umbralisib (TGR-1202)

For research use only.

Catalog No.S8194 Synonyms: Rp-5264

2 publications

umbralisib (TGR-1202) Chemical Structure

CAS No. 1532533-67-7

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.

Selleck's umbralisib (TGR-1202) has been cited by 2 publications

Purity & Quality Control

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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

Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female Balb/c mice
  • Dosages: 12.5, 25, 50 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (174.96 mM)
Water Insoluble
Ethanol '7 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+H2O
For best results, use promptly after mixing.
3mg/mL

* 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.

Chemical Information

Molecular Weight 571.55
Formula

C31H24F3N5O3

CAS No. 1532533-67-7
Storage powder
in solvent
Synonyms Rp-5264
Smiles CC(C)OC1=C(C=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)C4=C(C(=O)C5=C(O4)C=CC(=C5)F)C6=CC(=CC=C6)F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03207256 Enrolling by invitation Drug: TGR-1202|Drug: TGR-1202 + Ublituximab Chronic Lymphocytic Leukemia|Non Hodgkin Lymphoma TG Therapeutics Inc. August 9 2017 Phase 2
NCT03178201 Terminated Drug: TGR-1202 Follicular Lymphoma Columbia University|TG Therapeutics Inc. August 20 2017 Phase 2
NCT02867618 Terminated Drug: Carfilzomib|Drug: TGR-1202 Hodgkin Disease|Lymphoma Non-hodgkin Columbia University October 16 2016 Phase 1|Phase 2
NCT02493530 Active not recruiting Drug: TGR-1202|Drug: ruxolitinib Myelofibrosis|Polycythemia Vera Vanderbilt-Ingram Cancer Center July 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID