Home JAK/STAT JAK inhibitor - Syk inhibitor Cerdulatinib (PRT062070) hydrochloride

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Cerdulatinib (PRT062070) hydrochloride JAK inhibitor

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.
Cerdulatinib (PRT062070) hydrochloride JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 482

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Chemical Information, Storage & Stability

Molecular Weight 482 Formula

C20H28ClN7O3S

 Storage (From the date of receipt)
CAS No. 1369761-01-2 Download SDF Storage of Stock Solutions

Synonyms PRT2070 hydrochloride Smiles CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl

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

In vivo
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Mechanism of Action

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

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 S7634-WB1 28088788
Growth inhibition assay Cell metabolic activity S7634-viability1 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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