CEP-33779

Catalog No.S2806

CEP-33779 Chemical Structure

Molecular Weight(MW): 462.57

CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.

Size Price Stock Quantity  
In DMSO USD 500 In stock
USD 270 In stock
USD 370 In stock
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2 Customer Reviews

  • Potentiation of the antitumor effects of vincristine by CEP-33779 in a KBv200 cell xenograft model in nude mice. (A) The changes in tumor volume with time after tumor cell implantation. (B) The photograph of tumor size was taken on the 21st day after implantation. The various treatments were as follows: (a) Control (vehicle alone); (b) Vincristine (q2d x 6, ip, 0.2 mg/kg); (c) CEP-33779 (q2d x 6, p.o, 30 mg/kg) and (d) Vincristine (q2d x 6, ip, 0.2 mg/kg) plus CEP-33779 (q2d ?6, p.o, 30 mg/kg, given an hour before Vincristine administration).

    Biochem Pharmacol 2014 91(2), 144-56. CEP-33779 purchased from Selleck.

    CEP-33779 does not disorder microtubules reorganization in mouse oocytes. Metaphase I(M I) spindle morphology of mouse oocytes were observed during meiosis in control (n=77), DMSO (n=83), and CEP-33779 (n=72) groups. DNA (blue) and tubulin (green) were stained with DAPI and antitubulin antibody, respectively. The scale bar is 20 μm.

    Biosci Rep, 2017, 37(4). CEP-33779 purchased from Selleck.

Purity & Quality Control

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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.
Targets
JAK2 [1]
(Cell-free assay)
1.8 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TF-1 cells M4jlN2Z2dmO2aX;uJIF{e2G7 MWexJIg> M{DlUGlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBVTi1zIHPlcIx{KHW|aX7nJGdONUOVRjDwdoV1emWjdHXkJIZweiBzIHjyJJBzcW:{IITvJGdONUOVRjDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB3IHjyd{BjgSCIUlXUJIJie2WmIFflcoVDVEG8ZYKgZZN{[XluIFnDOVA:OC5yNkGg{txO MYWyNlU6PDZ7MB?=

... Click to View More Cell Line Experimental Data

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

Animal Research:[1]
+ Expand
  • Animal Models: Mice with collagen-induced arthritis (CIA) and collagen-antibody induced arthritis (CAIA)
  • Formulation: dimethyl sulfoxide (DMSO) (1% final concentration)
  • Dosages: 55 mg/kg
  • Administration: Orally administered twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL (77.82 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% PEG 300+1% Tween 80
30mg/mL

* 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.

Chemical Information

Molecular Weight 462.57
Formula

C24H26N6O2S

CAS No. 1257704-57-6
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    How to formulate the compound for in vivo use?

  • Answer:

    S2806 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension. It is fine for oral gavage, and can be further dilute with PBS. PEG 400 is ok.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID