PDK-IN-1_product_DataBase

Bioactivity	PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass[1].
Target	IC50: 0.03 ± 0.005 μM (PDK1); 0.1 μM (HSP90)
Invitro	PDK-IN-1 (compound 7o) 对 PSN-1 和 BxPC-3 胰腺细胞系显示出 2D 细胞毒活性，IC50 值分别为 0.1 ± 0.04 和 1.0 ± 0.2 μM。 PDK-IN-1 还显示出 3D 细胞毒活性，IC50 值分别为 3.3 ± 0.2 和 11.9 ± 1.1 μM[1]。
In Vivo	PDK-IN-1 (compound 7o) (20 mg/kg，腹腔注射，每天一次) 在减少肿瘤质量方面比顺铂 (HY-17394) 略微更有效[1]。PDK-IN-1 显著降低 Lewis 肺癌 (LLC) 小鼠的 PDH 磷酸化[1]。 Animal Model:
Name	PDK-IN-1
CAS	2897696-10-3
Formula	C20H16BrN7O
Molar Mass	450.29
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Pecoraro C, et al. 1,2,4-Amino-triazine derivatives as pyruvate dehydrogenase kinase inhibitors: Synthesis and pharmacological evaluation. Eur J Med Chem. 2023 Mar 5;249:115134.

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