Ceritinib dihydrochloride

目录号：S4967 批次号：S496701

化学数据

	别名	Zykadia, LDK378 dihydrochloride	储存条件 (自收到货起)	3年 -20°C 粉状
	化学式	C₂₈H₃₈Cl₃N₅O₃S
	分子量	631.06	CAS号	1380575-43-8
Solubility (25°C)*	体外	DMSO	13 mg/mL (20.6 mM)
		Ethanol	10 mg/mL (15.84 mM)
		Water	Insoluble
* <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.

制备储备液

生物活性

产品描述

Ceritinib (Zykadia, LDK378) dihydrochloride 是一种选择性的、口服可生物利用的、具有ATP竞争性的 ALK 的抑制剂，其IC50值为0.2 nM。Ceritinib dihydrochloride 也抑制 InsR、IGF-1R 和 STK22D，对应的IC50值分别为7 nM、8 nM和23 nM。Ceritinib 具有抗肿瘤活性。

靶点

ALK ^[1] (Cell-free assay)	InsR ^[1] (Cell-free assay)	IGF-1R ^[1] (Cell-free assay)	STK22D ^[1] (Cell-free assay)
0.2 nM	7 nM	8 nM	23 nM

参考文献

Ceritinib dihydrochloride在文献中得到引用

Crizotinib attenuates cancer metastasis by inhibiting TGFβ signaling in non-small cell lung cancer cells [ Exp Mol Med, 2022, 54(8):1225-1235]	PubMed: 35999455
Repurposing Ceritinib Induces DNA Damage and Enhances PARP Inhibitor Responses in High-Grade Serous Ovarian Carcinoma [ Cancer Res, 2022, 82(2):307-319]	PubMed: 34810199
STAT3 inhibition suppresses adaptive survival of ALK-rearranged lung cancer cells through transcriptional modulation of apoptosis [ NPJ Precis Oncol, 2022, 6(1):11]	PubMed: 35228642
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
Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models [ BMC Cancer, 2022, 22(1):752]	PubMed: 35820889
The CLIP1-LTK fusion is an oncogenic driver in non-small-cell lung cancer [ Nature, 2021, 600(7888):319-323]	PubMed: 34819663
Cell Type-specific Adaptive Signaling Responses to KRASG12C Inhibition [ Clin Cancer Res, 2021, 27(9):2533-2548]	PubMed: 33619172
Pharmacological inhibitors of anaplastic lymphoma kinase (ALK) induce immunogenic cell death through on-target effects [ Cell Death Dis, 2021, 12(8):713]	PubMed: 34272360
TPX-0131, a Potent CNS-Penetrant, Next-Generation Inhibitor of Wild-Type ALK and ALK-Resistant Mutations [ Mol Cancer Ther, 2021, molcanther.0221.2021]	PubMed: 34158340

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20°C，抑制剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

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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