(S)-Crizotinib
Based on 3 publication(s) in Google Scholar
(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.
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- 純度: 99.81%
- CAS 番号: 1374356-45-2
- 分子式: C21H22Cl2FN5O
- 分子量:450.34
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 (S)-Crizotinib
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生物活性
製品説明
IC50 & Target
IC50: 330 nM (MTH1)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
3.8 μM
Compound: 3
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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
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[PMID: 26878898] |
| IMR-32 | IC50 |
100 nM
Compound: 87; (S)-GTx-186
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Antiproliferative activity against human IMR32 cells by sulforhodamine B assay
Antiproliferative activity against human IMR32 cells by sulforhodamine B assay
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[PMID: 31077998] |
| MCF7 | GI50 |
4.4 μM
Compound: 3
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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
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[PMID: 26878898] |
| NCI-H358 | GI50 |
4.9 μM
Compound: 3
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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
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[PMID: 26878898] |
| U2OS | EC50 |
6.8 μM
Compound: (S)-Crizotinib
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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
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[PMID: 32184970] |
| U2OS | GI50 |
2.2 μM
Compound: 3
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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
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[PMID: 26878898] |
体外実験
(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.
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Cell Line:NSCLC cells, NCI-H460, H1975 and A549 cells
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Concentration:0.625, 1.25, 2.5, 5, 10, 20, 40, 60, 80 μM
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Incubation Time:24 hours
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Result:Decreased the viability of NCI-H460, H1975 and A549 cells with IC50 values of 14.29, 16.54 and 11.25 μM, respectively.
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Cell Line:NSCLC cells, NCI-H460, H1975 and A549 cells
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Concentration:10, 20 or 30 μM
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Incubation Time:24 hours
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Result:Induced cells apoptosis.
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Cell Line:NSCLC cells, NCI-H460, H1975 and A549 cells
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Concentration:10, 20 or 30 μM
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Incubation Time:24 hours
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Result:Decreased Bcl-2: Bax ratio.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five-week-old, athymic BALB/c nu/nu female mice (17-19 g) with NCI-H460 cells[2]
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Dosage:7.5 or 15 mg/kg
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Administration:Intraperitoneal injections; once daily for 10 days
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Result:Resulted in significant reductions in both tumor volume and tumor weight.
化学情報
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CAS 番号 1374356-45-2
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性状 Solid
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分子量 450.34
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分子式 C21H22Cl2FN5O
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Color Light yellow to yellow
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SMILES
NC1=NC=C(C2=CN(C3CCNCC3)N=C2)C=C1O[C@H](C4=C(Cl)C=CC(F)=C4Cl)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Hazard Mater
Cadmium exposure is associated with impaired ovarian function: Potential role of cadmium-induced ferroptosis in granulosa cells. [Abstract]2026 Feb 1:503:141148. PMID: 41548307 -
Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (277 KB)
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取扱説明書 (2659 KB)
参考文献
[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
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.
| 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 関連分類
HY-100549 関連分類
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