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Cerdulatinib (PRT062070) hydrochloride JAK inhibitor

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

Cat.No.S7634

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.

Chemical Structure

Molecular Weight: 482

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Quality Control

Batch: Purity: 99.66%

99.66

Related Targets	EGFR STAT Pim
Other JAK Inhibitors	AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) TG101209 Pacritinib NVP-BSK805 2HCl WHI-P154

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (41.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : 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.
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.

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

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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	482	Formula	C₂₀H₂₈ClN₇O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1369761-01-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PRT2070 hydrochloride			Smiles	CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl

Mechanism of Action

Targets/IC₅₀/Ki	TYK2 (Cell-free assay) 0.5 nM MST1 (Cell-free assay) 4 nM ARK5 (Cell-free assay) 4 nM MLK1 (Cell-free assay) 5 nM Fms (Cell-free assay) 5 nM AMPK (Cell-free assay) 6 nM JAK2 (Cell-free assay) 6 nM JAK3 (Cell-free assay) 8 nM TBK1 (Cell-free assay) 10 nM MARK1 (Cell-free assay) 10 nM JAK1 (Cell-free assay) 12 nM PAR1B-a (Cell-free assay) 13 nM TSSK (Cell-free assay) 14 nM MST2 (Cell-free assay) 15 nM GCK (Cell-free assay) 18 nM JNK3 (Cell-free assay) 18 nM RSK2 (Cell-free assay) 20 nM RSK4 (Cell-free assay) 28 nM Syk (Cell-free assay) 32 nM Chk1 (Cell-free assay) 42 nM FLT4 (Cell-free assay) 51 nM
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.
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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25253883/

Applications

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

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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