Loratinib (PF-06463922)
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MedKoo CAT#: 406533

CAS#: 1454846-35-5

Description: Loratinib, also known as PF-06463922, is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity. Upon administration, ALK/ROS1 inhibitor PF-06463922 binds to and inhibits both ALK and ROS1 kinases. The kinase inhibition leads to disruption of ALK- and ROS1-mediated signaling and eventually inhibits tumor cell growth in ALK- and ROS1-overexpressing tumor cells. In addition, PF-06463922 is able to cross the blood brain barrier.


Price and Availability

Size
Price

10mg
USD 90
100mg
USD 450
1g
USD 2850
Size
Price

25mg
USD 150
200mg
USD 750
2g
USD 4250
Size
Price

50mg
USD 250
500mg
USD 1650
5g
USD 6950

PF-06463922, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 1 g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406533
Name: Loratinib (PF-06463922)
CAS#: 1454846-35-5
Chemical Formula: C21H19FN6O2
Exact Mass: 406.15535
Molecular Weight: 406.41
Elemental Analysis: C, 62.06; H, 4.71; F, 4.67; N, 20.68; O, 7.87


Synonym: PF06463922; PF 06463922; PF-06463922; PF-6463922; PF6463922; PF 6463922; Loratinib.

IUPAC/Chemical Name: (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.

InChi Key: IIXWYSCJSQVBQM-LLVKDONJSA-N

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

SMILES Code: N#CC1=C(C(CN2C)=NN1C)C3=CN=C(N)C(O[C@H](C)C4=CC(F)=CC=C4C2=O)=C3


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP. 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) andc-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3. PubMed PMID: 24819116.