Home > Signaling Pathways>PI3K/Akt/mTOR>PI3K>Umbralisib (TGR1202; RP-5264)
Umbralisib (TGR1202; RP-5264)

This product is for research use only, not for human use. We do not sell to patients.

Umbralisib (TGR1202; RP-5264)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$1350Check With Us
500mg$2050Check With Us
1g$3075Check With Us

Cat #: V0556 CAS #: 1532533-67-7 Purity ≥ 98%

Description: Umbralisib (formerly TGR-1202; RP-5264; TGR1202; RP5264; Ukoniq) is a novel, highly specific, orally bioavailable and potent PI3Kδ inhibitor approved in 2021 by FDA to treat marginal zone lymphoma and follicular lymphoma.

References: Maharaj K, et al. The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells. Blood Adv. 2020 Jul 14;4(13):3072-3084.

Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products

Product Promise

Promise
Molecular Weight (MW)571.55
Molecular FormulaC31H24F3N5O3
CAS No.1532533-67-7
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 100 mg/mL (175 mM)r
Water:<1 mg/mL (slightly soluble or insoluble)r
Ethanol: 7 mg/mL (12.2 mM)
SMILES CodeO=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3C4=NC=NC(N)=C4C(C5=CC=C(C(F)=C5)OC(C)C)=N3)C)OC6=CC=C(F)C=C16
SynonymsRP 5264; RP-5264; TGR 1202; Umbralisib; TGR1202; TGR-1202; RP5264;
ProtocolIn VitroUmbralisib causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM.
In VivoUmbralisib (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25 in a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.7496 mL8.7481 mL17.4963 mL34.9926 mL
5mM0.3499 mL1.7496 mL3.4993 mL6.9985 mL
10mM0.1750 mL0.8748 mL1.7496 mL3.4993 mL
20mM0.0875 mL0.4374 mL0.8748 mL1.7496 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.