PF 06463922

Discontinued Product

PF 06463922 (Cat. No. 5640) has been withdrawn from sale for commercial reasons.
Cat.No. 5640 - PF 06463922 | C21H19FN6O2 | CAS No. 1454846-35-5
Description: High affinity and selective ALK and ROS1 inhibitor
Alternative Names: Lorlatinib
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
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (2)

Biological Activity

High affinity and selective ALK and ROS1 inhibitor (Ki values are <0.02, <0.07 and 0.7 nM for ROS1, wild-type ALK and ALK-L1196M, respectively). Exhibits >100-fold selectivity for ROS1 over a panel of 204 other kinases. Inhibits proliferation of BaF3 cells containing crizotinib-resistant ROS1 mutation in vitro. Inhibits tumor growth in relevant mouse models. Orally available and brain penetrant.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 406.41
Formula C21H19FN6O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1454846-35-5
PubChem ID 71731823
InChI Key IIXWYSCJSQVBQM-LLVKDONJSA-N
Smiles C[C@@H](O3)C4=C(C=CC(F)=C4)C(N(C)CC1=NN(C)C(C#N)=C1C2=CC3=C(N)N=C2)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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Keywords: PF 06463922, PF 06463922 supplier, anaplastic, lymphoma, kinases, (ALK), inhibitors, inhibits, inhibition, ROS1, c-ros, oncogenes, cancer, PF06463922, Lorlatinib, ALK, 5640, Tocris Bioscience

1 Citation for PF 06463922

Citations are publications that use Tocris products. Selected citations for PF 06463922 include:

Fadeev et al (2018) ALKALs are in vivo ligands for ALK family receptor tyrosine kinases in the neural crest and derived cells. Proc Natl Acad Sci U S A 115 E630 PMID: 29317532


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