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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.

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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 $ 297.00
100 mg In stock $ 455.00
200 mg In stock $ 637.00
500 mg In stock $ 987.00
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 effectively inhibits 60 CLL cells with IC50 values ranging between 0.37 to 10.02 μM, induces apoptosis via MCL-1 down-regulation and PARP cleavage, and overcomes microenvironmental support to trigger CLL cell death at 2 μM. It inhibits both ibrutinib-sensitive and -resistant primary CLL cell proliferation at concentrations of 250-500 nM, targets BTKC481S-transfected cell lines, halts BCR and JAK-STAT signaling, and blocks SYK and JAK leading to the downstream inhibition of AKT, ERK, and the NF-kB pathway. PRT062070, with an IC50 of 0.11 μM, limits stimulated B cell activation marker CD69 expression, demonstrating varied effectiveness against JAK/STAT pathways and induces apoptosis in BCR-signaling competent NHL cell lines at 1 or 3 μM. Cerdulatinib shows inhibitory actions on both ABC and GCB DLBCL cell subtypes, induces caspase 3 and PARP cleavage-mediated apoptosis, inhibits cell cycle progression through RB phosphorylation reduction and cyclin E down-regulation, and blocks JAK/STAT and BCR signaling. It elicits cell death in DLBCL cells under BCR stimulation and in primary human DLBCL samples, disrupts BCR-induced signaling, especially potent from 0.3 to 1 μM in IGHV-unmutated, high BCR signaling, sIgM, CD49d+, or ZAP70+ expressing samples, and neutralizes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing MCL-1 and BCL-XL upregulation, without affecting BCL-2 expression. Cerdulatinib also synergizes with venetoclax to enhance apoptosis in IL4/CD40L treated samples.
In vivo PRT062070 administered at 0.5 mg/kg results in a minor, non-significant reduction in ankle inflammation, whereas dosages of 1.5, 3, and 5 mg/kg significantly decrease inflammation. Furthermore, PRT062070 impacts the formation of anticollagen antibodies. At a higher dosage of 15 mg/kg, PRT062070 notably suppresses the upregulation of CD80/86 and CD69 on the surface of splenic B-cells and inhibits BCR signaling and activation in the spleen following oral administration 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 Active Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Stem Cell Differentiation Compound Library Bioactive Compound Library Anti-Cancer Compound Library

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Keywords

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

 

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