CEP-33779

CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.

Product Specifications

CAS Number

[1257704-57-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

JAK

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CEP-33779.html

Purity

99.23

Solubility

DMSO : 8.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(C)=O

Molecular Formula

C24H26N6O2S

Molecular Weight

462.57

Precautions

H302, H315, H319, H335

References & Citations

[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.