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Datasheet of CEP33779

Description:
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with IC50 of 1.8 nM.
in vitro: CEP-33779 is a novel, orally active, selective JAK2 inhibitor, CEP-33779, induced regression of established colorectal
tumors, reduced angiogenesis, and reduced proliferation of tumor cells. CEP-33779, at nontoxic concentrations, significantly
sensitized ABCB1 overexpressing MDR cells to its anticancer substrates. CEP-33779 significantly increased intracellular
accumulation and decreased the efflux of doxorubicin by inhibiting the ABCB1 transport function. Furthermore, CEP-33779 did
not alter the expression of ABCB1 both at protein and mRNA levels but did stimulate the activity of ABCB1 ATPase.
in vivo: Treatment with CEP-33779 extended survival and reduced splenomegaly/lymphomegaly. Several serum cytokines were
significantly decreased upon treatment including IL-12, IL-17A, IFN-, IL-1, and TNF-. Anti-nuclear Abs and frequencies of
autoantigen-specific, Ab-secreting cells declined upon CEP-33779 treatment. Increased serum complement levels were
associated with reduced renal JAK2 activity, histopathology, and spleen CD138(+) plasma cells.
Animal research:
CEP-33779 was prepared in a manner analogous to the five-step method described elsewhere. Full biochemical and molecular
characterization of CEP-33779 is described elsewhere. CEP-33779 was provided orally in suspension form, dissolved in DMSO
(1% final concentration; Sigma, St. Louis, MO), and further reconstituted in polyethylene glycol (PEG) 400 (Emerald
BioSystems, Bainbridge Island, WA) to desired concentration for oral administration. Mice were orally treated with CEP-33779
in PEG 400 at 30 mg/kg, 55 mg/kg, or 100 mg/kg twice daily. Dexamethasone was provided as standard of care at 1.5 mg/kg, i.p.,
three times a week. Vehicle was provided orally, twice daily, as PEG 400 only. Mice were treated from 8 to 11 and 18 to 21 wk of
age with a dosing holiday for both CEP-33779 and dexamethasone from 11 to 18 wk of age (i.e., total of 7 wk without treatment).
Serum and urine were collected throughout the study.

Chemical Information
Catalog

DC7099

Purity of current batch:

>98%

Molecular Weight (MW)

462.57

Molecular Formula

C24H26N6O2S

CAS No.

1257704-57-6

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.