PF-06463922

Alternative_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
Description

PF-06463922 is a potent, selective, brain-penetrant, and high affinity ALK (Anaplastic lymphoma kinase) and ROS1 (c-Ros oncogene 1) inhibitor displaying >100-fold selectivity for ROS1 over panel of 204 other kinases. 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). It inhibits proliferation of BaF3 cells containing Crizotinib resistant ROS1 mutation in vitro.
CAS Number

1454846-35-5
Structure Available

Yes
Salt Form

No
Molecular Formula

C₂₁H₁₉FN₆O₂
Molecular Weight

406.41
Cell Permeable

Yes
Purity

≥98% by HPLC
Solubilities

DMSO (>35 mg/ml)
Handling

Protect from air and light
Tag Line

A potent, high affinity and selective ALK and ROS1 inhibitor
Storage Condition

-20°C
Shipping Condition

gel pack
Shelf Life

36 months
PubChem CID

71731823
PubChem CID Link
SMILES

CC1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C
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
Data Sheet Link
MSDS Available

Yes