PF-4989216

Catalog No.S7675 Batch:S767501

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Technical Data

Formula

C18H13FN6OS
Molecular Weight 380.4 CAS No. 1276553-09-3
Solubility (25°C)* In vitro DMSO 76 mg/mL (199.78 mM)
Ethanol 7 mg/mL (18.4 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
Suspended in 0.5% methylcellulose
1.0mg/ml Taking the 1 mL working solution as an example, take 1 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.
Targets
p110δ [1]
(Cell-free assay)		 p110α [1]
(Cell-free assay)		 p110γ [1]
(Cell-free assay)
1 nM 2 nM 65 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]

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    NCI-H69, NCI-H1048, NCI-H1436, NCI-H82, NCI-H254, NCI-H526, NCI-H1963, NCI-H146, NCI-H841, Lu99A, Lu134B, and Lu134A cells.

  • Concentrations

    ~10 μM

  • Incubation Time

    72 hours

  • Method

    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.
Animal Study:[1]
  • Animal Models

    SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors

  • Dosages

    350 mg/kg

  • Administration

    p.o.

Selleck's PF-4989216 has been cited by 1 publication

Overexpression of ATP-Binding Cassette Subfamily G Member 2 Confers Resistance to Phosphatidylinositol 3-Kinase Inhibitor PF-4989216 in Cancer Cells. [ Mol Pharm, 2017, 14(7):2368-2377] PubMed: 28597653

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.