2-Keto Crizotinib

Names

[ Name ]:
2-Keto Crizotinib

[Synonym ]:
4-(4-{6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-pyridinyl}-1H-pyrazol-1-yl)-2-piperidinone
4-(4-{6-Amino-5-[(1R)-1-(2,6-dichlor-3-fluorphenyl)ethoxy]-3-pyridinyl}-1H-pyrazol-1-yl)-2-piperidinon
2-Piperidinone, 4-[4-[6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-pyridinyl]-1H-pyrazol-1-yl]-
4-(4-{6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophényl)éthoxy]-3-pyridinyl}-1H-pyrazol-1-yl)-2-pipéridinone

Biological Activity

[Description]:

2-Keto Crizotinib (PF-06260182) is an active lactam metabolite of crizotinib.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK

Research Areas >> Cancer

[In Vitro]

2-Keto Crizotinib (PF-06260182) is active and considerably less potent than crizotinib, and it is not thought to contribute significantly to the in vivo activity of crizotinib.

[References]

[1]. Balis FM, e al. First-dose and steady-state pharmacokinetics of orally administered crizotinib in children with solid tumors: a report on ADVL0912 from the Children's Oncology Group Phase 1/Pilot Consortium. Cancer Chemother Pharmacol. 2017 Jan;79(1):181-187.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
679.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₂₀Cl₂FN₅O₂

[ Molecular Weight ]:
464.320

[ Flash Point ]:
365.0±31.5 °C

[ Exact Mass ]:
463.097809

[ LogP ]:
3.09

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.688

Related Compounds

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