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/ Crizotinib/克唑替尼

Crizotinib/克唑替尼 {[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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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Crizotinib/克唑替尼 化学结构 CAS号：877399-52-5
Crizotinib/克唑替尼 化学结构
CAS号：877399-52-5
Crizotinib/克唑替尼 3D分子结构
CAS号：877399-52-5
Crizotinib/克唑替尼 化学结构 CAS号：877399-52-5
Crizotinib/克唑替尼 3D分子结构 CAS号：877399-52-5
规格 价格 会员价 库存 数量
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Crizotinib/克唑替尼 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:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
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

 		99%
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 (F1174L), IC50: 3.5 nM

ALK, IC50: 1.9 nM

 		98%
Ceritinib +++

ALK, IC50: 0.2 nM

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

ALK, IC50: 0.5 nM

 		Insulin Receptor,IGF-1R 98%
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(L1196M), IC50: 1.01 nM

ALK(G1202R), IC50: 1.26 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/克唑替尼 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/克唑替尼 细胞实验

Cell Line
Concentration Treated Time Description References
H3122 cells 1 µM 6 months Generate crizotinib-resistant cell models EMBO Mol Med. 2019 Dec;11(12):e10581.
HT29 1 μM 24 h To evaluate the effect of Crizotinib on autophagy, results showed that Crizotinib significantly induced autophagy. Mol Cancer Ther. 2018 Oct;17(10):2112-2122.
HCT116 1 μM 24 h To evaluate the effect of Crizotinib on autophagy, results showed that Crizotinib significantly induced autophagy. Mol Cancer Ther. 2018 Oct;17(10):2112-2122.
BM cells 20 μg/ml 16 h To analyze the effect of Crizotinib on HGF-induced phosphorylation of S6 and ERK, results showed that Crizotinib could prevent HGF-induced phosphorylation. Nat Med. 2012 Jun;18(6):883-91.
SG16 cells 10 nM 72 h To evaluate the sensitivity of SG16 cells to Crizotinib, results showed that Crizotinib significantly impaired cell viability EMBO Mol Med. 2018 Sep;10(9):e8746.
GTL16 cells 10 nM 72 h To evaluate the sensitivity of GTL16 cells to Crizotinib, results showed that Crizotinib significantly impaired cell viability EMBO Mol Med. 2018 Sep;10(9):e8746.
EBC-1 cells 10 nM 72 h To evaluate the sensitivity of EBC-1 cells to Crizotinib, results showed that Crizotinib significantly impaired cell viability EMBO Mol Med. 2018 Sep;10(9):e8746.
MCMs (mouse cardiomyocytes) 0.3125, 0.625, 1.25, 2.5, 5.0 µM 72 h To evaluate the effect of Crizotinib on cell survival, results showed that Crizotinib significantly reduced the survival fraction of MCMs. Autophagy. 2024 Feb;20(2):416-436.
CCC-HEH-2 cells 0.3125, 0.625, 1.25, 2.5, 5.0 µM 72 h To evaluate the effect of Crizotinib on cell survival, results showed that Crizotinib significantly reduced the survival fraction of CCC-HEH-2 cells. Autophagy. 2024 Feb;20(2):416-436.
RH30 cells 0.01 to 5 μM 72 h To evaluate the effect of Crizotinib on cell proliferation and viability, results showed that Crizotinib significantly inhibited the growth and viability of RH4 and RH30 cells in a dose-dependent manner J Exp Clin Cancer Res. 2015 Oct 6;34:112.
RH4 cells 0.01 to 5 μM 72 h To evaluate the effect of Crizotinib on cell proliferation and viability, results showed that Crizotinib significantly inhibited the growth and viability of RH4 and RH30 cells in a dose-dependent manner J Exp Clin Cancer Res. 2015 Oct 6;34:112.
ADK-VR2 AG143 1.5 μM 72 h To evaluate the inhibitory effect of Crizotinib on ADK-VR2 AG143 cells, results showed that the clone had significantly lower sensitivity to Crizotinib. Transl Lung Cancer Res. 2022 Nov;11(11):2216-2229.
ADK-VR2 0.5 μM 72 h To evaluate the inhibitory effect of Crizotinib on ADK-VR2 cells, results showed that Crizotinib partially inhibited cell growth. Transl Lung Cancer Res. 2022 Nov;11(11):2216-2229.
RH30 cells 1.5 μM 72 h Inhibited cell proliferation and viability, induced apoptosis and autophagy J Exp Clin Cancer Res. 2015 Oct 6;34:112.
RH4 cells 1.5 μM 72 h Inhibited cell proliferation and viability, induced apoptosis and autophagy J Exp Clin Cancer Res. 2015 Oct 6;34:112.
SK-N-BE(2)C 300 nM 6 h To study the effect of ALK inhibition on RET mRNA levels, results showed decreased RET mRNA levels Oncogene. 2018 Mar;37(11):1417-1429.
CLB-MA 300 nM 6 h To study the effect of ALK inhibition on RET mRNA levels, results showed decreased RET mRNA levels Oncogene. 2018 Mar;37(11):1417-1429.
CLB-GA 300 nM 6 h To study the effect of ALK inhibition on RET mRNA levels, results showed decreased RET mRNA levels Oncogene. 2018 Mar;37(11):1417-1429.

