Crizotinib

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H22Cl2FN5O
Molecular Weight	450.337
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C[C@@H](OC1=CC(=CN=C1N)C2=CN(N=C2)C3CCNCC3)C4=C(Cl)C=CC(F)=C4Cl

InChI

InChIKey=KTEIFNKAUNYNJU-GFCCVEGCSA-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

HIDE SMILES / InChI

Molecular Formula	C21H22Cl2FN5O
Molecular Weight	450.337
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm376058.htm?source=govdelivery&utm_medium=email&utm_source=govdeliveryhttps://www.ncbi.nlm.nih.gov/pubmed/24695225
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202570s006lbl.pdf; https://www.mskcc.org/cancer-care/clinical-trials/14-063

(S)-crizotinib was discovered as an attractive chemical entity for further pre-clinical evaluation, and small-molecule inhibitors of MTH1 as a promising novel class of anticancer agents.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
ALK tyrosine kinase receptor 25 Target ID: CHEMBL4247 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202570s006lbl.pdf	Inhibitor 8297	24.0 nM [IC50]
Hepatocyte growth factor receptor 54 Target ID: CHEMBL3717 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202570s006lbl.pdf	Inhibitor 8297	11.0 nM [IC50]
7,8-dihydro-8-oxoguanine triphosphatase 4 Target ID: P36639 Gene ID: 4521.0 Gene Symbol: NUDT1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/24695225	Inhibitor 8297	72.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Metastatic non-small cell lung cancer 13 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/202570s000lbl.pdf	Primary		Approved 8429	XALKORI Approved Use Indicated for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. Launch Date 2011
Cancer 592 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24695225	Primary		Basic research	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
475 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31778074	300 mg 2 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CRIZOTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
99.6 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24990113	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	CRIZOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
328 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	250 mg 2 times / day steady-state, oral dose: 250 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CRIZOTINIB unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
327 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	250 mg 2 times / day multiple, oral dose: 250 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CRIZOTINIB unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
87 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	CRIZOTINIB unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
3240 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31778074	300 mg 2 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CRIZOTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2321 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24990113	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	CRIZOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3054 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	250 mg 2 times / day steady-state, oral dose: 250 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	CRIZOTINIB unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3084 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	250 mg 2 times / day multiple, oral dose: 250 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CRIZOTINIB unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1817 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	CRIZOTINIB unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
29 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24990113	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:		CRIZOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
47.1 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:		CRIZOTINIB unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
9.3% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000PharmR.pdf			CRIZOTINIB plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
300 mg 2 times / day steady, oral Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31778074	unhealthy, 49 years n = 6 Health Status: unhealthy Age Group: 49 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/31778074	Disc. AE: Fatigue... AEs leading to discontinuation/dose reduction: Fatigue (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/31778074
250 mg 2 times / day steady, oral Recommended\|MTD Dose: 250 mg, 2 times / day Route: oral Route: steady Dose: 250 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf	unhealthy, 51 years (range: 21-79 years) n = 119 Health Status: unhealthy Condition: Adenocarcinoma \| Squamous Cell Carcinoma \|Non-small Cell Lung Cancer Age Group: 51 years (range: 21-79 years) Sex: M+F Population Size: 119 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf	Disc. AE: Autoimmune thyroiditis... AEs leading to discontinuation/dose reduction: Autoimmune thyroiditis (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf
250 mg 2 times / day steady, oral Recommended\|MTD Dose: 250 mg, 2 times / day Route: oral Route: steady Dose: 250 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf	unhealthy, 52 years (range: 29-82 years) n = 136 Health Status: unhealthy Condition: Adenocarcinoma \| Adenosquamous Carcinoma\|Non-small Cell Lung Cancer Age Group: 52 years (range: 29-82 years) Sex: M+F Population Size: 136 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf	Disc. AE: ALT increased, Pneumonitis... AEs leading to discontinuation/dose reduction: ALT increased (2.2%) Pneumonitis (1.5%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf

