Cat. No.: HY-13864

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PF-4989216

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PF-4989216 is a potent and selective PI3Kα inhibitor with a K_i of 0.6 nM.

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Pureté: 99.38%
CAS No.: 1276553-09-3
Formule: C₁₈H₁₃FN₆OS
Masse moléculaire:380.40

Stockage:

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

PF-4989216 Chemical Structure

CAS No.: 1276553-09-3

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

PF-4989216 is a potent and selective PI3Kα inhibitor with a K_i of 0.6 nM.

IC₅₀ & Target^[1]

PI3Kα

0.6 nM (Ki)

mTOR

1440 nM (Ki)

Voir tous les produits spécifiques à Isoform PI3K :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.58 μM Compound: 3; PF-4989216	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay	[PMID: 32375077]
NCI-H1975	IC₅₀	0.94 μM Compound: 3; PF-4989216	Antiproliferative activity against human NCI-H1975 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay Antiproliferative activity against human NCI-H1975 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay	[PMID: 32375077]
NCI-H460	IC₅₀	0.12 μM Compound: 3; PF-4989216	Antiproliferative activity against human NCI-H460 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay Antiproliferative activity against human NCI-H460 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay	[PMID: 32375077]
T47D	IC₅₀	0.34 μM Compound: 3; PF-4989216	Antiproliferative activity against human T47D cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay	[PMID: 32375077]
U-87MG ATCC	IC₅₀	2.31 μM Compound: 3; PF-4989216	Antiproliferative activity against human U87MG cells harboring PTEN deletion assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells harboring PTEN deletion assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay	[PMID: 32375077]

In Vitro

PF-4989216 (Compound 10) has excellent PI3Kα K_i (0.6 nM), good cellular potency (S473 IC₅₀=79 nM), and good selectivity against mTOR (mTOR K_i=1440 nM). PF-4989216 has PI3Kα K_i less than 1 nM and mTOR K_i more than 1 μM. PF-4989216 also has excellent selectivity over 40 other kinases, and no major CYP inhibitions are observed. Less than 30% inhibition is observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM^[1]. The toxicity of PF-4989216 in several drug-sensitive and MDR cancer cell lines, including cells overexpressing ABCB1 or ABCG2, and in HEK293 cells transfected with human ABCB1 or ABCG2 is determined. PF-4989216 inhibits human colon carcinoma S1 cell line and ABCG2-overexpressing subline S1-M1-80 with IC₅₀s of 1.11±0.09 and 6.79±1.00 uM, respectively. PF-4989216 inhibits human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 IC₅₀s of 2.30±0.68, 23.26±2.94 and 62.57±5.46 uM, respectively. PF-4989216 inhibits pcDNA-HEK293, ABCB1-transected MDR19-HEK293, ABCG2-tranfected R482-HEK293 cells with IC₅₀s of 0.44±0.05, 0.38±0.06 and 5.05±0.89 uM, respectively^[2].

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

In Vivo

PF-4989216 (Compound 10) is dosed orally in our in vivo antitumor model, PI3K driven NCI-H1975 xenograft tumors. PF-4989216 demonstrates dose responsive tumor growth inhibitory activity from 25 to 200 mg/kg in QD oral dosing^[1].

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

Chemical Information

CAS No. 1276553-09-3
Appearance Solid
Masse moléculaire 380.40
Formule C₁₈H₁₃FN₆OS
Color White to off-white
SMILES

N#CC1=C(N2CCOCC2)SC(C3=NC=NN3)=C1C4=CC=C(C#N)C=C4F
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (1)

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Journal Impact Factor

Nat Commun

Intrinsic signaling pathways modulate targeted protein degradation. [Abstract]

2024 Jul 2;15(1):5379. PMID: 38956052

Solvant et solubilité

In Vitro:

DMSO : ≥ 29 mg/mL (76.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.6288 mL

13.1441 mL

26.2881 mL

5 mM

0.5258 mL

2.6288 mL

5.2576 mL

10 mM

0.2629 mL

1.3144 mL

2.6288 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (6.57 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.57 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

Protocole

Cell Assay^[2]

MTT and CCK-8 assays are performed to determine the general sensitivities of cells to the tested drugs. The human colon carcinoma S1 cell line and ABCG2-overexpressing subline S1-M1-80 are treated with PF-4989216 (0.1, 1 and 10 μM). The human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 are treated with PF-4989216 (0.1, 1, 10 and 100 μM).The parental HEK293 and ABCG2-tranfected R482-HEK293 cells are treated with PF-4989216 (0.01, 0.1, 1 and 10 μM). For the reversal of cytotoxicity assays, PF-4989216 or Ko143 or Lapatinib at a nontoxic concentration is added into the cytotoxicity assay, and the extent of reversal is then calculated^[2].

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

Animal Administration^[1]

Mice^[1]
For animal studies, 6-8 week old nu/nu athymic female mice are used. Tumors are established by injecting 2×10⁶ cells suspended 1:1 (v/v) with reconstituted basement membrane. For tumor growth inhibition studies, mice with established tumors of ~150 mm³ are randomized. PF-4989216 (Compound 10) is dosed orally (25, 50, 100 and 200 mg/kg) in a mouse PI3K driven NCI-H1975 xenograft tumor model. Tumor dimensions are measured with vernier calipers, and tumor volumes are calculated. Tumor growth inhibition percentage (TGI %) is calculated.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 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)
- Korean - KR (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)
Instruction de manipulation (2659 KB)

Références

[1]. Liu KK, et al. Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity. ACS Med Chem Lett. 2011 Sep 19;2(11):809-813. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6288 mL	13.1441 mL	26.2881 mL	65.7203 mL
	5 mM	0.5258 mL	2.6288 mL	5.2576 mL	13.1441 mL
	10 mM	0.2629 mL	1.3144 mL	2.6288 mL	6.5720 mL
	15 mM	0.1753 mL	0.8763 mL	1.7525 mL	4.3814 mL
	20 mM	0.1314 mL	0.6572 mL	1.3144 mL	3.2860 mL
	25 mM	0.1052 mL	0.5258 mL	1.0515 mL	2.6288 mL
	30 mM	0.0876 mL	0.4381 mL	0.8763 mL	2.1907 mL
	40 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6430 mL
	50 mM	0.0526 mL	0.2629 mL	0.5258 mL	1.3144 mL
	60 mM	0.0438 mL	0.2191 mL	0.4381 mL	1.0953 mL

Keywords

PF-4989216

1 Cited Publications

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PF-4989216

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Publications Citing Use of MedChemExpress (MCE) PF-4989216

Voir tous les produits spécifiques à Isoform PI3K

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PF-4989216 Related Classifications

HY-13864 Related Classifications