Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cerdulatinib (PRT2070) is an novel oral dual Syk/JAK inhibitor.
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 | $ 318.00 | |
100 mg | In stock | $ 547.00 | |
200 mg | In stock | $ 703.00 | |
500 mg | In stock | $ 1,080.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 78.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: ~20 mg/mL (44.9 mM)
You can also refer to dose conversion for different animals. More
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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