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Item № 18371
CAS № 1454846-35-5
Purity ≥98%
product image
                (CAS 1454846-35-5)
     1 mg $29.00 0.00
     5 mg $73.00 0.00
     10 mg $131.00 0.00

Pricing updated 2019-04-25. Prices are subject to change without notice.

  • Lorlatinib

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = < 0.07 nM) and c-Ros oncogene 1 (ROS1, Ki = 0.7 nM).1 It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM).1,2,3 PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK.1,4 It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.2

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Technical Information
Formal Name
CAS Number
  • Lorlatinib
Molecular Formula
Formula Weight
A crystalline solid
319 nm
InChI Code
InChI Key

Warning - this product is not for human or veterinary use.

Shipping & Storage
Room temperature in continental US; may vary elsewhere
≥ 2 years
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References & Product Citations
Product Description References

1. Johnson, T.W., Richardson, P.F., Bailey, S., et al. Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations Journal of Medicinal Chemistry 57(11), 4720-4744 (2014).

2. Awad, M.M., and Shaw, A.T. ALK inhibitors in non-small cell lung cancer: Crizotinib and beyond Clin. Adv. Hematol. Oncol. 12(7), 429-439 (2014).

3. Zou, H.Y., Li, Q., Engstrom, L.D., et al. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations Proceedings of the National Academy of Sciences of the United States of America 112(11), 3493-3498 (2015).

4. Yamazaki, S., Lam, J.L., Zou, H.Y., et al. Translational pharmacokinetic-pharmacodynamic modeling for an orally available novel inhibitor of anaplastic lymphoma kinase and c-Ros oncogene 1 Journal of Pharmacology and Experimental Therapeutics 351, 67-76 (2014).

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