PI-3065

Catalog No.S7623 Batch:S762301

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Technical Data

Formula

C27H31FN6OS
Molecular Weight 506.64 CAS No. 955977-50-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (197.37 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.)

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Biological Activity

Description PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
Targets
p110δ [1]
(Cell-free assay)		 p110β [1]
(Cell-free assay)
15 nM 1078 nM
In vitro PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ. [1]
In vivo In mouse model, PI-3065 (75 mg/kg, p.o.) also suppresses 4T1 tumor growth and metastasis via inactivation of p110δ. In the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma, PI-3065 prolongs survival and reduces the incidence of macroscopic metastases and other disease-associated pathologies. [1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    4T1 cells

  • Concentrations

    ~10 μM

  • Incubation Time

    48 hours

  • Method

    Proliferation of 4T1 cells is assayed following a 4-h treatment with the indicated p110δ inhibitors, then washing and MTS staining are carried out after 48 h culture.
Animal Study:

[1]
  • Animal Models

    Female WT BALB/c mice bearing 4T1 tumors

  • Dosages

    75 mg/kg, once daily

  • Administration

    p.o.

Selleck's PI-3065 has been cited by 2 publications

MDM2's Dual mRNA Binding Domains Co-Ordinate Its Oncogenic and Tumour Suppressor Activities [ Nucleic Acids Res, 2020, 26;gkaa431] PubMed: 32453417
PI3Kδ inhibition modulates regulatory and effector T-cell differentiation and function in chronic lymphocytic leukemia [ Leukemia, 2019, 33(6):1427-1438] PubMed: 30573773

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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.