Home PI3K/Akt/mTOR PI3K inhibitor umbralisib (TGR-1202) For research use only.

umbralisib (TGR-1202)

Synonyms: Rp-5264

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

umbralisib (TGR-1202) Chemical Structure

CAS No. 1532533-67-7

Purity & Quality Control

umbralisib (TGR-1202) Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

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
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].
Cell Research 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.
In Vivo
In vivo The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile[1].
Animal Research Animal Models Female Balb/c mice
Dosages 12.5, 25, 50 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03207256 Terminated
Chronic Lymphocytic Leukemia|Non Hodgkin Lymphoma
TG Therapeutics Inc.
 August 9 2017 Phase 2
NCT03178201 Terminated
Follicular Lymphoma
Columbia University|TG Therapeutics Inc.
 August 20 2017 Phase 2
NCT02867618 Terminated
Hodgkin Disease|Lymphoma Non-hodgkin
Columbia University
 October 16 2016 Phase 1|Phase 2
NCT02493530 Active not recruiting
Myelofibrosis|Polycythemia Vera
Vanderbilt-Ingram Cancer Center
 July 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 571.55 Formula

C31H24F3N5O3
CAS No. 1532533-67-7 SDF Download umbralisib (TGR-1202) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (174.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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