research use only

umbralisib (TGR-1202) PI3K inhibitor

Name: umbralisib (TGR-1202)
Brand: Selleck Chemicals
SKU: S8194
Availability: InStock
Rating: 5 (7 reviews)

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.

Chemical Structure

Molecular Weight: 571.55

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.71%

99.71

Related Targets	Akt mTOR AMPK GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK PI4K PIKfyve MELK
Related Products	LY294002 3-Methyladenine (3-MA) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin (SL-2052) Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615

Chemical Information, Storage & Stability

Molecular Weight	571.55	Formula	C₃₁H₂₄F₃N₅O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1532533-67-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

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
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (5.25mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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: μL

Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	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].
References	[1] http://www.tgtxinc.com/AACR2012Poster3741.pdf

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):