Ceritinib | LDK378 | ALK | IGF-1R | Insulin Receptor | AmBeed-信号通路专用抑制剂

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色瑞替尼 /Ceritinib {[allProObj[0].p_purity_real_show]}

货号：A126440 同义名： LDK378

Ceritinib（LDK378）是一种选择性、口服可用的、ATP竞争性的ALK酪氨酸激酶抑制剂，IC50为200 pM。Ceritinib（LDK378）还以8、7和23 nM的IC50值抑制IGF-1R、InsR和STK22D。Ceritinib（LDK378）显示出强大的抗肿瘤活性。

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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+

Ceritinib 化学结构
CAS号：1032900-25-6

Ceritinib 3D分子结构
CAS号：1032900-25-6

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Ceritinib 纯度/质量文件产品仅供科研

货号：A126440 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

ALK 亚型比较
IGF-1R 亚型比较

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	++++ ROS1, Ki: <0.025 nM ALK, IC50: 24 nM		98%
Entrectinib	✔		99%+
Brigatinib	+++ ROS1, IC50: 1.9 nM ALK, IC50: 0.37 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	IGF-1R,Insulin Receptor	98%
GSK1838705A	+++ ALK, IC50: 0.5 nM	IGF-1R,Insulin Receptor	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。

产品名称	IGF-1R ↓ ↑	Insulin Receptor ↓ ↑	其他靶点	纯度
BMS-536924	++ IGF-1R, IC50: 100 nM	+++ Insulin Receptor, IC50: 73 nM	FAK,MEK	98%
GSK1904529A	+++ IGF-1R, IC50: 27 nM	+++ Insulin Receptor, IC50: 25 nM		98+%
Picropodophyllin	++++ IGF-1R, IC50: 1 nM			99%+
NVP-AEW541	++ IGF-1R, IC50: 0.15 μM	++ Insulin Receptor, IC50: 0.14 μM	FLT3	99%+
NVP-ADW742	+ IGF-1R, IC50: 0.17 μM			99%
GSK1838705A	+++ IGF-1R, IC50: 2 nM	++++ Insulin Receptor, IC50: 1.6 nM	ALK	99%
BMS-754807	++++ IGF-1R, IC50: 1.8 nM	++++ Insulin Receptor, IC50: 1.7 nM		99%+
Linsitinib	+++ IGF-1R, IC50: 35 nM	++ Insulin Receptor, IC50: 75 nM		99%+
AG1024	+ IGF-1R, IC50: 7 μM	+ Insulin Receptor, IC50: 57 μM		98%
PQ401	+ IGF-1R, IC50: <1 μM			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。

Ceritinib 生物活性

靶点	ALK ALK, IC50:0.2 nM
描述	ALK (anaplastic lymphoma kinase) is a tyrosine kinase that is constitutively activated in certain cancers, following gene alterations such as chromosomal translocation, amplification or point mutation. Ceritinib is a selective inhibitor of ALK with IC50 value of 0.2nM (measured by enzymatic kinase activity), and less potent to FLT3, IGF-1R, InsR and STK22D with IC50 values of 60nM, 8nM, 7nM and 23nM, respectively, and showed inhibitory activity on celluar kinase in Ba/F3 cells with IC50 values of 40.7nM, 2.2nM, 410nM and 141.8nM for Tel-ALK, EML4-ALK, Tel-IGF-1R and Tel-Ros, respectively. The cell proliferation study showed that Ceritinib exhibited preferential anti-proliferative activity in Ba/F3 cells expressing NPM-ALK (26nM) and in Karpas299 cells with NPM-ALK fusion (22.8nM)^[1]. As the second generation of ALK inhibitor, Ceritinib can overcome several crizotinib resistant mutations in non–small cell lung cancers, including in two ALK-rearranged lung cancer cell lines H3122 and H2228, ALK-mutant cells, H3122 CR1 (L1196M), MGH021-4 (G1269A) and MGH045 (L1196M) cells, as well as ALK wild-type (WT) crizotinib-resistant MGH051 cells from patient, and lead inhibition on p-ALK, p-AKT, p-ERK,p-S6 and cell proliferation at much lower dose than Crizotinib. Consistent with the in vitro study, ceritinib showed more potent anti-tumor activity at dose (50mg/kg) lower than crizotinib (100mg/kg) in mice bearing crizotinib-resistant tumors harboring EML4–ALK wild-type, I1171T, or C1156Y mutations^[2].
作用机制	Ceritinib is an ATP-competitive ALK inhibitor.^[1]

