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Cerdulatinib (PRT062070) hydrochloride

Name: Cerdulatinib (PRT062070) hydrochloride
Brand: Selleck Chemicals
SKU: S7634
Rating: 5 (13 reviews)

Catalog No.S7634 Synonyms: PRT2070 hydrochloride

For research use only.

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

Selleck's Cerdulatinib (PRT062070) hydrochloride has been cited by 13 publications

Purity & Quality Control

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JAK Signaling Pathway Map

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 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]

Assay

Methods	Test Index	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 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]

Protocol (from reference)

Kinase Assay:^[1]	Purified Kinase Assays: 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:^[1]	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. Cells are treated with the indicated concentrations of PRT062070, the SYK-selective inhibitor PRT060318, the pan-JAK inhibitor 1, a 1:1 combination of PRT060318 and JAK inhibitor 1, or vehicle control (0.5% dimethylsulfoxide) for 72 hours. Cell viability assays are performed using CellTiter Glo in 384-well plates. Cells are seeded at a density of 5000 cells per well.
Animal Research:^[1]	Animal Models: Rat collagen-induced arthritis model Dosages: ~5 mg/kg twice daily Administration: p.o.

References

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

Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 5% DMSO+corn oil For best results, use promptly after mixing. Click to purchase: Corn Oil	3mg/mL

Chemical Information

Molecular Weight	482
Formula	C₂₀H₂₈ClN₇O₃S
CAS No.	1369761-01-2
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl

Download Cerdulatinib (PRT062070) hydrochloride SDF

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04103060	Completed	Drug: Cerdulatinib 0.37% gel\|Drug: Vehicle gel	Vitiligo	Dermavant Sciences GmbH\|Dermavant Sciences Inc.	September 27 2019	Phase 2
NCT01994382	Completed	Drug: Cerdulatinib (PRT062070)	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)	Portola Pharmaceuticals\|Alexion Pharmaceuticals	August 31 2013	Phase 1\|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

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