PF 06463922

Pricing Availability Delivery Time Qty
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
Literature

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.

Compound Libraries

PF 06463922 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.64 100
ethanol 40.64 100

Preparing Stock Solutions

The following data is based on the product molecular weight 406.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.46 mL 12.3 mL 24.61 mL
5 mM 0.49 mL 2.46 mL 4.92 mL
10 mM 0.25 mL 1.23 mL 2.46 mL
50 mM 0.05 mL 0.25 mL 0.49 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Johnson et al (2014) 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), a macrocyclic inhibitor of anaplastic lympho J.Med.Chem. 57 4720 PMID: 24819116

Zou et al (2015) 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. 112 3493 PMID: 25733882


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Keywords: anaplastic lymphoma kinases (ALK) inhibitors inhibits inhibition ROS1 c-ros oncogenes cancer PF06463922 Lorlatinib ALK

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

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