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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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 |
+++
ROS1, IC50: 1.9 nM ALK, IC50: 0.37 nM |
FLT3 | 98% | ||||||||||||||||
NVP-TAE 684 |
+
ALK, IC50: 3 nM |
99%+ | |||||||||||||||||
Alectinib |
++
ALK, IC50: 1.9 nM ALK (F1174L), IC50: 3.5 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(G1202R), IC50: 1.26 nM ALK(L1196M), IC50: 1.01 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 |
MEK,FAK | 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。 |
靶点 |
|
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] |
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 | |
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.) |
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Administration | p.o., i.v. | ||||||||||||||||||||||||||||||||||||||||||||||||||
Pharmacokinetics |
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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 |
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 |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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 |