Crizotinib/克唑替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Cynomolgus monkey Healthy cynomolgus monkey Intravenous injection 34.8 MBq/kg, 0.29 µg/kg Single injection, observed for 180 minutes To evaluate the distribution and elimination routes of [18F](R)-crizotinib in cynomolgus monkeys, showing low brain penetration (SUVmean = 0.1). Pharmaceuticals (Basel). 2022 Dec 15;15(12):1568
Nude mice Tumor xenograft model Oral 50 mg/kg Once daily, continuous treatment Evaluate the anti-tumor effect of crizotinib in tumor xenograft models EMBO Mol Med. 2019 Dec;11(12):e10581.
NOD/SCID mice Subcutaneous tumor model Oral 25 mg/kg Once daily for 18 days To evaluate the anti-tumor effect of Crizotinib on GTL16 R-CRIZ cells in a mouse model, results showed that Crizotinib significantly inhibited tumor growth EMBO Mol Med. 2018 Sep;10(9):e8746.
C57BL/6J mice Cardiac complications model Intragastric administration 100 mg/kg Once daily for 6 weeks To evaluate the effect of Crizotinib on cardiac function in mice, results showed that Crizotinib caused left ventricular dysfunction, myocardial injury, and pathological remodeling. Autophagy. 2024 Feb;20(2):416-436.
NSG mice Immunodeficient mice Oral 50 mg/kg Daily, continuous treatment To evaluate the inhibitory effect of Crizotinib on ADK-VR2 tumor growth, results showed that Crizotinib significantly reduced tumor growth but did not completely eradicate the tumor. Transl Lung Cancer Res. 2022 Nov;11(11):2216-2229.
Mice MYCN/AlkF1178L neuroblastoma model Oral 100 mg/kg Daily treatment To study the effect of combining Crizotinib and Vandetanib on tumor growth, results showed the combination was more effective than Crizotinib alone Oncogene. 2018 Mar;37(11):1417-1429.
Mice MYCN/AlkF1178L neuroblastoma model Oral 100 mg/kg Once daily Combination of crizotinib and vandetanib more effectively inhibited tumor growth than crizotinib alone Oncogene. 2018 Mar;37(11):1417-1429.

Crizotinib/克唑替尼 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/克唑替尼 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/克唑替尼 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/克唑替尼 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/克唑替尼 技术信息

CAS号877399-52-5
分子式C21H22Cl2FN5O
分子量 450.34
SMILES Code NC1=NC=C(C2=CN(C3CCNCC3)N=C2)C=C1O[C@@H](C4=C(Cl)C=CC(F)=C4Cl)C
MDL No. MFCD12407409
别名 PF-02341066; PF 2341066; (R)-Crizotinib
运输蓝冰
InChI Key KTEIFNKAUNYNJU-GFCCVEGCSA-N
Pubchem ID 11626560
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

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

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