PF-06463922 (CAS 1454846-35-5) | Cayman Chemical
We collect cookies for vital website function and to better serve our customers. By continuing to browse you agree to the storing of cookies on your device. See our privacy policy for details.

PF-06463922

Item № 18371
CAS № 1454846-35-5
Purity ≥98%
product image
                (CAS 1454846-35-5)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $29.00 0.00
     5 mg $73.00 0.00
     10 mg $131.00 0.00

Pricing updated 2019-01-16. Prices are subject to change without notice.

Description
Synonyms
  • Lorlatinib

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = < 0.07 nM) and c-Ros oncogene 1 (ROS1, Ki = 0.7 nM).1 It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM).1,2,3 PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK.1,4 It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.2

Recommended Products

Related Products
View Related Product Categories
Technical Information
Formal 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
CAS Number
1454846-35-5
Synonyms
  • Lorlatinib
Molecular Formula
C21H19FN6O2
Formula Weight
406.4
Purity
≥98%
Formulation
A crystalline solid
λmax
319 nm
SMILES
FC1=CC=C(C(N(C)CC2=NN(C)C(C#N)=C32)=O)C([C@@H](C)OC4=C(N)N=CC3=C4)=C1
InChI Code
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
InChI Key
IIXWYSCJSQVBQM-LLVKDONJSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
Product Downloads

Download Product Insert

Download Safety Data Sheet (SDS)

Download free InChI Key generation software

Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

Get Batch-Specific Data and Documents by Batch Number

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data pack, and GC-MS data.

References & Product Citations
Product Description References

1. Johnson, T.W., Richardson, P.F., Bailey, S., 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), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations Journal of Medicinal Chemistry 57(11), 4720-4744 (2014).

2. Awad, M.M., and Shaw, A.T. ALK inhibitors in non-small cell lung cancer: Crizotinib and beyond Clin. Adv. Hematol. Oncol. 12(7), 429-439 (2014).

3. Zou, H.Y., Li, Q., Engstrom, L.D., et al. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations Proceedings of the National Academy of Sciences of the United States of America 112(11), 3493-3498 (2015).

4. Yamazaki, S., Lam, J.L., Zou, H.Y., et al. Translational pharmacokinetic-pharmacodynamic modeling for an orally available novel inhibitor of anaplastic lymphoma kinase and c-Ros oncogene 1 Journal of Pharmacology and Experimental Therapeutics 351, 67-76 (2014).

Technical Support
Contact Us
  • Toll Free Phone (USA and Canada Only): (888) 526-5351
  • Direct Phone: (734) 975-3888
Cayman Contract Services

We work with scientists to accelerate their research, drug discovery, and drug development needs through our expertise in the following areas:

Cayman Chemical

1180 East Ellsworth Road

Ann Arbor, Michigan 48108 USA

Toll Free: (800) 364-9897

(USA and Canada Only)

Fax: (734) 971-3640