(E) -Belizatinib

(E) -Belizatinib ((E) -TSR-011) ) (compound 36), the (E) -isomer of Belizatinib (HY-17603), is a potent, selective and orally active anaplastic lymphoma kinase (ALK) Inhibitor with an enzymatic IC50 of 0.005 μM and a cellular IC50 of 0.048 μM. (E) -Belizatinib shows >61-fold selectivity over JAK2, SRC, and IGF1R. (E) -Belizatinib shows favorable potency and PK characteristics in rats and dogs. (E) -Belizatinib can be used for ALK-driven cancer research[1].

Product Specifications

CAS Number

[1388225-72-6]

Product Name Alternative

(E) -TSR-011

UNSPSC

12352005

Target

Anaplastic lymphoma kinase (ALK)

Related Pathways

Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

O=C(C1=CC=C(C=C1)F)NC(N([C@H]2CC[C@H](CC2)C(NC(C)C)=O)C3=C4)=NC3=CC=C4CN5CCC(CC5)C(C)(O)C

Molecular Formula

C33H44FN5O3

Molecular Weight

577.73

References & Citations

[1]Lewis RT, et al. The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer. J Med Chem. 2012 Jul 26;55 (14) :6523-40.