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Lorlatinib (PF-06463922)

Cat. No. M3975
Lorlatinib (PF-06463922) Structure
Synonym:

PF-06463922

Size Price Availability Quantity
Free Sample (0.1-0.5 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 56  USD56 In stock
10mg USD 90  USD90 In stock
25mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

Lorlatinib (PF-06463922) is an oral active, selective, brain osmotic and ATP-competitive ROS1/ALK inhibitor. The Ki of Lorlatinib for ROS1, wild-type ALK and ALKL1196M were <0.025 nM, <0.07 nM and 0.7 nM, respectively. Lorlatinib has anticancer activity.

Chemical Information
Molecular Weight 406.41
Formula C21H19FN6O2
CAS Number 1454846-35-5
Solubility (25°C) DMSO 60 mg/mL (ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zou HY, et al. Proc Natl Acad Sci U S A. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.

[2] Johnson TW, et al. J Med Chem. 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.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Lorlatinib (PF-06463922), PF-06463922 supplier, ALK, inhibitors, activators


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