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/ Crizotinib

克唑替尼 /Crizotinib {[allProObj[0].p_purity_real_show]}

货号：A106537 同义名： PF-02341066;PF 2341066

Crizotinib (PF-02341066) 是一种具有口服活性的 ATP 竞争性 ALK 和 c-Met 抑制剂，IC50 分别为 20 nM 和 8 nM。

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Crizotinib 化学结构 CAS号：877399-52-5
Crizotinib 化学结构
CAS号：877399-52-5
Crizotinib 3D分子结构
CAS号：877399-52-5
Crizotinib 化学结构 CAS号：877399-52-5
Crizotinib 3D分子结构 CAS号：877399-52-5
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Crizotinib 纯度/质量文件 产品仅供科研

货号：A106537 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 ALK ↓ 其他靶点 纯度
ASP3026 +

ALK, IC50: 3.5 nM

 		99%+
ALK-IN-1 ++++

ALK, IC50: 0.07 nM

 		98+%
Crizotinib ++++

ALK, IC50: 24 nM

ROS1, Ki: <0.025 nM

 		98%
Entrectinib ✔ 99%+
Brigatinib +++

ALK, IC50: 0.37 nM

ROS1, IC50: 1.9 nM

 		FLT3 98%
NVP-TAE 684 +

ALK, IC50: 3 nM

 		99%+
Alectinib ++

ALK, IC50: 1.9 nM

ALK (F1174L), IC50: 3.5 nM

 		98%
Ceritinib +++

ALK, IC50: 0.2 nM

 		Insulin Receptor,IGF-1R 98%
GSK1838705A +++

ALK, IC50: 0.5 nM

 		Insulin Receptor,IGF-1R 99%
AZD-3463 ++

ALK, Ki: 0.75 nM

 		IGF-1R 99%
Lorlatinib ++++

ALK (L1196M), Ki: 0.07 nM

ROS1, Ki: <0.07 nM

 		98%
Repotrectinib +

ALK(G1202R), IC50: 1.26 nM

ALK(L1196M), IC50: 1.01 nM

 		Src 99%
Belizatinib ++

ALK, IC50: 0.7 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Crizotinib 生物活性

靶点

  • ALK

    ALK, IC50:24 nM

    ROS1, Ki:<0.025 nM
描述 c-Met, the prototypic member of a subfamily of RTKs, and its ligand HGF, are implicated in the progression of several human cancers and are attractive therapeutic targets. Activation of c-Met results in the binding and phosphorylation of adaptor proteins, such as Gab1, Grb2, Shc and c-Cbl and subsequent activation of signal transducers such as PI3K, Akt, PLC-γ, STAT and ERK1/2. Crizotinib is a potent and selective inhibitor of c-Met with Ki value of 4nM (measured by c-Met kinase activity) and ALK with IC50 value of 24nM (based on cell study). Antitumor activity of Crizotinib may be mediated by both direct effects on tumor cell growth or survival, as well as antiangiogenic mechanisms. It inhibited growth and induced apoptosis of human GTL-16 gastric carcinoma with IC50s of 9.7nM and 8.4nM, respectively, blocked the cell migration and invasion induced by HGF in NCI-H441 lung carcinoma cells with IC50 of 11nM and 6.1nM, as well as inhibited MDCK cell scattering with IC50 of 16nM. Treatment with Crizotinib resulted in inhibition on serum-stimulated HMVEC branching tubulogenesis, as well as inhibition on HGF-stimulated c-Met phosphorylation, cell survival and Matrigel invasion with IC50 values of 11nM, 14nM and 35nM, respectively, in HUVEC cells. And this two mechanism of anti-tumor effect also acted in tumor models. Oral administration of Crizotinib at dose of 6.25mg/kg, 12.5mg/kg and 50mg/kg showed tumor growth inhibition on 30%, 60% and 100% in c-Met–dependent GTL-16 tumor xenograft model with dose-dependent decrease in c-Met phosphorylation. The effect of Crizotinib on signal transduction pathways can be observed in tumors in vivo, as levels of phosphorylated c-Met, Akt, Erk, PLCE1 and STAT5 decreased in athymic mice bearing established GTL-16 xenografts orally administrated with Crizotinib at dose of 25 or 50mg/kg for 11 days[1].
作用机制 Crizotinib preferentially binds to the ATP binding pocket of ALK in its inactive conformation.[1]

Crizotinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
3T3 Function Assay 1 h Inhibition of RON assessed as growth factor-induced autophosphorylation with IC50 of 0.08 μM 21812414
3T3-E Function Assay 1 h Inhibition of TIE2 assessed growth factor-induced autophosphorylation with IC50 of 0.448 μM 21812414
697 Growth Inhibition Assay IC50=9.24329 μM SANGER
A101D Growth Inhibition Assay IC50=49.9736 μM SANGER

Crizotinib 动物研究

Dose Nude Mice: 12.5 mg/kg - 50 mg/kg[4] (p.o.), 25 mg/kg - 200 mg/kg[5] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[5] Dogs[5]
Dose 50 mg/kg (p.o.)
5 mg/kg (i.v.) 		10 mg/kg (p.o.)
5 mg/kg (i.v.)
Administration p.o.
i.v. 		p.o.
i.v.
F 60 ± 19 (%) (p.o.) 52 ± 44 (%) (p.o.)
T1/2 6.6 ± 2.6 h (p.o.)
9.6 ± 1.0 h (i.v.) 		13 ± 2 h (p.o.)
17 ± 4 h (i.v.)
Tmax 5.3 ± 1.2 h (p.o.) 3 ± 3 h (p.o.)
CL 47 ± 6 ml/min/kg (i.v.) 9.0 ± 0.7 ml/min/kg (i.v.)
Cmax 780 ± 200 ng/ml (p.o.) 620 ± 510 ng/ml (p.o.)
AUC0→∞ 11,000 ± 300 ng·h/ml (p.o.)
1800 ± 200 ng·h/ml (i.v.) 		9700 ± 6800 ng·h/ml (p.o.)
5900 ± 300 ng·h/ml (i.v.)
Vss 24 ± 4 L/kg (i.v.) 13 ± 2 L/kg (i.v.)

Crizotinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02559778 Neuroblastoma Phase 2 Recruiting September 2026 -
NCT03737994 ALK Gene Rearrangement ... 展开 >> ALK Positive Non-Squamous Non-Small Cell Lung Carcinoma Stage IV Lung Cancer AJCC v8 Stage IVA Lung Cancer AJCC v8 Stage IVB Lung Cancer AJCC v8 收起 << Phase 2 Not yet recruiting December 13, 2025 -
NCT01871805 Non-Small Cell Lung Cancer Phase 1 Phase 2 Completed - -

Crizotinib 参考文献

[1]Zou HY, Li Q, 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):4408-17.

[2]Yamazaki S, Vicini P, et al. Pharmacokinetic/pharmacodynamic modeling of crizotinib for anaplastic lymphoma kinase inhibition and antitumor efficacy in human tumor xenograft mouse models. J Pharmacol Exp Ther. 2012;340(3):549-57

[3]Zhou WJ, Zhang X, et al. Crizotinib (PF-02341066) reverses multidrug resistance in cancer cells by inhibiting the function of P-glycoprotein. Br J Pharmacol. 2012;166(5):1669-83.

[4]Baschnagel AM, Galoforo S, et al. Crizotinib Fails to Enhance the Effect of Radiation in Head and Neck Squamous Cell Carcinoma Xenografts. Anticancer Res. 2015 Nov;35(11):5973-82.

[5]Crizotinib

Crizotinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.21mL

4.44mL

2.22mL

Crizotinib 技术信息

CAS号877399-52-5
分子式C21H22Cl2FN5O
分子量 450.34
别名 PF-02341066;PF 2341066;(R)-Crizotinib
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C
溶解度

DMSO: 18 mg/mL(39.97 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

5% DMSO+30% PEG 300+dd water 5 mg/mL

Tags: Crizotinib | PF-02341066;PF 2341066;(R)-Crizotinib | c-Met/HGFR | ALK | AmBeed-信号通路专用抑制剂 | Crizotinib 纯度/质量文件 | Crizotinib 亚型比较 | Crizotinib 生物活性 | Crizotinib 细胞研究 | Crizotinib 动物研究 | Crizotinib 临床数据 | Crizotinib 参考文献 | Crizotinib 实验方案 | Crizotinib 技术信息

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