GlpBio

(R)-Crizotinib3X 积分

目录号: GC14729纯度: >99.50%同义词: 克唑替尼; PF-02341066
A c-MET and ALK receptor tyrosine kinase inhibitor
(R)-Crizotinib
Cas No.: 877399-52-5
规格价格库存数量操作
10mg¥324.00现货
1
50mg¥630.00现货
1
100mg¥814.00现货
1
10mM (in 1mL DMSO)¥455.00现货
1
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文献被引

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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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产品描述 Description

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].

References:
[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.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

LLC SP and MP cell lines

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.

Reaction Conditions

12 h; IC50=21.3 nM (MP cells); cell survival rate of 50.0±0.6%=22.4 nM (SP cells)

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]:

Animal models

NU/NU nude mice

Dosage form

intratumoral injection

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.

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.

References:

[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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
877399-52-5
同义词
克唑替尼; PF-02341066
化学名
3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
SMILES
CC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N
分子式
C21H22Cl2FN5O
分子量
450.34 g/mol
溶解性
≥ 7.5mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol