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- ALK (Anaplastic lymphoma kinase)
- (R)-Crizotinib
(R)-Crizotinib
A c-MET and ALK receptor tyrosine kinase inhibitor
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包装价格促销价数量
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10mg￥387.00310.00- +
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50mg￥762.00610.00- +
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100mg￥987.00790.00- +
- 货号: ajci13700
- CAS: 877399-52-5
- 别名: 克唑替尼; PF-02341066
- 分子式: C21H22Cl2FN5O
- 分子量: 450.34
- 纯度: ＞98%
- 溶解度: ≥ 7.5mg/mL in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
Crizotinib is a potent, ATP-competitive, small-molecule and orally available inhibitor of c-Met kinase with a Ki value?of 4 nmol/L[1].
Crizotinib has shown to inhibit?wild-type c-Met phosphorylation with a mean IC50 value of 11 nmol/L in multiple human endothelial and carcinoma cell lines. Crizotinib has been demonstrated to inhibit cell growth and induce apoptosis in?human GTL-16 gastric carcinoma cells. Additionally, crizotinib could inhibit cell migration and invasion induced by HGF in human NCI-H441 lung cancer cells. Moreover, crizotinib has revealed to block cell scattering of MDCK [1].
Crizotinib has been indicated to suppress tumor growth in GTL-16, NCI-H441 NSCLC, Caki-1 RCC, U87MG glioblastoma or PC-3 prostate tumor xenograft mice [1].
参考文献:
[1] Zou HY1,?Li Q,?Lee JH,?Arango ME,?McDonnell SR,?Yamazaki S,?Koudriakova TB,?Alton G,?Cui JJ,?Kung PP,?Nambu MD,?Los G,?Bender SL,Mroczkowski B,?Christensen JG. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res.?2007 May 1;67(9):4408-17.
Protocol
| Cell experiment [1]: | |
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Cell lines |
LLC SP and MP cell lines |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
12 h; IC50=21.3 nM (MP cells); cell survival rate of 50.0±0.6%=22.4 nM (SP cells) |
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Applications |
The inhibitory effects of crizotinib on MP cells and SP cells were determined by colony formation assay. The IC50 value of crizotinib for MP cells was 21.3 nM. Of note, the SP cells showed no significant changes after crizotinib treatment. However, the SP cells showed a cell survival rate of 50.0±0.6% following a combined treatment of crizotinib (22.4 nM) and verapamil (500 μM), compared with 105.3±0.4% survival of SP cells treated with crizotinib (22.4 nM) alone. The growth curves obtained demonstrate that crizotinib inhibited the growth of SP and MP cells, and this inhibition was dependent on both concentration and time. |
| Animal experiment [1]: | |
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Animal models |
NU/NU nude mice |
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Dosage form |
intratumoral injection |
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Applications |
Tumorigenicity was examined using immune-deficient mice, into which SP or MP cells of LLC were subcutaneously transplanted. Nonsorted LLC cells formed xenografts in mice at 1x105 cells. Tumor size was significantly decreased in the crizotinib-treated LLC groups (225±29 mm3) compared to the untreated group (PBS: 834±41 mm3) by 40 days after treatment. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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参考文献: [1] Xia P, Gou W F, Zhao S, et al. Crizotinib may be used in lewis lung carcinoma: A novel use for crizotinib[J]. Oncology reports, 2013, 30(1): 139-148. | |
