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Technical Data
| Formula | C24H26N6O2S |
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| Molecular Weight | 462.57 | CAS No. | 1257704-57-6 | |
| Solubility (25°C)* | In vitro | DMSO | 93 mg/mL (201.05 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2. | ||
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| In vitro | CEP33779(< 3 μM) inhibits phosphorylation of downstream target signal transducer and activator of transcription 5(pSTAT5) of JAK2 in a concentration dependent manner in HEL92 cells. [1] | ||
| In vivo | CEP33779 orally administrated with 55 mg/kg inhibits phosphorylation of STAT5 in HEL92 tumor extracts from HEL92 xenograft mice. CEP33779 orally administered twice daily at dose of 55 mg/kg reduces mean paw edema and clinical scores in mice with collagen-antibody induced arthritis (CAIA) or collagen-induced arthritis (CIA). CEP33779 orally administered twice daily at dose of 55 mg/kg totally inhibits paw phospho-STAT3 expression in CAIA or CIA mice, associated with decreased cytokines including IL-12, IFNγ, IL-2, IL-1β, TNFα and GM-CSF. CEP33779 results in reduced bone degradation, reduced tissue destruction, and reduced osteoarthritis in dose-dependent manner in CAIA or CIA mice. [1] CEP33779 orally administrated at 100 mg/kg extends survival and reduces splenomegaly/lymphomegaly in MRL/lpr systemic lupus erythematosus mice, thus protect mice from developing glomerulonephritis. CEP33779 orally administrated at 100 mg/kg decreases several SLE-associated proinflammatory cytokines and reduces levels of a bone resorption biomarker associated with increased osteoclast activity in MRL/lpr systemic lupus erythematosus mice. [2] CEP33779 orally administered twice daily at dose of 55 mg/kg induces regression of established colorectal tumors, reduces angiogenesis, and reduces proliferation of tumor cells in a mouse model of colitis-induced colorectal cancer. Tumor regression correlated with inhibition of STAT3 and NF-κB (RelA/p65) activation, and decreased the expression of proinflammatory, tumor-promoting cytokines interleukin (IL)-6 and IL-1β. [3] |
Protocol (from reference)
| Animal Study:[1] |
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References
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Customer Product Validation
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Data from [Data independently produced by Biochem Pharmacol, 2014, 91(2), 144-56]
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Data from [Data independently produced by , , Sci Rep, 2018, 8(1):15645]
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Data from [Data independently produced by , , Biosci Rep, 2017, 37(4)]
Selleck's CEP-33779 has been cited by 11 publications
| A panel of janus kinase inhibitors identified with anti-inflammatory effects protect mice from lethal influenza virus infection [ Antimicrob Agents Chemother, 2024, 68(4):e0135023.] | PubMed: 38470034 |
| Growth hormone reduces aneuploidy and improves oocytes quality by JAK2-MAPK3/1 pathway in aged mice [ J Transl Med, 2023, 21(1):426] | PubMed: 37386516 |
| JAK2 Inhibitor, Fedratinib, Inhibits P-gp Activity and Co-Treatment Induces Cytotoxicity in Antimitotic Drug-Treated P-gp Overexpressing Resistant KBV20C Cancer Cells [ Int J Mol Sci, 2022, 23(9)4597] | PubMed: 35562984 |
| Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
| A Single-Cell Landscape of High-Grade Serous Ovarian Cancer [ Nat Med, 2020, 10.1038/s41591-020-0926-0] | PubMed: 32572264 |
| A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] | PubMed: 31740922 |
| Inhibiting ex-vivo Th17 responses in Ankylosing Spondylitis by targeting Janus kinases [Hammitzsch A Sci Rep, 2018, 8(1):15645] | PubMed: 30353145 |
| Interferon Gamma Prevents Infectious Entry of Human Papillomavirus 16 via an L2-Dependent Mechanism [Day PM J Virol, 2017, 91(10)] | PubMed: 28250129 |
| JAK2 inhibitor CEP-33779 prevents mouse oocyte maturation in vitro. [Wu C, et al. Biosci Rep, 2017, 37(4)] | PubMed: 28615348 |
| P-gp Inhibition by XL019, a JAK2 Inhibitor, Increases Apoptosis of Vincristine-treated Resistant KBV20C Cells with Increased p21 and pH2AX Expression. [ Anticancer Res, 2017, 37(12):6761-6769] | PubMed: 29187454 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.