Cat. No.: HY-15177

PF-04691502

11 Cited Publications

Customer Review

Based on 11 publication(s) in Google Scholar

PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with K_is of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.

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

Purity: 99.33%
CAS No.: 1013101-36-4
Formula: C₂₂H₂₇N₅O₄
Molecular Weight:425.48

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

PF-04691502 Chemical Structure

CAS No.: 1013101-36-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with K_is of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.

IC₅₀ & Target^[1]

PI3Kδ

1.6 nM (Ki)

PI3Kα

1.8 nM (Ki)

PI3Kγ

1.9 nM (Ki)

PI3Kβ

2.1 nM (Ki)

mTOR

16 nM (Ki)

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-20	IC₅₀	13 nM Compound: 1, PF-04691502	Inhibition of AKT phosphorylation at S473 in human BT20 cells after 1 hr by sandwich ELISA Inhibition of AKT phosphorylation at S473 in human BT20 cells after 1 hr by sandwich ELISA	10.1039/C0MD00072H
BT-20	IC₅₀	13 nM Compound: PF-04691502	Inhibition of AKT phosphorylation at Ser 473 in human BT20 cells Inhibition of AKT phosphorylation at Ser 473 in human BT20 cells	[PMID: 23506825]
NCI-H460	IC₅₀	0.2 μM Compound: 1; PF-04691502	Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay	[PMID: 29927604]
SK-OV-3	IC₅₀	0.29 μM Compound: PF-04691502	Antiproliferative activity against human SKOV3 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human SKOV3 cells after 3 days by CellTiter-Glo assay	[PMID: 25139570]
SK-OV-3	IC₅₀	7.4 nM Compound: 1, PF-04691502	Inhibition of AKT phosphorylation at S473 in human SKOV3 cells after 1 hr by sandwich ELISA Inhibition of AKT phosphorylation at S473 in human SKOV3 cells after 1 hr by sandwich ELISA	10.1039/C0MD00072H
U-87MG ATCC	IC₅₀	0.34 μM Compound: PF-04691502	Antiproliferative activity against human U87MG cells after 4 days by Celltiter-Glo luminescence cell viability assay Antiproliferative activity against human U87MG cells after 4 days by Celltiter-Glo luminescence cell viability assay	[PMID: 29305298]
U-87MG ATCC	IC₅₀	0.52 μM Compound: PF-04691502	Antiproliferative activity against human U87MG cells after 4 days by CellTiter-Glo assay Antiproliferative activity against human U87MG cells after 4 days by CellTiter-Glo assay	[PMID: 25139570]

In Vitro

PF-04691502 inhibits recombinant mouse PI3Kα in an ATP-competitive inhibitor. PF-04691502 potently inhibits AKT phosphorylation on S473 and T308 in all the 3 cancer cell lines with IC₅₀ values of 3.8 to 20 nM and 7.5 to 47 nM, respectively. Using a 96-well plate-based P-S6RP(S235/236) ELISA assay, PF-04691502 potently inhibits mTORC1 activity with an IC₅₀ of 32 nM. PF-04691502 inhibits cell proliferation of BT20, SKOV3, and U87MG with IC₅₀ values of 313, 188, and 179 nM, respectively. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF-04691502 reduces phosphorylation of AKT T308 and AKT S473 (IC₅₀ of 7.5-47 nM and 3.8-20 nM, respectively) and inhibits cell proliferation (IC₅₀ of 179-313 nM). PF-04691502 inhibits mTORC1 activity in cells as measured by PI3K-independent nutrient stimulated assay, with an IC₅₀ of 32 nM and inhibits the activation of PI3K and mTOR downstream effectors including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nude mice bearing U87MG tumors are administered orally once a day with PF-04691502 at 0.5, 1, 5, and 10 mg/kg (maximum tolerated dose, MTD). Treatment with 10 mg/kg results in a significant reduction of P-AKT(S473) levels at 1 hour postdosing, and persistent inhibition is observed for 8 hours. P-AKT(S473) recovers to above baseline 24 hours after 10 mg/kg treatment. For P-S6RP(S235/236), a similar inhibition time course is observed, but after 24 hours of treatment, P-S6RP levels remain lower than vehicle tumors. Modulation of the AKT downstream effector, P-PRAS40(T246), and mTOR downstream effector, P-4EBP1(T37/46), is observed. The PF-04691502-treated tumors are also evaluated by immunohistochemistry for levels of P-AKT(S473), total AKT, P-S6RP, and total S6RP. Phosphorylation of AKT and S6RP are significantly reduced at 4 hours after a single dose of PF-04691502 at 10 mg/kg. Dose-dependent tumor growth inhibition (TGI) is obtained in the U87MG xenograft model and approximately 73% TGI is observed at the MTD dose of 10 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1013101-36-4
Appearance Solid
Molecular Weight 425.48
Formula C₂₂H₂₇N₅O₄
Color Off-white to gray
SMILES

OCCO[C@@H]1CC[C@@H](N2C(N=C(N)N=C3C)=C3C=C(C4=CC=C(OC)N=C4)C2=O)CC1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (11)

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Journal Impact Factor

Cell Death Differ

Constitutive GLI1 expression in chondrosarcoma is regulated by major vault protein via mTOR/S6K1 signaling cascade. [Abstract]

