(S)-Crizotinib

Name: (S)-Crizotinib
Brand: MedChemExpress
SKU: HY-100549
Rating: 4.5 (1 reviews)

Cat. No.: HY-100549 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

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(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC₅₀ of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models.

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

(S)-Crizotinib Chemical Structure

CAS No. : 1374356-45-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
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 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (S)-Crizotinib:

Crizotinib In-stock

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: 330 nM (MTH1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	3.8 μM Compound: 3	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 5 days by Hoechst 33342 dye based cell counting analysis Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 5 days by Hoechst 33342 dye based cell counting analysis	[PMID: 26878898]
IMR-32	IC₅₀	100 nM Compound: 87; (S)-GTx-186	Antiproliferative activity against human IMR32 cells by sulforhodamine B assay Antiproliferative activity against human IMR32 cells by sulforhodamine B assay	[PMID: 31077998]
MCF7	GI₅₀	4.4 μM Compound: 3	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 7 days by Hoechst 33342 dye based cell counting analysis Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 7 days by Hoechst 33342 dye based cell counting analysis	[PMID: 26878898]
NCI-H358	GI₅₀	4.9 μM Compound: 3	Antiproliferative activity against human NCI-H358 cells assessed as cell growth inhibition incubated for 5 days by Hoechst 33342 dye based cell counting analysis Antiproliferative activity against human NCI-H358 cells assessed as cell growth inhibition incubated for 5 days by Hoechst 33342 dye based cell counting analysis	[PMID: 26878898]
U2OS	GI₅₀	2.2 μM Compound: 3	Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 5 days by Hoechst 33342 dye based cell counting analysis Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 5 days by Hoechst 33342 dye based cell counting analysis	[PMID: 26878898]
U2OS	EC₅₀	6.8 μM Compound: (S)-Crizotinib	Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay	[PMID: 32184970]

In Vitro

(S)-crizotinib (0.625-80 μM; 24 hours) decreases the viability of NCI-H460, H1975 and A549 cells with IC₅₀ values of 14.29, 16.54 and 11.25 μM, respectively^[2].
(S)-crizotinib (10-30 μM; 24 hours) induces NCI-H460, H1975 and A549 cells apoptosis^[2].
(S)-crizotinib (10-30 μM; 24 hours) decreases Bcl-2: Bax ratio. (S)-crizotinib decreases B cell lymphoma 2 (Bcl-2), and Bcl-2 associated protein x (Bax) is either unaltered (H460 cells) or shows an increase (H1975 cells)^[2].
(S)-Crizotinib induces apoptosis in human non-small cell lung cancer (NSCLC) cells by activating ROS-dependent ER stress apoptotic pathway independent of mutT homologue (MTH1)^[2].

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

Cell Viability Assay^[2]

Cell Line:	NSCLC cells, NCI-H460, H1975 and A549 cells
Concentration:	0.625, 1.25, 2.5, 5, 10, 20, 40, 60, 80 μM
Incubation Time:	24 hours
Result:	Decreased the viability of NCI-H460, H1975 and A549 cells with IC₅₀ values of 14.29, 16.54 and 11.25 μM, respectively.

Apoptosis Analysis^[2]

Cell Line:	NSCLC cells, NCI-H460, H1975 and A549 cells
Concentration:	10, 20 or 30 μM
Incubation Time:	24 hours
Result:	Induced cells apoptosis.

Western Blot Analysis^[2]

Cell Line:	NSCLC cells, NCI-H460, H1975 and A549 cells
Concentration:	10, 20 or 30 μM
Incubation Time:	24 hours
Result:	Decreased Bcl-2: Bax ratio.

In Vivo

(S)-crizotinib (7.5 or 15 mg/kg; intraperitoneal injections; once daily for 10 days) results in significant reductions in both tumor volume and tumor weight^[2].

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

Animal Model:	Five-week-old, athymic BALB/c nu/nu female mice (17-19 g) with NCI-H460 cells^[2]
Dosage:	7.5 or 15 mg/kg
Administration:	Intraperitoneal injections; once daily for 10 days
Result:	Resulted in significant reductions in both tumor volume and tumor weight.

Molecular Weight

450.34

Formula

C₂₁H₂₂Cl₂FN₅O

CAS No.

1374356-45-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=NC=C(C2=CN(C3CCNCC3)N=C2)C=C1O[C@H](C4=C(Cl)C=CC(F)=C4Cl)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (27.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2205 mL	11.1027 mL	22.2054 mL
5 mM	0.4441 mL	2.2205 mL	4.4411 mL
10 mM	0.2221 mL	1.1103 mL	2.2205 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.78 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.78 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.78 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.81%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (247 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Huber KV, et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 2014 Apr 10;508(7495):222-7. [Content Brief]

[2]. Dai X, et al. (S)-crizotinib induces apoptosis in human non-small cell lung cancer cells by activating ROS independent of MTH1. J Exp Clin Cancer Res. 2017 Sep 7;36(1):120. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2205 mL	11.1027 mL	22.2054 mL	55.5136 mL
	5 mM	0.4441 mL	2.2205 mL	4.4411 mL	11.1027 mL
	10 mM	0.2221 mL	1.1103 mL	2.2205 mL	5.5514 mL
	15 mM	0.1480 mL	0.7402 mL	1.4804 mL	3.7009 mL
	20 mM	0.1110 mL	0.5551 mL	1.1103 mL	2.7757 mL
	25 mM	0.0888 mL	0.4441 mL	0.8882 mL	2.2205 mL

(S)-Crizotinib 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:

(S)-Crizotinib1374356-45-2DNA/RNA SynthesisApoptosismutThomologuenucleotidepoolanticanceractivityInhibitorinhibitorinhibit

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(S)-Crizotinib

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