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PF 06463922
- Lorlatinib
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C21H19FN6O2
- MW: 406.41
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.
More Information
| Parent CAS No. | 1454846-35-5 |
|---|---|
| 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 |
| SMILES | C12O[C@H](C)C3C=C(F)C=CC=3C(N(C)CC3C(=C(C#N)N(C)N=3)C(=C1)C=NC=2N)=O |&1:2,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H19FN6O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12/h4-7,9,11H,10H2,1-3H3,(H2,24,25)/t11-/m1/s1 |
| InChiKey | IIXWYSCJSQVBQM-LLVKDONJSA-N |
| CID | 71731823 |
| Short Description | ALK/ROS1 inhibitor |
References
- 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.
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