Gedatolisib_product_DataBase

Bioactivity

Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively[1]. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2[2].

Invitro

Gedatolisib (PKI-587) 在使用 MDA-361 和 PC3-MM2 细胞系的细胞生长抑制试验中表现出良好的效力，IC50 分别为 4.0 和 13.1 nM[1]。 Gedatolisib 可有效抑制 MDA-361 肿瘤细胞中 PI3K/mTOR 信号通路蛋白的磷酸化。Gedatolisib (0.03-3 μM；4 小时) 阻止 Akt 在 Thr 308 处的磷酸化并在 30 nM 诱导裂解的 PARP[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Gedatolisib 相关抗体: Western Blot Analysis[1] Cell Line:

In Vivo

Gedatolisib（PKI-587；在第 1、5、9 天以 20 mg/kg 静脉注射）对小鼠 MDA-361 肿瘤表现出有效的抗肿瘤功效[1]。由于高血浆清除率 (7 mL/min/kg) 和静脉注射后的大分布体积 (分别为 7.2 L/kg)，Gedatolisib 表现出最终消除半衰期 (T1/2 14.4 h)。给药（25 mg/kg）雌性裸鼠[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

CAS

1197160-78-3

Formula

C32H41N9O4

Molar Mass

615.73

Appearance

固体

Transport

Room temperature in continental US; may vary elsewhere.

Storage

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

Reference

[1]. Venkatesan AM, et al. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem. 2010, 53(6), 2636-2645. [2]. Freitag H, et al. Inhibition of mTOR's Catalytic Site by PKI-587 Is a Promising Therapeutic Option for Gastroenteropancreatic Neuroendocrine Tumor Disease. Neuroendocrinology. 2017;105(1):90-104.

PeptideDB

Gedatolisib

CAS: 1197160-78-3 F: C32H41N9O4 W: 615.73