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

Name: Gedatolisib
Brand: MedChemExpress
SKU: HY-10681
Rating: 5.0 (5 reviews)

Cat. No.: HY-10681 Purity: 99.89%: Data Sheet
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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.

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
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 5 publication(s) in Google Scholar

Other Forms of Gedatolisib:

5 Publications Citing Use of MCE Gedatolisib

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: Gedatolisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Combined Palbociclib- and Fulvestrant-resistant cells, M-S and T-S, and the corresponding resistant cells, MPF-R and TPF-R, were treated with different inhibitors of the PI3K/AKT/mTOR pathway including Alpelisib (HY-15244; Alp; 1 μM in M-S/MPF-R and 250 to 500 nM in T-S/TPF-R), Capivasertib (Cap; 250 to 500 nM in M-S/MPF-R and 100 nM in T-S/TPF-R), Sapanisertib (Sap; 10 nM in M-S/MPF-R and 5 nM in T-S/TPF-R), and Gedatolisib (HY-10681; Ged; 10 nM) in combination with Palbociclib (HY-50767; Palbo; 200 nM) and Fulvestrant (HY-13636; Fulv; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

: Gedatolisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Combined Palbociclib- and Fulvestrant-resistant cells (wild type ER+ breast cancer cells), ZPF-R, and the corresponding sensitive cells, Z-S, were treated with different inhibitors of PI3K/AKT/mTOR including Alpelisib (HY-15244; 6 μM), Capivasertib (50 nM), Sapanisertib (5 nM), and Gedatolisib (HY-10681; 5 nM) in combination with Palbociclib (HY-50767; 150 nM) and Fulvestrant (HY-13636; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

: Gedatolisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Triple combination with Gedatolisib (HY-10681), Palbociclib (HY-50767), and Fulvestrant (HY-13636) effectively inhibits growth of PIK3CA-mutant ER+ tumor xenografts resistant to combined palbociclib and fulvestrant. MPF-R cells (1 × 106) resistant to combined palbociclib and fulvestrant were injected into the mammary fat pads of NOG CIEA mice, and tumors were allowed to establish for 2 weeks to a size of ≈30 mm3. Mice were then treated with the combination of Fulvestrant (100 mg/kg, sc weekly), Palbociclib (25 mg/kg, oral gavage daily), and Capivasertib (100 mg/kg, oral gavage daily; n = 6) or Alpelisib (HY-15244; 25 mg/kg, oral gavage daily; n = 5). Tumor size was measured weekly. Average tumor growth curves measured weekly and Tumor volumes measured after excision.

: Gedatolisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Gedatolisib efficiently reduced the viability of ER+ PIK3CA- or AKT1-mutant breast cancer PDOs resistant to Abemaciclib. Dose-effect curves of CDK4/6i Abemaciclib, dual PI3K/mTORi Gedatolisib (HY-10681), PI3Ki Alpelisib (HY-15244), and dual mTORC1/2i Sapanisertib at day 7 of treatment in three breast cancer PDOs, PDO-P40, PDO-P46, and PDO-P48 (n = 3 biological replicates per group), developed from ER+ breast tumors and selected because of their differing IC50 toward Abemaciclib.

: Gedatolisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Effect of 1 μM Abemaciclib, Gedatolisib (HY-10681), Alpelisib (HY-15244), or Sapanisertib on viability of PDO-P40, PDO-P46, or PDO-P48 during 7 days of treatment. Data are presented as means ± SEM. Significant differences are calculated by one-way ANOVA test (*P < 0.05, **P < 0.01, and ***P < 0.001).

: Gedatolisib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]; The efficacy of Fulvestrant (Fulv, 100 nM), CDK4/6 inhibitor (CDK4/6i) Palbociclib (Palbociclib isothiocyanate; 200 nM) and the dual PI3K/mTOR inhibitor (PI3K/mTORi) Gedatolisib (10 nM) as single agents or in double and triple combination, was assessed in M-S and MPF-R cells by crystal violet growth assay performed over 6 days.

: Gedatolisib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]; The efficacy of Fulvestrant (Fulv, 100 nM), CDK4/6 inhibitor (CDK4/6i) Palbociclib (Palbociclib isothiocyanate; 200 nM) and the dual PI3K/mTOR inhibitor (PI3K/mTORi) Gedatolisib (10 nM) as single agents or in double and triple combination, was assessed in T-S and TPF-R cells by crystal violet growth assay performed over 6 days.

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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]
CNE-2	IC₅₀	2.97 μM Compound: PT-1	Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38661655]
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]
HCT-116	IC₅₀	0.98 μM Compound: PT-1	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38661655]
HeLa	IC₅₀	1.07 μM Compound: PT-1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38661655]
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]
HepG2	IC₅₀	3.6 μM Compound: PT-1	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38661655]
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]
L02	IC₅₀	4.38 μM Compound: PT-1	Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38661655]
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]
MCF7	IC₅₀	1.49 μM Compound: PT-1	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38661655]
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-231	IC₅₀	2.47 μM Compound: PT-1	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38661655]
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	4 nM Compound: 26, PKI-587	Cytotoxicity against human MDA-MB-361 cells Cytotoxicity against human MDA-MB-361 cells	[PMID: 20166697]
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]
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]
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:

H₂O : 20 mg/mL (32.48 mM; adjust pH to 2 with 1 M HCL)

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	0.1624 mL	0.8120 mL	1.6241 mL

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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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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.

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Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (274 KB) SDS (396 KB)

COA (245 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

H₂O	1 mM	1.6241 mL	8.1204 mL	16.2409 mL	40.6022 mL
	5 mM	0.3248 mL	1.6241 mL	3.2482 mL	8.1204 mL
	10 mM	0.1624 mL	0.8120 mL	1.6241 mL	4.0602 mL
	15 mM	0.1083 mL	0.5414 mL	1.0827 mL	2.7068 mL
	20 mM	0.0812 mL	0.4060 mL	0.8120 mL	2.0301 mL
	25 mM	0.0650 mL	0.3248 mL	0.6496 mL	1.6241 mL
	30 mM	0.0541 mL	0.2707 mL	0.5414 mL	1.3534 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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)

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5 Publications Citing Use of MCE Gedatolisib

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Complete Stock Solution Preparation Table

Gedatolisib Related Classifications

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