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Cerdulatinib hydrochloride

Catalog No. T6104   CAS 1369761-01-2
Synonyms: Cerdulatinib, PRT2070, PRT062070 hydrochloride, PRT062070, PRT2070 hydrochloride

Cerdulatinib hydrochloride (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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Cerdulatinib hydrochloride Chemical Structure
Cerdulatinib hydrochloride, CAS 1369761-01-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
5 mg In stock $ 87.00
10 mg In stock $ 117.00
25 mg In stock $ 223.00
50 mg In stock $ 393.00
100 mg In stock $ 585.00
500 mg In stock $ 1,270.00
1 mL * 10 mM (in DMSO) In stock $ 91.00
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Purity: 99.23%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cerdulatinib hydrochloride (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.
Targets&IC50 JAK2:6 nM, JAK1:12 nM, TYK2:0.5 nM, JAK3:8 nM, Syk:32 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]
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]
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.
Cell Research 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. (Only for Reference)
Synonyms Cerdulatinib, PRT2070, PRT062070 hydrochloride, PRT062070, PRT2070 hydrochloride
Molecular Weight 482
Formula C20H28ClN7O3S
CAS No. 1369761-01-2

Storage

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

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 40 mg/mL (83 mM)

TargetMolReferences and Literature

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

Related compound libraries

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

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IM-54 LY-364947 AZ7550 trimesylate salt (E/Z)-Necrosulfonamide Necrosulfonamide GW806742X MLKL-IN-2 PRT062607 hydrochloride

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Keywords

Cerdulatinib hydrochloride 1369761-01-2 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling MAPK Stem Cells Tyrosine Kinase/Adaptors MLK c-Fms Tyrosine Kinases Hippo pathway JAK Syk Inhibitor Cerdulatinib PRT2070 malignancies Tyk2 PRT-2070 PRT-062070 Hydrochloride PRT 062070 Hydrochloride PRT-2070 Hydrochloride PRT 2070 Hydrochloride PRT062070 Hydrochloride Janus kinase PRT2070 Hydrochloride Cerdulatinib Hydrochloride autoimmune dual PRT 062070 B-cell PRT-062070 Spleen tyrosine kinase PRT062070 hydrochloride PRT062070 PRT 2070 inhibit PRT2070 hydrochloride inhibitor

 

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