AEs

AE	Significance	Dose	Population
Fatigue	grade 3, 1 patient Disc. AE	300 mg 2 times / day steady, oral Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31778074	unhealthy, 49 years n = 6 Health Status: unhealthy Age Group: 49 years Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/31778074
Autoimmune thyroiditis	1 patient Disc. AE	250 mg 2 times / day steady, oral Recommended\|MTD Dose: 250 mg, 2 times / day Route: oral Route: steady Dose: 250 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf	unhealthy, 51 years (range: 21-79 years) n = 119 Health Status: unhealthy Condition: Adenocarcinoma \| Squamous Cell Carcinoma \|Non-small Cell Lung Cancer Age Group: 51 years (range: 21-79 years) Sex: M+F Population Size: 119 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf
Pneumonitis	1.5% Disc. AE	250 mg 2 times / day steady, oral Recommended\|MTD Dose: 250 mg, 2 times / day Route: oral Route: steady Dose: 250 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf	unhealthy, 52 years (range: 29-82 years) n = 136 Health Status: unhealthy Condition: Adenocarcinoma \| Adenosquamous Carcinoma\|Non-small Cell Lung Cancer Age Group: 52 years (range: 29-82 years) Sex: M+F Population Size: 136 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf
ALT increased	2.2% Disc. AE	250 mg 2 times / day steady, oral Recommended\|MTD Dose: 250 mg, 2 times / day Route: oral Route: steady Dose: 250 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf	unhealthy, 52 years (range: 29-82 years) n = 136 Health Status: unhealthy Condition: Adenocarcinoma \| Adenosquamous Carcinoma\|Non-small Cell Lung Cancer Age Group: 52 years (range: 29-82 years) Sex: M+F Population Size: 136 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000MedR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inducer 781	substrate 1037 inhibitor 1767	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A 214 P-gp 1461 CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 OATP1B1 788 OATP1B3 706 BCRP 699 Ca2+ channels 57 L-type Ca2+ channels 28 Nav1.5 97	CYP3A5 395 CYP2C19 991 CYP2C8 693 CYP1A2 1054 P-gp 1537	CYP3A 129 CYP1A2 701

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	no
CYP3A 298	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	weak [IC50 44 uM]
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	weak [IC50 48 uM]
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	weak [Inhibition 30 uM]
Ca2+ channels 60	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000PharmR.pdf	yes [IC50 0.83 uM]
L-type Ca2+ channels 30	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000PharmR.pdf	yes [IC50 14.6 uM]
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 22 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 23 uM]
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 5.79 uM]
CYP3A 298	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 7.3 uM]	yes (co-administration study) Comment: crizotinib increased AUC of midazolam by 3.7x Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 >30 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 >30 uM]
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 >30 uM]
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes [IC50 >30 uM]
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes	no (co-administration study) Comment: effect is masked by inhibition Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	major	yes (co-administration study) Comment: ketoconazole increased cmax of crizotinib by 44%, auc by 216% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf
CYP3A5 395	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	major	yes (co-administration study) Comment: ketoconazole increased cmax of crizotinib by 44%, auc by 216% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	minor
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	minor
CYP1A2 1054	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	no
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	no
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000ClinPharmR.pdf	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Nav1.5 100	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000PharmR.pdf
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202570Orig1s000PharmR.pdf

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:64310	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:64310
MolPort	MolPort-009-679-404	https://www.molport.com/shop/molecule-link/MolPort-009-679-404
Selleck Chemicals	PF-2341066	http://www.selleckchem.com/products/PF-2341066.html
ZINC	ZINC000035902489	http://zinc15.docking.org/substances/ZINC000035902489
eMolecules	31526065	https://www.emolecules.com/cgi-bin/more?vid=31526065

