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PF-4989216

Name: PF-4989216
Brand: TargetMol
SKU: T6938
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T6938Cas No. 1276553-09-3

Alias PF 4989216

PF-4989216 is a potent and selective PI3K inhibitor with IC50 values of 2 nM (p110α), 142 nM (p110β), 65 nM (p110γ), 1 nM (p110δ), and 110 nM (VPS34).

PF-4989216

🥰Excellent

Purity: 99.85%

Catalog No. T6938Alias PF 4989216Cas No. 1276553-09-3

PF-4989216 is a potent and selective PI3K inhibitor with IC50 values of 2 nM (p110α), 142 nM (p110β), 65 nM (p110γ), 1 nM (p110δ), and 110 nM (VPS34).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$33	In Stock	In Stock
5 mg	$59	In Stock	In Stock
10 mg	$103	In Stock	In Stock
25 mg	$197	In Stock	In Stock
50 mg	$346	In Stock	In Stock
100 mg	$418	In Stock	In Stock
200 mg	$595	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$62	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.85%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	PF-4989216 is a potent and selective PI3K inhibitor with IC50 values of 2 nM (p110α), 142 nM (p110β), 65 nM (p110γ), 1 nM (p110δ), and 110 nM (VPS34).
Targets&IC50	p110α:2 nM, p110γ:65 nM, p110δ:1 nM, p110β:142 nM, VPS34:110 nM, mTOR:1440 nM (Ki), PI3Kα:0.6 nM (Ki)
In vitro	PF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis. [1]
In vivo	In SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity. [1]
Cell Research	SCLC cells are cultured (5,000 cells/well) in a 96-well microtiter plate at 37°C in 5% CO2 in supplier-recommended growth media and compounds are added to each well starting at 10 μM with a 3-fold serial dilution. At 72 hours after compound addition, CellTiter-Glo (CTG) Solution is added per the manufacturer's instructions. Luminescence is read on an Envision plate reader. All experiments are run in duplicate and have been repeated at least three times.(Only for Reference)
Synonyms	PF 4989216

Chemical Properties

Molecular Weight	380.4
Formula	C₁₈H₁₃FN₆OS
Cas No.	1276553-09-3
Smiles	Fc1cc(ccc1-c1c(sc(N2CCOCC2)c1C#N)-c1ncn[nH]1)C#N
Relative Density.	no data available

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 7 mg/mL (18.4 mM), Heating is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 71 mg/mL (186.65 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.26 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6288 mL	13.1441 mL	26.2881 mL	131.4406 mL
5 mM	0.5258 mL	2.6288 mL	5.2576 mL	26.2881 mL
10 mM	0.2629 mL	1.3144 mL	2.6288 mL	13.1441 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1314 mL	0.6572 mL	1.3144 mL	6.5720 mL
50 mM	0.0526 mL	0.2629 mL	0.5258 mL	2.6288 mL
100 mM	0.0263 mL	0.1314 mL	0.2629 mL	1.3144 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc