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.
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.
Alternate Name/Synonyms: (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
Appearance: White Solid
Formulation: N/A
CAS Number: 1454846-35-5
Structure Available?: Yes
Peptide sequence: N/A
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
Country of Origin: USA
Tag Line: A potent, high affinity and selective ALK and ROS1 inhibitor
MDL Number: N/A
PubChem CID: 71731823
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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |
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