CEP-33779

Alias: CEP-33779; CEP 33779; CEP33779
Cat No.:V0333 Purity: ≥98%
CEP33779 is a novel, potent,orally bioactive,highly selective inhibitor of JAK2 (Janus kinase) with potential antitumor and anti-inflammatoryactivity.
CEP-33779 Chemical Structure CAS No.: 1257704-57-6
Product category: JAK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

CEP33779 is a novel, potent, orally bioactive, highly selective inhibitor of JAK2 (Janus kinase) with potential antitumor and anti-inflammatory activity. It inhibits JAK2 with an IC50 of 1.8 nM, and exhibits >40- and >800-fold selectivity for JAK2 over JAK1 and TYK2. CEP33779 showed high activity in mice with collagen-induced arthritis (CIA) and collagen-antibody induced arthritis (CAIA). It induced regression of established colorectal tumors, reduced angiogenesis, and reduced proliferation of tumor cells. The ability of CEP-33779 to suppress growth of colorectal tumors by inhibiting the IL-6/JAK2/STAT3 signaling suggests a potential therapeutic utility of JAK2 inhibitors in multiple tumors types, particularly those with a strong inflammatory component.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
At non-toxic concentrations, P-glycoprotein-overexpressing multidrug-resistant cells' overexpression sensitivity to CEP-33779's anti-cancer substrates is markedly increased. Through inhibition of P-glycoprotein transport function overexpression, CEP-33779 drastically lowers doxorubicin efflux and increases intracellular accumulation [3].
ln Vivo
In nude mice, CEP-33779 showed a good PK profile with an intravenous half-life of one hour, a moderate distribution (Vd=2.6 L/kg), and a detectable oral exposure with an estimated 33% bioavailability. In the CWR22 xenograft model, it demonstrated antitumor efficacy; oral administration at 30 mg/kg bid for 14 days led to tumor stasis and partial regression in 5/10 animals [1]. Most animals that received CEP-33779 had almost total tumor shrinkage; the few tumor nodules that remained were tiny, poorly vascularized, and appeared necrotic. Tumor-associated NF-κB activation is inhibited by CEP-33779 [2].
Animal Protocol
Dissolved in DMSO; 55 mg/kg; Oral administration
Mice with collagen-induced arthritis (CIA) and collagen-antibody induced arthritis (CAIA)
References
[1]. Dugan BJ, et al. A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. J Med Chem. 2012 Jun 14;55(11):5243-54.
[2]. Seavey MM, et al. Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Mol Cancer Ther. 2012 Apr;11(4):984-93.
[3]. Tang SJ, et al. CEP-33779 antagonizes ATP-binding cassette subfamily B member 1 mediated multidrug resistance by inhibiting its transport function. Biochem Pharmacol. 2014 Sep 15;91(2):144-56
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H26N6O2S
Molecular Weight
462.57
CAS #
1257704-57-6
SMILES
O=S(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(C)=O
InChi Key
RFZKSQIFOZZIAQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H26N6O2S/c1-28-13-15-29(16-14-28)20-6-3-5-19(17-20)25-24-26-23-22(7-4-12-30(23)27-24)18-8-10-21(11-9-18)33(2,31)32/h3-12,17H,13-16H2,1-2H3,(H,25,27)
Chemical Name
N-(3-(4-methylpiperazin-1-yl)phenyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine
Synonyms
CEP-33779; CEP 33779; CEP33779
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 93 mg/mL (201.1 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80:30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1618 mL 10.8092 mL 21.6183 mL
5 mM 0.4324 mL 2.1618 mL 4.3237 mL
10 mM 0.2162 mL 1.0809 mL 2.1618 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • CEP-33779

    JAK2 blockade ameliorates collagen antibody-induced arthritis (CAIA) paw inflammation.Arthritis Res Ther.2011 Apr 21;13(2):R68.

  • CEP-33779


    CEP-33779

    JAK2 blockade reduces several disease correlates in a model of chronic degenerative arthritis.Arthritis Res Ther.2011 Apr 21;13(2):R68.

  • CEP-33779

    Suppression of carrageenan-induced inflammation by CEP-33779. Arthritis Res Ther. 2011; 13(2): R68.Arthritis Res Ther.2011 Apr 21;13(2):R68.

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