Crizotinib acetate (Synonyms: PF-02341066 acetate)

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Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition.

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Crizotinib acetate Chemical Structure

CAS No. : 877399-53-6

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Other In-stock Forms of Crizotinib acetate:

Crizotinib Crizotinib-d₅

Other Forms of Crizotinib acetate:

Crizotinib In-stock
Crizotinib-d₅ In-stock

60 Publications Citing Use of MCE Crizotinib acetate

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2019 Nov 7;2019:4253846. [Abstract]; Western blot analysis of cleaved caspase 3, Bax, and Bcl-2 expression after serum-free culture for 72 h with or without Crizotinib.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]; At 50mg/kg, Crizotinib inhibits MET phosphorylation and downstream signaling pathway activation.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 May 28;422:19-28. [Abstract]; CD74-ROS1 or CD74-ROS1 G2032R mutation cells are treated with Crizotinib for 24 h, the expression of ROS1 or p-ROS1 is determined by western blot.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006. [Abstract]; Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Dis Model Mech. 2016 Sep 1;9(9):941-52. [Abstract]; CLB-BAR, CLB-GE neuroblastoma cells are treated for 6 h with either Crizotinib or PF-04643922. Cells are harvested and pre-cleared cell lysates are analyzed on SDS PAGE followed by western blotting for ALK, phospho-ALK-Y1278, phospho-ERK5, pan-ERK5 phospho-ERK1/2 and pan-ERK. Actin is employed as a loading control. Protein band intensities are quantified by Image Studio Lite 3.1 and normalized to untreated samples.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 17;7(20):29011-22. [Abstract]; A, B. CLB-BAR (ALK-Δ4-11) and CLB-GE (ALK-F1174V), both ALK addicted cell lines, are treated with increasing doses of Brigatinib for 6 hours. Crizotinib (250 nM) is employed as a positive control. Cells lysates are resolved on SDS/PAGE followed by immunoblotting for pALK (Y1604) and additional downstream targets as indicated.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Sci Signal. 2014 Oct 28;7(349):ra102. [Abstract]; Activation of ERK5 in neuroblastoma cell lines expressing activated ALK. (A to C) Immunoblotting for the indicated proteins in neuroblastoma cells CLB-BAR (A), CLB-GE (B), and IMR32 (C) cultured on six-well plates in complete growth medium and treated with inhibitors as indicated for 6 hours alone (A and B) or before (C) stimulation with mAb46 for 30 min.

: Crizotinib acetate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 May 15;5(9):2688-702. [Abstract]; The Ret expression level is investigated by Western blot in MYCN/KI Alk^R1279Q and MYCN/KI Alk^F1178L treated tumors and controls using the anti-Ret antibody EPR2871. Actin is used as a standard for quantification.

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Description	Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition^[1]^[2]^[3].
Molecular Weight	510.39
Formula	C₂₃H₂₆Cl₂FN₅O₃
CAS No.	877399-53-6
SMILES	NC1=NC=C(C=C1O[C@H](C)C2=C(C=CC(F)=C2Cl)Cl)C3=CN(N=C3)C4CCNCC4.CC(O)=O
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (266 KB) Handling Instructions (2659 KB)
References	[1]. Zou HY, et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 2007, 67(9), 4408-4417. [Content Brief] [2]. Christensen JG, et al. Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol Cancer Ther. 2007, 6(12 Pt 1), 3314-3322. [Content Brief] [3]. Cui JJ, et al. Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63. [Content Brief]

Crizotinib acetate Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Crizotinib877399-53-6PF-02341066PF02341066PF 02341066c-Met/HGFRROS KinaseAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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Crizotinib acetate (Synonyms: PF-02341066 acetate)

Other Forms of Crizotinib acetate:

Crizotinib acetate Related Antibodies

60 Publications Citing Use of MCE Crizotinib acetate

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity

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Customer Review