umbralisib (TGR-1202)

Catalog No.S8194 Synonyms: Rp-5264

For research use only.

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.

umbralisib (TGR-1202) Chemical Structure

CAS No. 1532533-67-7

Selleck's umbralisib (TGR-1202) has been cited by 3 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 (from reference)

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 571.55
Formula

C31H24F3N5O3

CAS No. 1532533-67-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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