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Cerdulatinib hydrochloride

Catalog No. T6104 CAS 1369761-01-2

Synonyms: PRT062070 hydrochloride, Cerdulatinib, 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.

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
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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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	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	PRT062070 hydrochloride, Cerdulatinib, PRT2070, 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 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 compound libraries

This product is contained In the following compound libraries：

Clinical Compound Library Angiogenesis related Compound Library Bioactive Compound Library Anti-Obesity Compound Library Preclinical Compound Library Drug Repurposing Compound Library Hematonosis Compound Library Anti-Cancer Compound Library Kinase Inhibitor Library Anti-Ovarian Cancer Compound Library

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Keywords

Cerdulatinib hydrochloride 1369761-01-2 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling MAPK Stem Cells Tyrosine Kinase/Adaptors Syk JAK MLK c-Fms Hippo pathway Tyrosine Kinases 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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