Ceritinib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
Ba/F3 EA C1156Y		Growth Inhibition Assay	72 h	IC50=0.026 μM	25727400
Ba/F3 EA G1202R		Growth Inhibition Assay	72 h	IC50=0.467 μM	25727400
Ba/F3 EA G1269A		Growth Inhibition Assay	72 h	IC50=0.033 μM	25727400
Ba/F3 EA L1152R		Growth Inhibition Assay	72 h	IC50=0.099 μM	25727400

Ceritinib 动物研究

Dose

Nude Mice: 25 mg/kg, 50 mg/kg^[4] (p.o.)
Mice: 5 mg/kg - 25 mg/kg^[1] (i.v.), 20 mg/kg^[1] (p.o.)
Rat: 3 mg/kg - 10 mg/kg^[1] (p.o.)

Administration

p.o., i.v.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]	Dogs^[1]	Monkeys^[1]
Dose	5 mg/kg (i.v.) 20 mg/kg (p.o.)	3 mg/kg (i.v.) 10 mg/kg (p.o.)	5 mg/kg (i.v.) 20 mg/kg (p.o.)	5 mg/kg (i.v.) 60 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.	i.v. p.o.	i.v. p.o.
F	95% (p.o.)	66% (p.o.)	119% (p.o.)	56% (p.o.)
T_1/2	6.2 h (i.v.)	9.1 h (i.v.)	21 h (i.v.)	26 h (i.v.)
T_max	0.03 h (i.v.) 7.0 h (p.o.)	0.03 h (i.v.) 7.0 h (p.o.)	0.03 h (i.v.) 8.0 h (p.o.)	7 h (i.v.) 13 h (p.o.)
CL	26.6 ml/min/kg (i.v.)	26.6 ml/min/kg (i.v.)	9.2 ml/min/kg (i.v.)	12.8 ml/min/kg (i.v.)
C_max	1756 nM (i.v.) 696 nM (p.o.)	770 nM (i.v.) 259 nM (p.o.)	2329 nM (i.v.) 1899 nM (p.o.)	2526 nM (i.v.) 169 nM (p.o.)
Vss	9.7 L/kg (i.v.)	21.2 L/kg (i.v.)	13.5 L/kg (i.v.)	15 L/kg (i.v.)
AUC	5634 hrs·nM (i.v.) 12296 hrs·nM (p.o.)	2779 hrs·nM (i.v.) 6092 hrs·nM (p.o.)	6790 hrs·nM (p.o.)	11305 hrs·nM (i.v.) 763 hrs·nM (p.o.)

Ceritinib 参考文献

[1]Marsilje TH, Pei W, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013;56(14):5675-90.

[2]Friboulet L, Li N, et al. The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer. Cancer Discov. 2014;4(6):662-673.

[3]Burns MW, Kim ES. Profile of ceritinib in the treatment of ALK+ metastatic non-small-cell lung cancer. Lung Cancer (Auckl). 2015.

[4]van Erp AEM, Hillebrandt-Roeffen MHS, et al. Targeting Anaplastic Lymphoma Kinase (ALK) in Rhabdomyosarcoma (RMS) with the Second-Generation ALK Inhibitor Ceritinib. Target Oncol. 2017 Dec;12(6):815-826.

Ceritinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.79mL

0.36mL

0.18mL

8.96mL

1.79mL

0.90mL

17.92mL

3.58mL

1.79mL

Ceritinib 技术信息

CAS号	1032900-25-6
分子式	C₂₈H₃₆ClN₅O₃S
分子量	558.135

别名	LDK378
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,Inert atmosphere,2-8°C

溶解度

DMSO: 12 mg/mL(21.5 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

IP 10% DMSO+water 0.5 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

色瑞替尼 /Ceritinib {[allProObj[0].p_purity_real_show]}

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色瑞替尼 /Ceritinib {[allProObj[0].p_purity_real_show]}

Ceritinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Ceritinib 质控信息

Ceritinib 生物活性

Ceritinib 细胞研究

Ceritinib 动物研究

Ceritinib 参考文献

Ceritinib 实验方案

Ceritinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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临床研究

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