SBP-7455 是一种有效的，高亲和力，具有口服活性的双重 ULK1/ULK2 自噬抑制剂，在 ADP-Glo 分析中的 IC₅₀ 分别为 13 nM 和 476 nM。SBP-7455 有效抑制 ULK1/2 酶活性，并可用于三阴性乳腺癌 (TNBC) 的研究。

SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC 50 s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research.

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ULK1 13 nM (IC50) ULK2 476 nM (IC50

SBP-7455 (compound 26; 72 h) treatment inhibits cell growth with an IC50 of 0.3 μM for MDA-MB-468 cells. SBP-7455 inhibits starvation-induced autophagic flux in TNBC cells that are dependent on autophagy for survival. has not independently confirmed the accuracy of these methods. They are for reference only.

A single dose of SBP-7455 (compound 26) (30 mg/kg) is orally administered to mice. The T max for SBP-7455 is approximately 1 h, the C max is 990 nM and the T 1/2 is 1.7 h. The plasma concentration of SBP-7455 remains above the ULK1 IC 50 for almost 4 h after oral dosing.
The mice are dosed with SBP-7455 (compound 26) (10 mg/kg) by oral gavage, and liver samples were collected after 2 h. The results reveals robust inhibition of pATG13 (Ser318), as well as downregulation of total ATG13 and ULK1 levels by SBP-7455. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Huiyu Ren, et al. Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer. J Med Chem. 2020 Dec 10;63(23):1460

In Vitro: DMSO : 125 mg/mL (352.78 mM; Need ultrasonic)配制储备液