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  3. Gedatolisib

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

目录号: HY-10681 纯度: 99.68%
产品使用指南

Gedatolisib (PKI-587) 是一种高效的双重 PI3KαPI3KγmTOR 抑制剂, IC50 分别为 0.4 nM,5.4 nM 和 1.6 nM。PKI-587 在 mTOR 复合物 mTORC1mTORC2 中同样有效。

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Gedatolisib Chemical Structure

Gedatolisib Chemical Structure

CAS No. : 1197160-78-3

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Description

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]. PKI-587 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

 

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].

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).
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].

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.
Clinical Trial
Molecular Weight

615.73

Formula

C₃₂H₄₁N₉O₄

CAS No.

1197160-78-3

SMILES

CN(C1CCN(C(C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=NC(N6CCOCC6)=N4)C=C3)=O)C=C2)=O)CC1)C

Shipping

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
Solvent & Solubility
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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 --- --- ---
*

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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。

References

Purity: 99.68%

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Keywords:

GedatolisibPKI-587 PF-05212384PKI587PKI 587PF05212384PF 05212384PF-05212384PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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