1. PI3K/Akt/mTOR
  2. PI3K
    mTOR
  3. Gedatolisib

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

Cat. No.: HY-10681 Purity: 99.68%
Handling Instructions

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. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2.

For research use only. We do not sell to patients.

Gedatolisib Chemical Structure

Gedatolisib Chemical Structure

CAS No. : 1197160-78-3

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10 mM * 1 mL in DMSO Get quote
5 mg USD 108 Get quote
10 mg USD 192 Get quote
50 mg USD 552 Get quote
100 mg USD 1020 Get quote

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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]. 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

 

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].

MCE 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).
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].

MCE 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.
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 --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
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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