Crizotinib hydrochloride

目录号：S5190 批次号：S519003

化学数据

	别名	Xalkori, PF-02341066 hydrochloride	储存条件 (自收到货起)	3年 -20°C 粉状
	化学式	C₂₁H₂₃Cl₃FN₅O
	分子量	486.8	CAS号	1415560-69-8
Solubility (25°C)*	体外	DMSO	97 mg/mL (199.26 mM)
		Water	97 mg/mL (199.26 mM)
		Ethanol	97 mg/mL (199.26 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

产品描述

Crizotinib (PF-02341066) hydrochloride (Xalkori) 可抑制 c-Met 和核磷脂(NPM)-anaplastic lymphoma kinase (ALK) 的酪氨酸磷酸化，对应基于细胞的测定中的IC50值分别为 11 nM 和 24 nM。Crizotinib hydrochloride 也是一种有效的 ROS1 的抑制剂，Ki值小于0.025 nM。Crizotinib 可通过抑制多种肺癌细胞系中的STAT3途径诱导自噬。

靶点

ROS1 ^[2] (Cell-free assay)	c-Met ^[1] (Cell-based assay)	NPM-ALK ^[2] (Cell-based assay)
<0.025 nM(Ki)	11 nM	24 nM

参考文献

[4] Zou HY, et al. Cancer Res. 2007, 67(9), 4408-4417.

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Crizotinib hydrochloride在文献中得到引用

NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations [ Cancer Discov, 2023, 13(3):598-615]	PubMed: 36511802
Adaptive c-Met-PLXDC2 Signaling Axis Mediates Cancer Stem Cell Plasticity to Confer Radioresistance-associated Aggressiveness in Head and Neck Cancer [ Cancer Res Commun, 2023, 3(4):659-671]	PubMed: 37089864
Efficacy of CAR-T immunotherapy in MET overexpressing tumors not eligible for anti-MET targeted therapy [ J Exp Clin Cancer Res, 2022, 41(1):309]	PubMed: 36271379
EGFR/MET promotes hepatocellular carcinoma metastasis by stabilizing tumor cells and resisting to RTKs inhibitors in circulating tumor microemboli [ Cell Death Dis, 2022, 13(4):351]	PubMed: 35428350
HER3 activation contributes toward the emergence of ALK inhibitor-tolerant cells in ALK-rearranged lung cancer with mesenchymal features [ NPJ Precis Oncol, 2022, 6(1):5]	PubMed: 35042943
The multi-kinase inhibitor afatinib serves as a novel candidate for the treatment of human uveal melanoma [ Cell Oncol (Dordr), 2022, 45(4):601-619]	PubMed: 35781872
Establishment and large-scale validation of a three-dimensional tumor model on an array chip for anticancer drug evaluation [ Front Pharmacol, 2022, 13:1032975]	PubMed: 36313330
Novel human-derived EML4-ALK fusion cell lines identify ribonucleotide reductase RRM2 as a target of activated ALK in NSCLC [ Lung Cancer, 2022, 171:103-114]	PubMed: 35933914
MYC promotes tyrosine kinase inhibitor resistance in ROS1 fusion-positive lung cancer [ Mol Cancer Res, 2022, molcanres.MCR-22-0025-E.2022]	PubMed: 35149545
MET Exon 14 Splice-Site Mutations Preferentially Activate KRAS Signaling to Drive Tumourigenesis [ Cancers (Basel), 2022, 14(6)1378]	PubMed: 35326531

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如果需要长期保存，请于零下二十度低温保存。禁止用于人体及治疗！

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