产品名称

PF 06463922 - Lorlatinib

产品货号

Axon 2600 CAS [1454846-35-5] MF C21H19FN6O2MW 406.41 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor (mean Ki value of <0.07 nM for inhibition of recombinant human wild-type ALK) displaying superior potency against all known clinically acquired ALK mutations (all displaying sub-nanomolar Ki values), including the highly resistant G1202R mutant. PF 06463922 (Lorlatinib) is capable of blocking Crizotinib-resistant ROS1 mutations and treatment with PF 06463922 led to superior regression of EML4-ALK-driven brain metastases compared with other clinically available ALK inhibitors. KEYWORDS: PF 06463922 | supplier | ALK/ROS1 inhibitor | Lorlatinib | PF06463922 | CAS [1454846-35-5] | ALK | ROS | Inhibitor | RTK | receptor tyrosine kinase | c-ROS | G1202R | mutant | Crizotinib | EML4-ALK | oncogene | fusion protein | Anaplastic Lymphoma Kinase | insulin receptor

产品价格

现货询价，电话：010-67529703

产品规格

产品品牌

axonmedchem

产品概述

产品详情

PF 06463922 - Lorlatinib

Based on 223 reference(s) in Google Scholar 9 10 223

Axon 2600

CAS [1454846-35-5]

MF C21H19FN6O2
MW 406.41

Purity: 99%
Optical purity: Optically pure
Soluble in DMSO

PF 06463922

Description

Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor (mean Ki value of <0.07 nM for inhibition of recombinant human wild-type ALK) displaying superior potency against all known clinically acquired ALK mutations (all displaying sub-nanomolar Ki values), including the highly resistant G1202R mutant. PF 06463922 (Lorlatinib) is capable of blocking Crizotinib-resistant ROS1 mutations and treatment with PF 06463922 led to superior regression of EML4-ALK-driven brain metastases compared with other clinically available ALK inhibitors.

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

HY Zou 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 U S A. 2015 Mar 17;112(11):3493-8.

HY Zou et al. PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models. Cancer Cell. 2015 Jul 13;28(1):70-81.

Cell Signaling & Oncology ALK Oncogene Fusion Proteins TGF-β RTK class XIX; 2.7.10.1 ALK Pfizer Licensed Products ROS

Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor

Chemical name

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

Parent CAS No.

[1454846-35-5]

产品资料