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

Name: Gedatolisib
Brand: MedChemExpress
SKU: HY-10681
Rating: 5.0 (4 reviews)

Cat. No.: HY-10681 Purity: 99.68%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 1197160-78-3

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Gedatolisib

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mTOR mTORC1 mTORC2

Biological Activity
Purity & Documentation
References
Customer Review

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

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.06 μM Compound: 6aa	Antiproliferative activity against human A431 cells harboring wild type EGFR mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A431 cells harboring wild type EGFR mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
BaF3	IC₅₀	0.1 μM Compound: 6aa	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
CNE-2	IC₅₀	0.2 μM Compound: 6aa	Antiproliferative activity against human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HCT-116	IC₅₀	0.51 μM Compound: 6aa	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HeLa	IC₅₀	5.51 μM Compound: 6aa	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HepG2	IC₅₀	14.76 μM Compound: 6aa	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
L02	IC₅₀	27.33 μM Compound: 6aa	Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MCF7	IC₅₀	0.37 μM Compound: 6aa	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MDA-MB-231	IC₅₀	1.08 μM Compound: 6aa	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MDA-MB-361	IC₅₀	< 10 nM Compound: 26, PKI-587	Inhibition of Akt S473 phosphorylation in human MDA-MB-361 cells by Western blotting Inhibition of Akt S473 phosphorylation in human MDA-MB-361 cells by Western blotting	[PMID: 20166697]
MDA-MB-361	IC₅₀	3 nM Compound: 1, PKI-587	Growth inhibition of human MDA-MB-361 cells after 72 hrs Growth inhibition of human MDA-MB-361 cells after 72 hrs	[PMID: 21763134]
MDA-MB-361	IC₅₀	8 nM Compound: 26, PKI-587	Inhibition of Akt T308 phosphorylation in human MDA-MB-361 cells by Western blotting Inhibition of Akt T308 phosphorylation in human MDA-MB-361 cells by Western blotting	[PMID: 20166697]
NCI-H1975	IC₅₀	0.115 μM Compound: 6aa	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
PC-3	IC₅₀	11 nM Compound: 1, PKI-587	Growth inhibition of human PC3 cells after 72 hrs Growth inhibition of human PC3 cells after 72 hrs	[PMID: 21763134]
Sf9	IC₅₀	0.4 nM Compound: 1, PKI-587	Inhibition of human PI3Kalpha expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay Inhibition of human PI3Kalpha expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay	[PMID: 21763134]
Sf9	IC₅₀	11 nM Compound: 1, PKI-587	Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay	[PMID: 21763134]

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].

MedChemExpress (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 (T_1/2 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].

MedChemExpress (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

Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (245 KB) LCMS (122 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6241 mL	8.1204 mL	16.2409 mL	40.6022 mL
DMSO	5 mM	0.3248 mL	1.6241 mL	3.2482 mL	8.1204 mL

Gedatolisib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gedatolisib1197160-78-3PKI-587 PF-05212384PKI587PKI 587PF05212384PF 05212384PF-05212384PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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

Customer Review

Gedatolisib Related Antibodies

4 Publications Citing Use of MCE Gedatolisib

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Biological Activity

Purity & Documentation

References

Customer Review

Gedatolisib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Gedatolisib Related Classifications

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