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Cerdulatinib

Catalog No. T2487   CAS 1198300-79-6
Synonyms: PRT2070, PRT062070

Cerdulatinib (PRT2070) is an novel oral dual Syk/JAK inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Cerdulatinib Chemical Structure
Cerdulatinib, CAS 1198300-79-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 50.00
5 mg In stock $ 72.00
10 mg In stock $ 108.00
25 mg In stock $ 195.00
50 mg In stock $ 318.00
100 mg In stock $ 547.00
200 mg In stock $ 703.00
500 mg In stock $ 1,080.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 99.64%
Purity: 98.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cerdulatinib (PRT2070) is an novel oral dual Syk/JAK inhibitor.
Targets&IC50 Tyk2:0.5 nM
In vitro Cerdulatinib exhibits an inhibitory effect on 60 CLL with IC50 ranging from 0.37 to 10.02 μM. Cerdulatinib induces apoptosis in CLL in association with MCL-1 down-regulation and PARP cleavage. Cerdulatinib (2 μM) is able to overcome the support of the microenvironment and induces cell death of CLL. Cerdulatinib (250-500 nM) blocks proliferation of ibrutinib-sensitive and ibrutinib-resistant primary CLL cells. Cerdulatinib also blocks proliferation of both ibrutinib-sensitive and ibrutinib-resistant primary CLL cells as well as BTKC481S-transfected cell lines, and blocks BCR and JAK-STAT signaling pathways. Furthermore, inhibition of SYK and JAK by cerdulatinib translates to downstream inhibition of AKT and ERK. Cerdulatinib inhibits the activity of NF-kB pathway[1]. PRT062070 reduces the ability of stimulated B cells to upregulate cell-surface expression of the early activation marker CD69 (IC50=0.11 μM). PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. PRT062070 (1 or 3 μM) induces apoptosis in BCR-signaling competent NHL cell lines[2]. Cerdulatinib demonstrates inhibitory activity against both ABC and GCB subtypes of DLBCL cells. Cerdulatinib also induces apoptosis in both GCB and ABC subtypes of DLBCL cell lines via caspase 3 and PARP cleavage. And cerdulatinib blocks cell cycle in both ABC and GCB subtypes of DLBCL via inhibition of RB phosphorylation and down-regulation of cyclin E. Cerdulatinib induces cell cycle arrest and apoptosis under the condition of BCR stimulation in all DLBCL cell lines. Besides, cerdulatinib blocks JAK/STAT and BCR signaling in both ABC and GCB DLBCL cell lines. Cerdulatinib induces cell death in primary human DLBCL samples[3]. Cerdulatinib inhibits BCR-induced signals in a dose-dependent manner and most strongly between 0.3 to 1 μM. and particularly in IGHV-unmutated samples with greater BCR signaling capacity and response to IL4, or samples expressing higher levels of sIgM, CD49d+, or ZAP70+. Cerdulatinib overcomes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing upregulation of MCL-1 and BCL-XL; however, BCL-2 expression is unaffected. Moreover, cerdulatinib synergizes with venetoclax in vitro to induce greater apoptosis than either drug alone in samples treated with IL4/CD40L[4].
In vivo PRT062070 (0.5 mg/kg) causes a nonstatistically significant trend toward reduced ankle inflammation, whereas significant reductions in inflammation are achieved with the 1.5, 3, and 5 mg/kg doses. Besides, PRT062070 also affects anticollagen antibody formation. PRT062070 (15 mg/kg) suppresses upregulation of splenic B-cell surface CD80/86 and CD69, and inhibits BCR signaling and activation in the spleen after oral dosing in mice[2].
Cell Research Cerdulatinib is dissolved in DMSO. TMD8 cells are transfected with constructs of WT BTK or BTKC481S mutants using kit V, Program U-13 on Amaxa Nucleofector. After transfection, the cells are co-cultured with NKTert cells in a 24-well plate for 24 hrs for recovery. Ibrutinib, cerdulatinib and vehicle (DMSO) are then added into the transfected TMD8 cells and cellular viability is determined with MuseTM Count & Viability kit using Muse Cell Analyzer. The cell survival is determined by flow cytometry using the Annexin V/7-AAD Apoptosis Detection Kit I on freshly isolated CLL cells.
Synonyms PRT2070, PRT062070
Molecular Weight 445.54
Formula C20H27N7O3S
CAS No. 1198300-79-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: ~20 mg/mL (44.9 mM)

TargetMolReferences and Literature

1. Guo A, et al. Dual SYK/JAK inhibition overcomes ibrutinib resistance in chronic lymphocytic leukemia: Cerdulatinib, but not ibrutinib, induces apoptosis of tumor cells protected by the microenvironment. Oncotarget. 2017 Feb 21;8(8):12953-12967. 2. Coffey G, et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48. 3. Ma J, et al. Cerdulatinib, a novel dual SYK/JAK kinase inhibitor, has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma. Oncotarget. 2015 Dec 22;6(41):43881-96. 4. Blunt MD, et al. The Dual Syk/JAK Inhibitor Cerdulatinib Antagonizes B-cell Receptor and Microenvironmental Signaling in Chronic Lymphocytic Leukemia. Clin Cancer Res. 2017 May 1;23(9):2313-2324.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Inhibitor Library Angiogenesis related Compound Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max Drug Repurposing Compound Library

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Keywords

Cerdulatinib 1198300-79-6 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Syk PRT2070 Spleen tyrosine kinase inhibit PRT 2070 PRT 062070 Inhibitor Janus kinase PRT062070 PRT-062070 PRT-2070 inhibitor

 

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