SBP-7455 是一种高亲和力,可口服的双重ULK1/ULK2自噬抑制剂,可有效抑制ULK1/2酶活性,可研究三阴性乳腺癌,在 ADP-Glo 分析中的IC50分别为 13 nM 和 476 nM。
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SBP-7455 potently inhibited ULK1/2 enzymatic activity in vitro and in cells, reduced the viability of TNBC cells and had oral bioavailability in mice.
体外活性
SBP-7455 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[1].
体内活性
To evaluate the PD profile and in vivo target engagement, mice were dosed with SBP-7455 (10 mg/kg) or vehicle by oral gavage, and liver samples were collected after 2 h.Based on the PK and PD profiles, our data show that SBP-7455 is an efficacious tool that can be used to modulate autophagy in vivop[1].
Cas No.
1884222-74-5
分子式
C16H17F3N4O2
分子量
354.333
储存和溶解度
DMSO:120mg/mL (338.67 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years