PubMed

Title	Date	PubMed
		252160340
Crizotinib, a small-molecule dual inhibitor of the c-Met and ALK receptor tyrosine kinases.	2010 Dec	21154129
Trial watch: success for crizotinib in ALK-driven cancer.	2010 Dec	21119722
ALK inhibition for non-small cell lung cancer: from discovery to therapy in record time.	2010 Dec 14	21156280
The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers.	2010 Dec 15	21030459
Deciding priorities in Pharma.	2010 Dec 20	21172084
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.	2010 Nov 24	21095574
Crizotinib--latest champion in the cancer wars?	2010 Oct 28	20979477
Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer.	2010 Oct 28	20979469
Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen.	2011 Dec	22034911
ALK mutations conferring differential resistance to structurally diverse ALK inhibitors.	2011 Dec 1	21948233
Activity of crizotinib (PF02341066), a dual mesenchymal-epithelial transition (MET) and anaplastic lymphoma kinase (ALK) inhibitor, in a non-small cell lung cancer patient with de novo MET amplification.	2011 May	21623265
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.	2011 Sep 22	21823617
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).	2011 Sep 22	21812414
Personalized therapy of lung cancer.	2012	22286583
Anaplastic Lymphoma Kinase (ALK) regulates initiation of transcription of MYCN in neuroblastoma cells.	2012 Dec 13	22286764
Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers.	2012 Feb 8	22277784
Paracrine receptor activation by microenvironment triggers bypass survival signals and ALK inhibitor resistance in EML4-ALK lung cancer cells.	2012 Jul 1	22553343
The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma.	2012 Jul 10	22789543
Remarkable tumor response to crizotinib in a 14-year-old girl with ALK-positive non-small-cell lung cancer.	2012 Jun 1	22508824
ROS1 rearrangements define a unique molecular class of lung cancers.	2012 Mar 10	22215748
ALK inhibitor crizotinib combined with intrathecal methotrexate treatment for non-small cell lung cancer with leptomeningeal carcinomatosis.	2012 May	22385925
Rapid-onset hypogonadism secondary to crizotinib use in men with metastatic nonsmall cell lung cancer.	2012 Nov 1	22488744
Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study.	2012 Oct	22954507
[Cavitating nodules in a 40-year-old non-smoking woman: a very particular tumour].	2012 Sep	22980554
Targeting ALK: a promising strategy for the treatment of non-small cell lung cancer, non-Hodgkin's lymphoma, and neuroblastoma.	2012 Sep	22968692
Enhancement of the antiproliferative activity of gemcitabine by modulation of c-Met pathway in pancreatic cancer.	2013	22973962
Elucidating mechanisms of toxicity using phenotypic data from primary human cell systems--a chemical biology approach for thrombosis-related side effects.	2015 Jan 5	25569083

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose and schedule for crizotinib is 250 mg orally, twice daily, with or without food.

Route of Administration: fVal

In Vitro Use Guide

PF-2341066 potently inhibited NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells (mean IC50 value of 24 nmol/L). In biochemical and cellular screens, PF-2341066 was shown to be selective for c-Met and ALK at pharmacologically relevant concentrations across a panel of >120 diverse kinases. PF-2341066 potently inhibited cell proliferation, which was associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells at IC50 values of approximately 30 nmol/L but not ALK-negative lymphoma cells.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 17:39:59 GMT 2023` Edited by `admin` on `Sat Dec 16 17:39:59 GMT 2023`
Record UNII	53AH36668S
Record Status	`Validated (UNII)`
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Name

Type

Language

Crizotinib

Official Name

English

CRIZOTINIB [USAN]

Common Name

English

CRIZOTINIB [JAN]

Common Name

English

CRIZOTINIB [ORANGE BOOK]

Common Name

English

CRIZOTINIB [MI]

Common Name

English

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

Systematic Name

English

PF-02341066

Code

English

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

Systematic Name

English

NSC-756645

Code

English

CRIZOTINIB [MART.]

Common Name

English

CRIZOTINIB [VANDF]

Common Name

English

1066

Code

English

PF-2341066

Common Name

English

Crizotinib [WHO-DD]

Common Name

English

XALKORI

Brand Name

English

crizotinib [INN]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QL01XE16