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Lorlatinib

Chemical Structure : Lorlatinib

CAS No.: 1454846-35-5

Lorlatinib (PF-06463922;PF 06463922;PF06463922)

Catalog No.: PC-42919Not For Human Use, Lab Use Only.

A novel CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with IC50 of 0.07/0.025 nM respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A novel CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with IC50 of 0.07/0.025 nM respectively; also inhibits ALK L1196M (IC50=0.7 nM) and exhibits selectivity >100-fold for ROS1 over 204 kinases; inhibits crizotinib-resistant mutant ROS1G2032R and ROS1L2026M and orally available in vivo.

Lung Cancer

Phase 3 Clinical

Physicochemical Properties

M.Wt 406.413
Formula C21H19FN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 28 mg/mL

Chemical Name/SMILES

2H-4,8-Methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, 7-amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-, (10R)-

References

1. Zou HY, et al. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8.

2. Johnson TW, et al. J Med Chem. 2014 Jun 12;57(11):4720-44.

3. Infarinato NR, et al. Cancer Discov. 2016 Jan;6(1):96-107.

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