umbralisib (TGR-1202)

Catalog No.S8194 Batch:S819403

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Technical Data

Formula

C31H24F3N5O3
Molecular Weight 571.55 CAS No. 1532533-67-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (174.96 mM)
Ethanol 6 mg/mL (10.49 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2%DMSO 30%PEG300 2%Tween80 66%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. 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 Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.
Targets
PI3Kδ [1]
(Cell-free assay)
22.2 nM
In vitro The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells[1].
In vivo The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile[1].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells

  • Concentrations

    --

  • Incubation Time

    96 h

  • Method

    Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells are incubated with desired concentrations of RP5264. Growth is assessed after 96 h by a MTT assay.
Animal Study:[1]
  • Animal Models

    Female Balb/c mice

  • Dosages

    12.5, 25, 50 mg/kg

  • Administration

    oral administration

Selleck's umbralisib (TGR-1202) has been cited by 5 publications

Targeting IRAK4 with Emavusertib in Lymphoma Models with Secondary Resistance to PI3K and BTK Inhibitors [ J Clin Med, 2023, 12(2)399] PubMed: 36675328
Functional Testing to Characterize and Stratify PI3K Inhibitor Responses in Chronic Lymphocytic Leukemia [ Clin Cancer Res, 2022, 28-20:4444-4455] PubMed: 35998013
Resistance to PI3κδ inhibitors in marginal zone lymphoma can be reverted by targeting the IL-6/PDGFRA axis [ Haematologica, 2022, 10.3324/haematol.2021.279957] PubMed: 35484662
The delta isoform of PI3K predominates in chronic myelomonocytic leukemia and can be targeted effectively with umbralisib and ruxolitinib [ Exp Hematol, 2021, S0301-472X(21)00089-8] PubMed: 33617893
Ex vivo blockade of PI3K gamma or delta signaling enhances the antitumor potency of adoptively transferred CD8+ T cells. [ Eur J Immunol, 2020, 8] PubMed: 32383488

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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.