Crizotinib hydrochloride (Synonyms: PF-02341066 hydrochloride)

Name: Crizotinib hydrochloride
Brand: MedChemExpress
SKU: HY-50878A
Rating: 5.0 (75 reviews)

Cat. No.: HY-50878A Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.

For research use only. We do not sell to patients.

Crizotinib hydrochloride Chemical Structure

CAS No. : 1415560-69-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 168	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
1 g		Get quote
5 g		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 75 publication(s) in Google Scholar

Other Forms of Crizotinib hydrochloride:

66 Publications Citing Use of MCE Crizotinib hydrochloride

: Crizotinib hydrochloride 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 hydrochloride purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109. [Abstract]; Resistant cells are treated with 200 nM Afatinib alone or in combination with 1 μM Crizotinib for 48 h.

: Crizotinib hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 20 nM (ALK), 8 nM (c-Met)^[3]

In Vitro

PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC₅₀ of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC₅₀ of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC₅₀ of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC₅₀ of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC₅₀ of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively^[1].
PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC₅₀ of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC₅₀ of 30 nM, but not ALK-negative lymphoma cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-2341066 reveals the ability to cause marked regression of large established tumors (> 600 mm³) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule in the GTL-16 model. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. A significant dose-dependent reduction of CD31-positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displays a significant dose-dependent reduction of human VEGFA and IL-8 plasma levels in both the GTL-16 and U87MG models. Marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels is observed in GTL-16 tumors following p.o. administration of PF-2341066^[1].
Treatment of c-MET-amplified GTL-16 xenografts with 50 mg/kg PF-2341066 elicits tumor regression that is associated with a slow reduction in 18F-FDG uptake and decreases expression of the glucose transporter 1, GLUT-1^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

486.80

Formula

C₂₁H₂₃Cl₃FN₅O

CAS No.

1415560-69-8

Appearance

Solid

Color

Yellow to brown

SMILES

ClC1=C(F)C=CC(Cl)=C1[C@H](OC2=CC(C3=CN(N=C3)C4CCNCC4)=CN=C2N)C.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (102.71 mM; Need ultrasonic)

DMSO : ≥ 4.9 mg/mL (10.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0542 mL	10.2712 mL	20.5423 mL
5 mM	0.4108 mL	2.0542 mL	4.1085 mL
10 mM	0.2054 mL	1.0271 mL	2.0542 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 55 mg/mL (112.98 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (248 KB) HNMR (201 KB) LCMS (452 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]

[4]. Cullinane C, et al. Differential (18)F-FDG and 3'-deoxy-3'-(18)F-fluorothymidine PET responses to pharmacologic inhibition of the c-MET receptor in preclinical tumor models. J Nucl Med. 2011 Aug;52(8):1261-7 [Content Brief]

Cell Assay ^[1]	Tumor cells are seeded in 96-well plates at low density in media supplemented with 10% FBS (growth media) and transferred to serum-free media (0% FBS and 0.04% BSA) after 24 h. Appropriate controls or designated concentrations of PF-2341066 are added to each well, and cells are incubated for 24 to 72 h. Human umbilical vascular endothelial cells (HUVEC) are seeded in 96-well plates in EGM2 media for 5 to 6 h at > 20,000 cells per well and transferred to serum-free media overnight. The following day, appropriate controls or designated concentrations of PF-2341066 are added to each well, and after 1 h incubation, HGF is added to designated wells at 100 ng/mL. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay is done to determine the relative tumor cell or HUVEC numbers. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Athymic mice bearing xenografts (300-800 mm³) are given PF-2341066 in water by oral gavage at designated dose levels. At designated times following PF-2341066 administration, mice are humanely euthanized, and tumors are resected. Tumors are snap frozen and pulverized using a liquid nitrogen-cooled cryomortar and pestle, protein lysates are generated, and protein concentrations are determined using a BSA assay. The level of total and phosphorylated protein is determined using a capture ELISA or immunoprecipitation-immunoblotting method. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] [4]. Cullinane C, et al. Differential (18)F-FDG and 3'-deoxy-3'-(18)F-fluorothymidine PET responses to pharmacologic inhibition of the c-MET receptor in preclinical tumor models. J Nucl Med. 2011 Aug;52(8):1261-7 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.0542 mL	10.2712 mL	20.5423 mL	51.3558 mL
	5 mM	0.4108 mL	2.0542 mL	4.1085 mL	10.2712 mL
	10 mM	0.2054 mL	1.0271 mL	2.0542 mL	5.1356 mL
H₂O	15 mM	0.1369 mL	0.6847 mL	1.3695 mL	3.4237 mL
	20 mM	0.1027 mL	0.5136 mL	1.0271 mL	2.5678 mL
	25 mM	0.0822 mL	0.4108 mL	0.8217 mL	2.0542 mL
	30 mM	0.0685 mL	0.3424 mL	0.6847 mL	1.7119 mL
	40 mM	0.0514 mL	0.2568 mL	0.5136 mL	1.2839 mL
	50 mM	0.0411 mL	0.2054 mL	0.4108 mL	1.0271 mL
	60 mM	0.0342 mL	0.1712 mL	0.3424 mL	0.8559 mL
	80 mM	0.0257 mL	0.1284 mL	0.2568 mL	0.6419 mL
	100 mM	0.0205 mL	0.1027 mL	0.2054 mL	0.5136 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Crizotinib hydrochloride Related Classifications

Help & FAQs

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:

Crizotinib1415560-69-8PF-02341066PF02341066PF 02341066Anaplastic lymphoma kinase (ALK)c-Met/HGFRROS KinaseAutophagyAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Crizotinib hydrochloride (Synonyms: PF-02341066 hydrochloride)

Customer Review

Other Forms of Crizotinib hydrochloride:

Crizotinib hydrochloride Related Antibodies

66 Publications Citing Use of MCE Crizotinib hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Crizotinib hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Crizotinib hydrochloride Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report