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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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+ |
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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 |
99%+ | |||||||||||||||||
Crizotinib |
++++
ROS1, Ki: <0.025 nM ALK, IC50: 24 nM |
99%+ | |||||||||||||||||
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 | 99% | ||||||||||||||||
AZD-3463 |
++
ALK, Ki: 0.75 nM |
IGF-1R | 99% | ||||||||||||||||
Lorlatinib |
++++
ROS1, Ki: <0.07 nM ALK (L1196M), 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。 |
靶点 |
|
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] |
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 | ||
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 |
|
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 | - | - |
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 |
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 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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 |