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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).

Catalog No. T6938Cas No. 1276553-09-3

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Purity:99.53%

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COA HNMR LCMS

PF-4989216

Catalog No. T6938Cas 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).

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.

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

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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, p110δ:1 nM, p110γ:65 nM, VPS34:110 nM, p110β:142 nM
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)
Alias	PF 4989216

Chemical Properties

Molecular Weight	380.4
Formula	C₁₈H₁₃FN₆OS
Cas No.	1276553-09-3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

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

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

DMSO: 71 mg/mL (186.6 mM)

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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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