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Cerdulatinib hydrochloride

Catalog No. T6104 CAS 1369761-01-2

Synonyms: Cerdulatinib, PRT062070 hydrochloride, PRT2070, PRT062070, PRT2070 hydrochloride

Cerdulatinib (PRT-062070) 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.

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Cerdulatinib hydrochloride, CAS 1369761-01-2

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	Cerdulatinib (PRT-062070) 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	JAK3:8 nM, Syk:32 nM, JAK1:12 nM, Tyk2:0.5 nM, JAK2:6 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, PRT062070 hydrochloride, PRT2070, PRT062070, PRT2070 hydrochloride
Molecular Weight	482.0
Formula	C20H28ClN7O3S
CAS No.	1369761-01-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

Ethanol: <1 mg/mL

DMSO: 40 mg/mL (83 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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

Related Products

Related compounds with same targets

Linocinnamarin Damnacanthal Cevidoplenib dimesylate hydrochloride PRT-060318 Cerdulatinib hydrochloride GSK1904529A Fostamatinib Disodium SRX3207

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Keywords

Cerdulatinib hydrochloride 1369761-01-2 JAK/STAT信号通路 MAPK信号通路表观遗传蛋白酪氨酸激酶干细胞血管生成 Syk Tyrosine Kinases MLK JAK Hippo pathway c-Fms PRT062070 hydrochloride PRT 062070 PRT 2070 Inhibitor Cerdulatinib PRT2070 malignancies Tyk2 PRT-062070 PRT062070 Janus kinase PRT-2070 PRT2070 hydrochloride autoimmune dual B-cell Spleen tyrosine kinase inhibit inhibitor

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