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Cerdulatinib (PRT062070) hydrochloride

Name: Cerdulatinib (PRT062070) hydrochloride
Brand: Selleck Chemicals
SKU: S7634
Rating: 5 (18 reviews)

Synonyms: PRT2070 hydrochloride

Catalog No.S7634 Purity:99.66%

Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

Cerdulatinib (PRT062070) hydrochloride Chemical Structure

CAS No. 1369761-01-2

Purity & Quality Control

Batch: Purity: 99.66%

99.66

Cerdulatinib (PRT062070) hydrochloride Related Products

Related Targets	JAK1 JAK2 JAK3 Tyk2	Click to Expand
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Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Tyrosine Kinase Inhibitor Library JAK/STAT compound library	Click to Expand

Signaling Pathway

JAK Signaling Pathway

Biological Activity

Description

Targets

TYK2 ^[1] (Cell-free assay)	MST1 ^[1] (Cell-free assay)	ARK5 ^[1] (Cell-free assay)	MLK1 ^[1] (Cell-free assay)	Fms ^[1] (Cell-free assay)	Click to View More Targets
0.5 nM	4 nM	4 nM	5 nM	5 nM	Click to View More Targets

In vitro
In vitro	In human whole blood from normal donors, Cerdulatinib affects BCR-mediated B-cell activation by dual inhibition of SYK and JAK. As a dual SYK/JAK inhibitor, Cerdulatinib significantly reduces cell viability in a subset of NHL cell lines, and induces apoptosis in BCR-signaling competent NHL cell lines. ^[1]
Kinase Assay	Purified Kinase Assays
Kinase Assay	Potency against purified SYK is determined by fluorescence resonance energy transfer. A broader panel of 270 purified kinases is surveyed in which PRT062070 is tested at a fixed concentration of 300 nM. [³³P]-labeled substrate is measured after incubation of purified kinase with peptide substrate and [³³P]ATP at the Km concentration for the kinase.
Cell Research	Cell lines	Ramos RA-1, Daudi, Toledo, SU-DHL4 and SU-DHL6 cells
	Concentrations	~15 μM
	Incubation Time	72 hours
	Method	Cell lines (Ramos RA-1, Daudi, Toledo, SU-DHL4 and SU-DHL6) are cultured in RPMI media supplemented with 10% fetal bovine serum. Cell viability assays are performed using CellTiter Glo in 384-well plates. Cells are seeded at a density of 5000 cells per well.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	Mcl-1 / PARP p-SYK / SYK / p-BTK / BTK p-JAK1 / JAK1 / p-JAK3 / JAK3 / p-STAT6 / STAT6 / p-JAK2 / JAK2 / p-STAT3		28088788
	Growth inhibition assay	Cell metabolic activity		26575169

In Vivo
In vivo	In a rat collagen-induced arthritis model, Cerdulatinib (5 mg/kg p.o.) significantly improves inflammatory infiltrate within the synovium and the integrity of the articular cartilage. In addition, Cerdulatinib also blocks BCR-induced B-cell activation and splenomegaly in mice. ^[1]
Animal Research	Animal Models	Rat collagen-induced arthritis model
	Dosages	~5 mg/kg twice daily
	Administration	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04103060	Completed	Vitiligo	Dermavant Sciences GmbH\|Dermavant Sciences Inc.	September 27 2019	Phase 2
NCT01994382	Completed	Follicular Lymphoma (FL/Indolent NHL)\|Aggressive NHL (a NHL)\|Chronic Lymphocytic Leukemia (CLL) / Small Lymphocytic Lymphoma (SLL)\|T-cell Lymphoma (PTCL and CTCL)\|B-cell Non Hodgkin Lymphoma (NHL)	Alexion Pharmaceuticals Inc.\|Portola Pharmaceuticals	August 30 2013	Phase 1\|Phase 2

References

[1] Coffey G, J Pharmacol Exp Ther. 2014, 351(3), 538-548.

Chemical Information & Solubility

Molecular Weight	482	Formula	C₂₀H₂₈ClN₇O₃S
CAS No.	1369761-01-2	SDF	Download Cerdulatinib (PRT062070) hydrochloride SDF
Smiles	CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 20 mg/mL ( (41.49 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
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.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (6.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.07mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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.

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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