, a Half-Life Extended, DLL3-Targeted Bispecific T-Cell Engager, Shows High Potency and Sensitivity in Preclinical Models of Small-Cell Lung Cancer. Clin Cancer Res. 2021 Mar 1;27(5):1526-1537.  [Content Brief]