TG100713

Catalog No.S2870 Batch:S287001

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Technical Data

Formula

C12H10N6
Molecular Weight 254.25 CAS No. 925705-73-3
Solubility (25°C)* In vitro DMSO 2 mg/mL (7.86 mM)
Water Insoluble
Ethanol Insoluble
* <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 TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
Targets
PI3Kδ [1] PI3Kγ [1] PI3Kα [1] PI3Kβ [1]
24 nM 50 nM 165 nM 215 nM
In vitro TG 100713 also strongly inhibits EC proliferation. [1]

Protocol (from reference)

Kinase Assay:[1]
  • Kinase Assays

    PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Protein kinase assays are performed by using commercial screening services.

Cell Assay:[1]
  • Cell lines

    HUVEC

  • Concentrations

    10 μM

  • Incubation Time

    24, 48, 72 h

  • Method

    Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of test compounds (10 μM), and cell numbers are quantified by XTT assay.

Customer Product Validation

, , Dr. Antonino Maria Spartà from University of Bolog

Selleck's TG100713 has been cited by 3 publications

A pyridinesulfonamide derivative FD268 suppresses cell proliferation and induces apoptosis via inhibiting PI3K pathway in acute myeloid leukemia [ PLoS One, 2022, 17(11):e0277893] PubMed: 36413544
STAT3 serine phosphorylation is required for TLR4 metabolic reprogramming and IL-1β expression [ Nat Commun, 2020, 11(1):3816] PubMed: 32732870
Design and synthesis of a novel series of N,4-diphenylpyrimidin-2-amine derivatives as potent and selective PI3Kγ inhibitors [Hua-Lin Yang MedChemComm, 2013, 10.1039/c3md00301a]

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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.