- CEP-33779
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- $38.00 / 1mg
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2024-11-19
- CAS:1257704-57-6
- Min. Order:
- Purity: ≥95%
- Supply Ability: 10g
- CEP 33779
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- $9.80 / 1.79999995231628KG
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2019-12-25
- CAS:1257704-57-6
- Min. Order: 1g
- Purity: ≥99%
- Supply Ability: 100kg
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| | CEP 33779 Basic information |
| Product Name: | CEP 33779 | | Synonyms: | [8-(4-Methylsulfonylphenyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl][3-(4-methylpiperazin-1-yl)phenyl]amine;N-[3-(4-Methyl-1-piperazinyl)phenyl]-8-[4-(methylsulfonyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-amine;[1,2,4]Triazolo[1,5-a]pyridin-2-amine, N-[3-(4-methyl-1-piperazinyl)phenyl]-8-[4-(methylsulfonyl)phenyl]-;N-(3-(4-Methylpiperazin-1-yl)phenyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridi;N-[3-(4-methylpiperazin-1-yl)phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine;CEP 33779 USP/EP/BP;CS-1066;CEP33779; CEP-33779; CEP 33779. | | CAS: | 1257704-57-6 | | MF: | C24H26N6O2S | | MW: | 462.57 | | EINECS: | | | Product Categories: | Inhibitors;JAK;STAT;Inhibitor;JAK/STAT | | Mol File: | 1257704-57-6.mol |  |
| | CEP 33779 Chemical Properties |
| density | 1.35 | | storage temp. | Store at -20°C | | solubility | ≥23.15 mg/mL in DMSO with gentle warming; insoluble in EtOH | | form | solid | | pka | 7.78±0.42(Predicted) | | color | Light yellow to yellow |
| | CEP 33779 Usage And Synthesis |
| Description | Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription family. CEP-33779 is a potent, orally available inhibitor of JAK2 (IC50 = 1.3 nM). It shows 65-fold selectivity for JAK2 over JAK3. In mouse models of systemic lupus erythematosus, CEP-33779 reduces the production of inflammatory cytokines, decreases splenomegaly and lymphomegaly, and extends survival. It also diminishes inflammatory signaling and improves clinical scores in mice during collagen antibody-induced arthritis and collagen type II-induced arthritis. CEP-33779 induces regression of established colorectal tumors in mice, reducing angiogenesis and proliferation of tumor cells. | | Uses | CEP-33779 acts as an orally available inhibitor of JAK2 reducing the production of inflammatory cytokines and decreasing splenomegaly. Anti-arthritic agent. Anticancer agent. | | in vivo | CEP-33779 exhibits a favorable PK profile in nude mice, an iv half-life of 1 h, moderate distribution (Vd=2.6 L/kg), and measurable oral exposure with an estimated bioavailability of 33%. It demonstrates antitumor efficacy in the CWR22 xenograft model; oral dosing for 14 days at 30 mg/kg bid results in tumor stasis and partial regressions in 5/10 animals[1]. CEP-33779 administration results in an almost complete shrinkage of tumors in most animals; few remaining tumor nodules were small, poorly vascularized, and had a necrotic appearance. CEP-33779 suppressed activation of NF-κB in tumors[2]. | | target | JAK2 | | IC 50 | JAK2: 1.8 nM (IC50); JAK3: 150 nM (IC50) |
| | CEP 33779 Preparation Products And Raw materials |
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