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PF-4989216

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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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 SizePriceAvailabilityQuantity
2 mg$33In Stock
5 mg$59In Stock
10 mg$103In Stock
25 mg$197In Stock
50 mg$346In Stock
100 mg$418In Stock
200 mg$595In Stock
1 mL x 10 mM (in DMSO)$62In 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)
AliasPF 4989216
Chemical Properties
Molecular Weight380.4
FormulaC18H13FN6OS
Cas No.1276553-09-3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.6288 mL13.1441 mL26.2881 mL131.4406 mL
5 mM0.5258 mL2.6288 mL5.2576 mL26.2881 mL
10 mM0.2629 mL1.3144 mL2.6288 mL13.1441 mL
DMSO
1mg5mg10mg50mg
20 mM0.1314 mL0.6572 mL1.3144 mL6.5720 mL
50 mM0.0526 mL0.2629 mL0.5258 mL2.6288 mL
100 mM0.0263 mL0.1314 mL0.2629 mL1.3144 mL

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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:
TargetMol | Animal experimentsFor 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 DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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