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Drug Details
01. General Information
Name Crizotinib
PubChem CID 11626560
Molecular Weight 450.3g/mol
Synonyms

Crizotinib, 877399-52-5, PF-02341066, (R)-crizotinib, PF-2341066, Xalkori, PF 2341066, (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine, Crizotinib (PF-02341066), 3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine, crizotinibum, Crizotinib (PF-2341066), UNII-53AH36668S, CHEBI:64310, PF2341066, 53AH36668S, NSC-756645, CHEMBL601719, 3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-[1-(4-PIPERIDINYL)-1H-PYRAZOL-4-YL]PYRIDIN-2-AMINE, DTXSID701009329, 877399-52-5 (free base), NSC 756645, 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]pyridin-2-amine, CRIZOTINIB (MART.), CRIZOTINIB [MART.], 2-Pyridinamine, 3-((1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(4-piperidinyl)-1H-pyrazol-4-yl)-, 3-[(1r)-1-(2,6-Dichloro-3-Fluorophenyl)ethoxy]-5-(1-Piperidin-4-Yl-1h-Pyrazol-4-Yl)pyridin-2-Amine, PF 02341066, 2-PYRIDINAMINE, 3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-[1-(4-PIPERIDINYL)-1H-PYRAZOL-4-YL]-, Xalkori (TN), Crizotinib [USAN], Crizotinib [USAN:INN], 3-((1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY)-5-(1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE, VGH, Crizotinib- Bio-X, CRIZOTINIB [MI], CRIZOTINIB [INN], CRIZOTINIB [JAN], CRIZOTINIB [VANDF], CRIZOTINIB [WHO-DD], SCHEMBL93829, PF-2341066,Crizotinib, Crizotinib (JAN/USAN/INN), GTPL4903, CRIZOTINIB [ORANGE BOOK], Crizotinib, >=98% (HPLC), EX-A096, L01XE16, KTEIFNKAUNYNJU-GFCCVEGCSA-N, BCPP000116, DTXCID601436157, GLXC-04599, AMY10313, PF 2341066;(R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, BDBM50306682, MFCD12407409, NSC749005, NSC749769, NSC800080, AKOS015901233, AKOS015995207, CCG-264803, DB08865, GS-6178, NSC-749005, NSC-749769, NSC-800080, NCGC00250400-01, NCGC00250400-02, NCGC00250400-09, NCGC00250400-12, BC164334, HY-50878, NS00072165, SW202555-3, MET Tyrosine Kinase Inhibitor PF-02341066, D09731, J-510370, Q5186964, BRD-K78431006-001-01-1, BRD-K78431006-001-03-7, 877399-52-5, 877399-53-6 (acetate), Z2065417924, 3-(2,6-dichloro-3-fluorobenzyloxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine, (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-am ine, (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine, 3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyra zol-4-yl]-2-pyridinamine, 3-[(R)-1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine

Drug Type Small molecule
Formula C₂₁H₂₂Cl₂FN₅O
SMILES CC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N
InChI 1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1
InChIKey KTEIFNKAUNYNJU-GFCCVEGCSA-N
CAS Number 877399-52-5
ChEMBL ID CHEMBL601719
ChEBI ID CHEBI:64310
TTD ID D03ZBT
Drug Bank ID DB08865
KEGG ID D09731
Toxicity Organism Test Type Route(Dose)
rat LD50 intraperitoneal(165 mg/kg)
mouse LD50 intraperitoneal(254 mg/kg)
rat LD50 oral(322 mg/kg)
Structure 2D-img
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2D MOL 3D MOL
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 32
Pair Name (S)-10-Hydroxycamptothecin, Crizotinib
Partner Name (S)-10-Hydroxycamptothecin
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Down-regulation Expression BCL-xL hsa598
Up-regulation Expression CYCS hsa54205
Down-regulation Phosphorylation EGFR hsa1956
Down-regulation Phosphorylation MAPK1 hsa5594
Up-regulation Phosphorylation MAPK14 hsa1432
Down-regulation Phosphorylation MAPK8 hsa5599
In Vitro Model NCI-H1975 Lung adenocarcinoma Homo sapiens (Human) CVCL_1511
HCC827 Lung adenocarcinoma Homo sapiens (Human) CVCL_2063
NCI-H460 Lung large cell carcinoma Homo sapiens (Human) CVCL_0459
Result Development of 10-Hydroxycamptothecin-crizotinib conjugate based on the synergistic effect on lung cancer cells
03. Reference
No. Title Href
1 Development of 10-Hydroxycamptothecin-crizotinib conjugate based on the synergistic effect on lung cancer cells. J Enzyme Inhib Med Chem. 2023 Dec;38(1):1-11. doi: 10.1080/14756366.2022.2132487. Click
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