Gedatolisib(Synonyms: PKI-587; PF-05212384)

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Gedatolisib (Synonyms: PKI-587; PF-05212384) 纯度: 99.68%

Gedatolisib (PKI-587) 是一种高效的双重 PI3Kα，PI3Kγ 和 mTOR 抑制剂, IC50 分别为 0.4 nM，5.4 nM 和 1.6 nM。Gedatolisib 在 mTOR 复合物 mTORC1 和 mTORC2 中同样有效。

Gedatolisib(Synonyms: PKI-587; PF-05212384)

Gedatolisib Chemical Structure

CAS No. : 1197160-78-3

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5 mg ￥990 In-stock
10 mg ￥1700 In-stock
50 mg ￥4900 In-stock
100 mg ￥8500 In-stock
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生物活性

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].

IC50 & Target[1][3]

PI3Kα

0.4 nM (IC50)

PI3Kα-H1047R

0.6 nM (IC50)

PI3Kα-E545K

0.6 nM (IC50)

PI3Kγ

5.4 nM (IC50)

PI3Kβ

6 nM (IC50)

PI3Kδ

6 nM (IC50)

mTOR

1.6 nM (IC50)

mTORC1

 

mTORC2

 

体外研究
(In Vitro)

Gedatolisib (PKI-587) shows good potency in cell growth inhibition assays using MDA-361 and PC3-MM2 cell lines with IC50s of 4.0 and 13.1 nM, respectively[1].
Gedatolisib shows potent suppression of phosphorylation of PI3K/mTOR signaling pathway proteins in MDA-361 tumor cells. Gedatolisib (0.03-3 μM; 4 hours) prevents the phosphorylation of Akt at Thr 308 and induces cleaved PARP at 30 nM[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.

Western Blot Analysis[1]

Cell Line: MDA-361 tumor cells
Concentration: 0.03, 0.1, 0.3, 1, and 3 μM
Incubation Time: 4 hours
Result: Prevented the phosphorylation of Akt (pAkt) at threonine 308 (T308; IC50=8 nM).

体内研究
(In Vivo)

Gedatolisib (PKI-587; administered i.v. at 20 mg/kg on days 1, 5, 9) exhibits potent antitumor efficacy against MDA-361 tumors in mice[1].
Gedatolisib exhibits terminal elimination half-life (T1/2 14.4 h) due to high plasma clearance (7 mL/min/kg) combined with large volumes of distribution (7.2 L/kg respectively) following i.v. administration (25 mg/kg) female nude mice[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.

Animal Model: Female nude mice bearing MDA-361 xenograft model[1].
Dosage: 20 mg/kg
Administration: Administered i.v. at 20 mg/kg on an intermittent regimen (days 1, 5, 9).
Result: Caused regression of large staged (~900 mm3) tumors.
The minimum efficacious dose (MED) was determined to be 3 mg/kg against MDA-361 tumors and maximum tolerated single dose (MTD) was determined to be 30 mg/kg.

分子量

615.73

Formula

C32H41N9O4
CAS 号

1197160-78-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO : 4 mg/mL (6.50 mM; Need warming)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6241 mL 8.1204 mL 16.2409 mL
5 mM 0.3248 mL 1.6241 mL 3.2482 mL
10 mM — — —

参考文献

  • [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.

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