Home PI3K/Akt/mTOR PI3K inhibitor umbralisib (TGR-1202)

research use only

umbralisib (TGR-1202) PI3K inhibitor

Cat.No.S8194

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) PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 571.55

Jump to

Quality Control

Batch: Purity: 99.71%
99.71

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (174.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

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.

Chemical Information, Storage & Stability

Molecular Weight 571.55 Formula

C31H24F3N5O3

 Storage (From the date of receipt)
CAS No. 1532533-67-7 Download SDF Storage of Stock Solutions

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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
PI3Kδ
(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.
In vivo
The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-02-07)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03283137 ACTIVE_NOT_RECRUITING
CLL; B-cell Non Hodgkin Lymphoma
University of Chicago
 2018-01-23 PHASE1
NCT03269669 ACTIVE_NOT_RECRUITING
Grade 1 Follicular Lymphoma; Grade 2 Follicular Lymphoma; Grade 3a Follicular Lymphoma; Recurrent Follicular Lymphoma; Refractory Follicular Lymphoma
National Cancer Institute (NCI)
 2018-01-23 PHASE2
NCT05152459 WITHDRAWN
Recurrent Follicular Lymphoma; Refractory Follicular Lymphoma
City of Hope Medical Center
 2023-05-01 PHASE1; PHASE2
NCT03671590 TERMINATED
Non Hodgkin Lymphoma; Chronic Lymphocytic Leukemia
TG Therapeutics, Inc.
 2018-09-10 PHASE1
NCT03919175 TERMINATED
Lymphoma; Follicular Lymphoma; Follicular Lymphoma, Grade 1; Follicular Lymphoma Grade 2; Follicular Lymphoma Grade IIIa; Marginal Zone Lymphoma; Marginal Zone B Cell Lymphoma
Massachusetts General Hospital
 2019-09-01 PHASE2
NCT04635683 WITHDRAWN
Recurrent B-Cell Non-Hodgkin Lymphoma; Recurrent Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue; Recurrent Follicular Lymphoma; Recurrent Grade 1 Follicular Lymphoma; Recurrent Grade 2 Follicular Lymphoma; Recurrent Grade 3a Follicular Lymphoma; Recurrent Lymphoplasmacytic Lymphoma; Recurrent Mantle Cell Lymphoma; Recurrent Marginal Zone Lymphoma; Recurrent Nodal Marginal Zone Lymphoma; Recurrent Splenic Marginal Zone Lymphoma; Recurrent Waldenstrom Macroglobulinemia; Refractory B-Cell Non-Hodgkin Lymphoma; Refractory Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue; Refractory Follicular Lymphoma; Refractory Grade 1 Follicular Lymphoma; Refractory Grade 2 Follicular Lymphoma; Refractory Grade 3a Follicular Lymphoma; Refractory Lymphoplasmacytic Lymphoma; Refractory Mantle Cell Lymphoma; Refractory Marginal Zone Lymphoma; Refractory Nodal Marginal Zone Lymphoma; Refractory Splenic Marginal Zone Lymphoma; Refractory Waldenstrom Macroglobulinemia
Yazeed Sawalha
 2022-09-30 PHASE1

Read more about Clinical Trials

Tech Support

Handling Instructions

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

If you have any other enquiries, please leave a message.

Signaling Pathway Map