AZD0095

Names

[ Name ]:
AZD0095

Biological Activity

[Description]:

AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205)[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monocarboxylate Transporter

Research Areas >> Cancer

[Target]

MCT4:1.3 nM (IC50)

[In Vitro]

AZD0095 (0-50 µM) 抑制 NCI-H358 细胞 (MCT4 高表达) 的增殖，IC50 为 26 nM[1]。

[In Vivo]

AZD0095 (100 mg/kg, 口服，一天两次) 与 Cediranib (HY-10205) 联合使用抑制小鼠 NCI-H358 异种移植肿瘤的生长[1]。 Animal Model: Murine NCI-H358 xenograft[1] Dosage: 100 mg/kg together with Cediranib (3 mg/kg) Administration: Oral administration (p.o.) Result: Reduced tumor growth more efficiently than AZD0095 or AZD2171 alone.

[References]

[1]. Goldberg FW, et al. Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology. J Med Chem. 2022 Dec 16.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₃₂N₈O₂

[ Molecular Weight ]:
500.60

Related Compounds

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