Umbralisib HCl

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

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$1350	Check With Us
500mg	$2080	Check With Us
1g	$3120	Check With Us

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Cat #: V4754 CAS #: 1532533-78-0 Purity ≥ 98%

Description: Umbralisib HCl (also known as TGR-1202; RP5264; trade name Ukoniq), the hydrochloride salt of Umbralisib, is an orally bioavailable PI3Kδ inhibitor that has gained FDA approval in 2021for treating 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	608.01
Molecular Formula	C31H25ClF3N5O3
CAS No.	1532533-78-0
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
SMILES Code	O=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3N=C(C4=CC=C(OC(C)C)C(F)=C4)C5=C(N)N=CN=C53)C)OC6=C1C=C(F)C=C6.[H]Cl
Synonyms	TGR1202 hydrochloride; TGR-1202 HCl; TGR 1202 HCl; TGR1202 HCl; TGR-1202 hydrochloride; TGR 1202 hydrochloride;

Protocol	In Vitro	Umbralisib hydrochloride causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM.
Protocol	In Vivo	Umbralisib hydrochloride (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	1mg	5mg	10mg	20mg
1mM	1.6447 mL	8.2235 mL	16.4471 mL	32.8942 mL
5mM	0.3289 mL	1.6447 mL	3.2894 mL	6.5788 mL
10mM	0.1645 mL	0.8224 mL	1.6447 mL	3.2894 mL
20mM	0.0822 mL	0.4112 mL	0.8224 mL	1.6447 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

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)

Volume_(start)

Concentration_(final)

Volume_(final)

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.