2021 Jul;28(7):2221-2237. PMID: 33637972
Acta Pharm Sin B

Engineering prodrug nanomicelles as pyroptosis inducer for codelivery of PI3K/mTOR and CDK inhibitors to enhance antitumor immunity. [Abstract]

2022 Jul;12(7):3139-3155. PMID: 35865097
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Theranostics

Response to mTOR and PI3K inhibitors in enzalutamide-resistant luminal androgen receptor triple-negative breast cancer patient-derived xenografts. [Abstract]

2020 Jan 1;10(4):1531-1543. PMID: 32042320
Cell Death Dis

HGF/c-Met pathway facilitates the perineural invasion of pancreatic cancer by activating the mTOR/NGF axis. [Abstract]

2022 Apr 21;13(4):387. PMID: 35449152
J Med Chem

Revitalizing PI3K Inhibitors for PET/CT Imaging and Radionuclide Therapy of Multiple Cancers. [Abstract]

2026 Feb 12;69(3):3519-3536. PMID: 41593021
Cells

PF-04691502, a PI3K/mTOR Dual Inhibitor, Ameliorates AD-like Pathology in a Mouse Model of AD. [Abstract]

2025 Sep 21;14(18):1474. PMID: 41002439
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
bioRxiv

2023 Feb 8.
bioRxiv

2020 Jun.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (117.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3503 mL

11.7514 mL

23.5029 mL

5 mM

0.4701 mL

2.3503 mL

4.7006 mL

10 mM

0.2350 mL

1.1751 mL

2.3503 mL

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[1]

The biochemical protein kinase assays for class I PI3K and mTOR are assessed. The fluorescence polarization assay for ATP competitive inhibition is done as follows: mPI3Kα dilution solution (90 nM) is prepared in fresh assay buffer (50 mM Hepes pH 7.4, 150 mM NaCl, 5 mM DTT, 0.05% CHAPS) and kept on ice. The enzyme reaction contained 0.5 nM mouse PI3Kα (p110α/p85α complex purified from insect cells), 30 μM PIP2, PF-04691502 (0, 1, 4, and 8 nM), 5 mM MgCl₂, and 2-fold serial dilutions of ATP (0-800 μM). Final DMSO is 2.5%. The reaction is initiated by the addition of ATP and terminated after 30 minutes with 10 mM EDTA. In a detection plate, 15 uL of detector/probe mixture containing 480 nM GST-Grp1PH domain and 12 nM TAMRA tagged fluorescent PIP3 in assay buffer is mixed with 15 uL of kinase reaction mixture. The plate is shaken for 3 minutes, and incubated for 35 to 40 minutes before reading on an LJL Analyst HT^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

BT20, U87MG, and SKOV3 cells are plated at 3,000 cell/well in 96-well culture plates in growth medium with 10% FBS. Cells are incubated overnight and treated with DMSO (0.1% final) or serial diluted compound for 3 days. Resazurin is added to 0.1 mg/mL. Plates are incubated at 37°C in 5% CO₂ for 3 hours. Fluorescence signals are read as emission at 590 nm after excitation at 530 nm. IC₅₀ values are calculated by plotting fluorescence intensity to drug concentration in nonlinear curves. U87MG and SKOV3 cells are plated in 96-well plates overnight and caspase-3/caspase-7 activity is assessed with the Caspase-Glo 3/7 Assay Kit^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Female nu/nu mice (6-8 weeks old) are used. Tumor cells for implantation are harvested and resuspended in serum-free medium mixed with matrigel (1:1). SKOV3, U87MG, or NSCLC cells (2.5-4×10⁶) are implanted subcutaneously into the hind flank region. Treatment started when average tumor size is 100 to 200 mm³. PF-04691502 is formulated in 0.5% methylcellulose in water suspension and given orally once a day. Animal body weights and tumor volumes are measured every 2 to 3 days. Tumor volume is determined with Vernier calipers and calculated. Percentage of tumor growth inhibition (TGI) is calculated. Data are presented as mean±SE. Comparisons between treatment groups and vehicle group are done using 1-way ANOVA by Dunnett's tests. Student's t test is used to determine the P value for the comparison of 2 groups.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yuan J, et al. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol Cancer Ther. 2011 Nov;10(11):2189-99. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3503 mL	11.7514 mL	23.5029 mL	58.7572 mL
	5 mM	0.4701 mL	2.3503 mL	4.7006 mL	11.7514 mL
	10 mM	0.2350 mL	1.1751 mL	2.3503 mL	5.8757 mL
	15 mM	0.1567 mL	0.7834 mL	1.5669 mL	3.9171 mL
	20 mM	0.1175 mL	0.5876 mL	1.1751 mL	2.9379 mL
	25 mM	0.0940 mL	0.4701 mL	0.9401 mL	2.3503 mL
	30 mM	0.0783 mL	0.3917 mL	0.7834 mL	1.9586 mL
	40 mM	0.0588 mL	0.2938 mL	0.5876 mL	1.4689 mL
	50 mM	0.0470 mL	0.2350 mL	0.4701 mL	1.1751 mL
	60 mM	0.0392 mL	0.1959 mL	0.3917 mL	0.9793 mL
	80 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7345 mL
	100 mM	0.0235 mL	0.1175 mL	0.2350 mL	0.5876 mL

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PF-04691502

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

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Pain-Related Compound Library

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Highly Selective Inhibitors Library

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Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-04691502

All PI3K Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PF-04691502 Related Classifications

Cat. No.: HY-15177