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抑制剂/激活剂

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凋亡与自噬

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SAR405

SAR405 是一种低分子量的PIK3C3/Vps34抑制剂（Kd=1.5 nM），具有高选择性，在浓度高达10 μM时，对I类和Ⅱ类PI3Ks及mTOR没有活性。SAR405 可防止自噬并与肿瘤细胞MTOR (mechanistic target of rapamycin) 的抑制作用发挥协同作用。

货号：
TK0165
规格：

2mg

5mg
价格：
￥0.00

产品参数

CAS No.	1523406-39-4
生物活性	SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.
分子式	C19H21ClF3N5O2
分子量	443.85
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : ≥ 27 mg/mL (60.83 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
体外研究	The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line. SAR405 prevents autophagy and synergizes with mTOR inhibition in tumor cells. SAR405 prevents autophagosome formation with an IC50 of 42 nM. Treatment of starved cells with SAR405 completely inhibits the conversion to LC3-II in a dose-dependent manner. The effect of SAR405 on autophagy is then investigated. The GFP-LC3 model is used for the HTS and confirmed its activity on starved cells (IC50=419 nM). The conversion of LC3-I into LC3-II is also analyzed by western blotting on wild-type HeLa and H1299 cells.
文献	暂无相关参考文献
纯度及产品资料	98%

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