[CAS NO. 1454846-35-5] Lorlatinib (PF-6463922)

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Catalog:	SLK-S7536
Brand:	Selleck
CAS:	1454846-35-5

Overview

MDL	MFCD28144520
Molecular Weight	406.41
Molecular Formula	C21H19FN6O2
SMILES	C(#N)C1=C2C=3C=C(O[C@H](C)C=4C(C(=O)N(C)CC2=NN1C)=CC=C(F)C4)C(N)=NC3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Lorlatinib (PF-6463922) is a potent, dual inhibitor with of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces . Phase 1.

Targets

In vitro

PF-06463922 demonstrates significant cell activity against ALK and a large set of ALK clinical mutations with IC50 ranging from 0.2 nM-77 nM. PF-06463922 significantly inhibits cell proliferation and induces cell apoptosis in the HCC78 human NSCLC cells harboring SLC34A2-ROS1 fusions and the BaF3-CD74-ROS1 cells expressing human CD74-ROS1. PF-06463922 also shows potent growth inhibitory activity and induces apoptosis in the NSCLC cells harboring either non-mutant ALK or mutant ALK fusions.

In vivo

In rats, PF-06463922 displays low plasma clearance, a moderate volume of distribution, a reasonable half-life, low propensity for p-glycoprotein 1-mediated efflux and a bioavailability of 100%. In vivo, PF-06463922 shows cytoreductive antitumor efficacy in the NIH3T3 xenograft models expressing human CD74-ROS1 and Fig-ROS1 via inhibition in ROS1 phosphorylation and the downstream signaling molecules, as well as inhibition of the cell cycle protein Cyclin D1 in tumors. In vivo, PF-06463922 also demonstrates marked antitumor activity in mice bearing tumor xenografts expressing EML4-ALK, EML4-ALK-L1196M, EML4-ALK-G1269A, EML4-ALK-G1202R or NPM-ALK.

References

[1] Johnson TW, et al. J Med Chem. 2014, 57(11), 4720-4744.
[2] Zou HY, et al. Mol Cancer Ther. 2013, 12, A277.
[3] Zou HY, et al. Mol Cancer Ther. 2013, 12, C253.

Synonyms

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)-

(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

PF 06463922

Lorlatinib

Lorbrena

Lorviqua

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