Cerdulatinib hydrochloride

SKU: orb1688997

Description

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an orally bioavailable, multi-targeted tyrosine kinase inhibitor with potent activity against JAK1, JAK2, JAK3, TYK2, and Syk, as well as 19 other kinases. It is utilized in preclinical research for investigating hematological malignancies and autoimmune disorders in both in vitro and in vivo models.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1369761-01-2
MW	482
Purity	99.85%
Formula	C₂₀H₂₈ClN₇O₃S
SMILES	Cl.CCS(=O)(=O)N1CCN(CC1)c1ccc(Nc2ncc(C(N)=O)c(NC3CC3)n2)cc1
Target	JAK,c-Fms,Hippo pathway,Tyrosine Kinases,MLK,Syk
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.07 mM);DMSO:4.82 mg/mL (10 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	JNK3:18 nM\|AMPK:6 nM\|RSK2:20 nM\|FMS:5 nM\|RET:105 nM\|MST1:4 nM\|Syk:32 nM\|ITK:194 nM\|MARK1:10 nM\|FLT4:51 nM\|MLK1:5 nM\|Flt3:90 nM\|PAR1B-a:13 nM\|JAK3:8 nM\|Rsk4:28 nM\|TYK2:0.5 nM\|MST2:15 nM\|Chk1:42 nM\|JAK1:12 nM\|TSSK:14 nM\|GCK:18 nM\|TBK1:10 nM\|ARK5:4 nM\|JAK2:6 nM Read more...
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. Read more...
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. Read more...
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) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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dual, autoimmune, ARK5, B-cell, cFms, c-Fms, MLK1, MST1, JAK, Hippo pathway, Hippopathway, Tyrosine Kinases, TyrosineKinases, Tyk2, Syk, PRT 062070, PRT 062070 Hydrochloride, PRT 2070, PRT 2070 Hydrochloride, PRT-062070, PRT062070 hydrochloride, PRT-062070 Hydrochloride, PRT-2070, PRT2070 hydrochloride, PRT-2070 Hydrochloride

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Compound Identifiers

PubChem CID

56960607 ↗

Key Properties

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No computed properties available.

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