SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC₅₀s 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^[1].

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^[1].

上海金畔生物科技有限公司 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 IC₅₀ for almost 4 h after oral dosing^[1].
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^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

354.33

C₁₆H₁₇F₃N₄O₂

1884222-74-5

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 125 mg/mL (352.78 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.87 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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):14609-14625