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Crizotinib

Chemical Structure : Crizotinib

CAS No.: 877399-52-5

Crizotinib (PF-02341066;PF-2341066)

Catalog No.: PC-45885Not For Human Use, Lab Use Only.

Crizotinib (PF-02341066;PF-2341066) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of c-Met catalytic activity with Ki of 4 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Crizotinib (PF-02341066, PF-2341066) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of c-Met catalytic activity with Ki of 4 nM.
Crizotinib (PF-02341066) displays >1,000-fold selective for the VEGFR2 and PDGFRβ RTKs, >250-fold selective for IRK and Lck, and ∼40- to 60-fold selective for Tie2, TrkA, and TrkB.
Crizotinib (PF-02341066) also inhibits ALK (IC50=24 nM), potently inhibits c-Met phosphorylation and c-Met-dependent proliferation, migration, or invasion of human tumor cells in vitro (IC50=5-20 nM).
Crizotinib (PF-02341066) shows antitumor efficacy in tumor models at well-tolerated doses in vivo.

Physicochemical Properties

M.Wt 450.3367
Formula C21H22Cl2FN5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 55 mg/mL (Need ultrasonic)

Chemical Name/SMILES

2-Pyridinamine, 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-

References

1. Zou HY, et al. Cancer Res. 2007 May 1;67(9):4408-17.

2. Christensen JG, et al. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3314-22.

3. Knowles LM, et al. Clin Cancer Res. 2009 Jun 1;15(11):3740-50.

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