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Lorlatinib

Product ID L582694
Cas No. 1454846-35-5
Purity ≥98%
Product Unit SizeCostQuantityStock
5 mg $84.00 In stock
25 mg $340.00 In stock
100 mg $1,019.80 In stock
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  • Product Info
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  • Description
  • Product Info
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Description

Lorlatinib is a 3rd generation macrocyclic ALK inhibitor that shows significant improvement of inhibition against ROS1 kinase over 2nd generation inhibitors. Several cancers, when treated by ALK inhibitors, eventually develop point mutations, making the treatment ineffective. In a glioblastoma tumor model genetically engineered to reproduce ROS1 mutation, lorlatinib was yet able to demonstrate anticancer activity. Lorlatinib has also been shown to be effective as a single agent treatment on a mouse model of neuroblastoma. In addition, PET studies have found that lorlatinib successfully penetrates the blood-brain barrier resulting in high brain permeability of this inhibitor.

Product Info

Cas No.

1454846-35-5

Purity

≥98%

Formula

C21H19FN6O2

Formula Wt.

406.21

Chemical Name

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

IUPAC Name

(16R)-19-Amino-13-fluoro-4,8,16-trimethyl-9-oxo-17-oxa-4,5,8,20-tetraazatetracyclo[16.3.1.02,6.010,15]docosa-1(22),2,5,10,12,14,18,20-octaene-3-carbonitrile

Synonym

PF-6463922, PF-06463922

Shipping and Storage

Store Temp

Ambient

Ship Temp

Ambient

Downloads

MSDS

L582694 MSDS PDF

Info Sheet

L582694 Info Sheet PDF

References

Zou HY, Li Q, Engstrom LD, et al. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proc Natl Acad Sci USA. 2015 Mar 17;112(11):3493-3498. PMID: 25733882.

Basit S, Ashraf Z, Lee K, et al. First macrocyclic 3rd-generation ALK inhibitor for treatment of ALK/ROS1 cancer: clinical and designing strategy update of lorlatinib. Eur J Med Chem. 2017 Jul 7;134:348-356. PMID: 28431340.

Guan J, Tucker ER, Wan H, et al. The ALK inhibitor PF-06463922 is effective as a single agent in neuroblastoma driven by expression of ALK and MYCN. Dis Model Mech. 2016 Sep 1;9(9):941-952. PMID: 27483357.

Collier TL, Maresca KP, Normandin MD, et al. Brain penetration of the ROS1/ALK inhibitor lorlatinib confirmed by PET. Mol Imaging. 2017 Jan-Dec;16:1536012117736669. PMID: 29067878.

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