Eftozanermin alfa  (Synonyms: ABBV-621)

Eftozanermin alfa (ABBV-621) is a tumor necrosis factor-related apoptosis-inducing ligand receptor (TRAIL-R) agonist. Eftozanermin alfa is a fusion protein consisting of a mutant immunoglobulin G1-Fc linked to 2 single-chain trimers of TRAIL. Eftozanermin alfa induces apoptosis in tumor cells by activation of death receptors (DR4 receptor and DR5 receptor) with K_ds of 780 nM and 635 nM. Eftozanermin alfa can be used for the research of multiple solid and heme malignancies^[1][2][3].

Eftozanermin alfa 在急性髓系白血病细胞系中与 Venetoclax (HY-15531) 和蛋白酶体抑制剂 (Bortezomib (HY-10227) 或 Carfilzomib (HY-10455)) 联合使用时，表现出高度显著的协同作用^[1][2]。
Eftozanermin alfa (0-1 nM, 24 h) 通过凋亡途径 (增加caspase-3/7/8 活性) 对 36% (45/126) 的人类实体瘤细胞具有杀伤作用^[1][3]。

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

Eftozanermin alfa (1 mg/kg，腹腔注射，隔日一次，连续 5 天) 在小鼠中诱导强大的单药抗 SKM-1 肿瘤活性^[1]。
Eftozanermin alfa (5 mg/kg，腹腔注射，隔日一次，连续 5 天) 在患者来源的异种移植瘤 (PDX) 小鼠模型中表现出显著而广泛的抗肿瘤活性^[3]。
Eftozanermin alfa (0.3-30 mg/kg，腹腔注射，隔日一次，连续 5 天) 在小鼠中表现出明显的剂量依赖性抗结直肠癌和乳腺癌活性^[3]。
Eftozanermin alfa (3-15 mg/kg，腹腔注射，每两天一次或每周 2-5 次) 在小鼠实验中与 Irinotecan (HY-16562)、Docetaxel (HY-B0011) 或 A-1331852 (HY-19741) 联用时表现出显著更高的抗肿瘤疗效^[3]。
依托扎纳明 (Eftozanermin alfa) (4-100 mg/kg，静脉注射，每周一次，共 5 周) 在食蟹猴中表现出良好的药代动力学特征和较宽的治疗窗^[3]。

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

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

167.52 kDa

1820660-69-2

液体

Colorless to light yellow

Shipping with dry ice.

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

• 
  [Homo sapiens TNFSF10 (TNF superfamily member 10, tumor necrosis factor (ligand)superfamily, member 10)]2-Homo sapiens IGHG1 Fc (Fragment constant)

• 
  Immobilized Human DR5/TRAIL R2 Protein (His Tag) can bind Eftozanermin alfa. The EC₅₀ for this effect is 4.94 ng/mL.

• [1]. Tahir SK, et al. Activity of eftozanermin alfa plus venetoclax in preclinical models and patients with acute myeloid leukemia. Blood. 2023 Jan 30:blood.2022017333.  [Content Brief]

  [2]. Silva A S, et al. Ex Vivo Drug Sensitivity and Functional Genomics Platform Identifies Novel Combinations Targeting Intrinsic and Extrinsic Apoptotic Signaling Pathways in Multiple Myeloma. Blood, 2020, 136(Supplement 1):49-50.

  [3]. Phillips DC, et al. Hexavalent TRAIL Fusion Protein Eftozanermin Alfa Optimally Clusters Apoptosis-Inducing TRAIL Receptors to Induce On-Target Antitumor Activity in Solid Tumors. Cancer Res. 2021 Jun 15;81(12):3402-3414.  [Content Brief]