Conatumumab

Names

[ Name ]:
Conatumumab

[Synonym ]:
4-Chloro-2-[(2-furylmethyl)amino]-5-sulfamoylbenzoic acid - 1,3-dipropyl-8-(tricyclo[3.3.1.03,7]non-3-yl)-3,7-dihydro-1H-purine-2,6-dione (1:1)
Benzoic acid, 5-(aminosulfonyl)-4-chloro-2-[(2-furanylmethyl)amino]-, compd. with 8-(hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione (1:1)

Biological Activity

[Description]:

Conatumumab (AMG 655) is a human monoclonal agonist antibody against human death receptor 5 (DR5, TRAILR2) (Kd: 1 nM for the long form of DR5, 0.8 nM for the short form of DR5). Conatumumab induces apoptosis via caspase activation. Conatumumab can be used in the research of cancers. [1][2][3].

[Related Catalog]:

Research Areas >> Cancer

[Target]

IC50: DR5 (<1 nM)[2]

[In Vitro]

Conatumumab (0-10 μg/mL，4 小时) 激活 Colo205、H-2122 和 MiaPaCa2 细胞中的 caspase-3/7[2]。 Conatumumab (0-10 μg/mL，24 小时) 降低敏感肿瘤细胞系 (Colo205、H-2122 和 MiaPaCa2 细胞) 的细胞活力[2]。 Cell Viability Assay[2] Cell Line: Colo205, H-2122, and MiaPaCa2 cells Concentration: 0-10 μg/mL Incubation Time: 24 h Result: Dose-dependently inhibited cell viability.

[In Vivo]

Conatumumab (0-100 μg，腹腔注射，每周两次) 抑制 Colo205、H2122 或 MiaPaCa2/T2 异种移植肿瘤的小鼠的肿瘤生长[2]。 Conatumumab (2.5 μg，i.p.，每周 3 次) 增强化疗药物 (CPT11，HY- 16562) (80 mg/kg) 在 Colo 205 移植瘤中的抗肿瘤活性[2]。 Animal Model: Mice bearing Colo205, H2122, or MiaPaCa2/T2 xenograft tumors[2] Dosage: 0, 0.1, 0.3, 1, 3, 10, 30, 100 μg Administration: Intraperitoneal injection (i.p.), twice weekly. Result: Dose-dependently inhibited tumor growth. Induced caspase-3 activation in tumors (determined by IHC).

[References]

[1]. Herbst RS, et al. A first-in-human study of conatumumab in adult patients with advanced solid tumors. Clin Cancer Res. 2010 Dec 1;16(23):5883-91.

[2]. Kaplan-Lefko PJ, et al. Conatumumab, a fully human agonist antibody to death receptor 5, induces apoptosis via caspase activation in multiple tumor types. Cancer Biol Ther. 2010 Apr 15;9(8):618-31.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₃₉ClN₆O₇S

[ Molecular Weight ]:
687.206

[ Exact Mass ]:
686.228943

Related Compounds

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