Ceritinib

别名: LDK378 中文名称:

Ceritinib是一种有效的ALK抑制剂,在无细胞试验中IC50为0.2 nM。Ceritinib (LDK378)还可抑制IGF-1RInsRSTK22DFLT3对应的IC50值分别为8 nM、7 nM、23 nM和60 nM。Phase 3。

Ceritinib Chemical Structure

Ceritinib Chemical Structure

CAS: 1032900-25-6

规格 价格 库存 购买数量
5mg 1182.86 现货
50mg 3868.47 现货
200mg 10720.71 现货
1g 23900 现货
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相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
KARPAS299 Apoptosis assay 60 nM 24 hrs Induction of apoptosis in human KARPAS299 cells harboring NPM-ALK at 60 nM after 24 hrs by acridine orange/ethidium bromide staining based fluorescence microscopic method 29174809
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK phosphorylation at Y1278 residue in human SU-DHL1 cells at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human NCI-H3122 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human NCI-H3122 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human SU-DHL1 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human SU-DHL1 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK phosphorylation at Y1278 residue in human NCI-H3122 cells at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human NCI-H3122 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 30 nM 16 hrs Inhibition of ALK autophosphorylation at Y1507 residue in human SU-DHL1 cells at 30 nM after 16 hrs by Western blot analysis 29627725
SU-DHL1 Function assay 30 nM 16 hrs Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 30 nM after 16 hrs by Western blot analysis 29627725
NCI-H3122 Function assay 50 to 250 nM 16 hrs Induction of ALK degradation in human NCI-H3122 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method 29660984
KARPAS299 Function assay 50 to 250 nM 16 hrs Induction of ALK degradation in human KARPAS299 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method 29660984
KARPAS299 Apoptosis assay 50 nM 24 hrs Induction of apoptosis in human KARPAS299 cells assessed as unclear cell shrinkage at 50 nM after 24 hrs by Hoechst 33258 staining based inverted fluorescence microscopy 30223120
KARPAS299 Apoptosis assay 50 nM 24 hrs Induction of apoptosis in human KARPAS299 cells assessed as late apoptotic cells at 50 nM after 24 hrs by AO/EB double staining based inverted fluorescence microscopy 30223120
KARPAS299 Apoptosis assay 50 nM 24 hrs Induction of apoptosis in human KARPAS299 cells assessed as fragmentation at 50 nM after 24 hrs by Hoechst 33258 staining based inverted fluorescence microscopy 30223120
Ba/F3 NA C1156Y Growth Inhibition Assay 72 h IC50=0.071 μM 25727400
Ba/F3 NA WT Growth Inhibition Assay 72 h IC50=0.020 μM 25727400
C1156F/D1203N 2809 Growth Inhibition Assay 72 h IC50=254 ± 99 nM 25749034
E1210K 748 Growth Inhibition Assay 72 h IC50=187 ± 84 nM 25749034
N1178H 169 Growth Inhibition Assay 72 h IC50=42 ± 6 nM 25749034
F1174I 184 Growth Inhibition Assay 72 h IC50=13 ± 0.1 nM 25749034
I1171T 445 Growth Inhibition Assay 72 h IC50=82 ± 12 nM 25749034
I1171N 519 Growth Inhibition Assay 72 h IC50=187 ± 87 nM 25749034
C1156F 1293 Growth Inhibition Assay 72 h IC50=217 ± 115 nM 25749034
G1128S 1022 Growth Inhibition Assay 72 h IC50=102 ± 38 nM 25749034
WT 70 Growth Inhibition Assay 72 h IC50=21 ± 8 nM 25749034
Parental(+IL3) Growth Inhibition Assay 72 h IC50=1586 ± 173 nM 25749034
Ba/F3 NA L1196M Growth Inhibition Assay 72 h IC50=0.042 μM 25727400
Ba/F3 NA L1152R Growth Inhibition Assay 72 h IC50=0.288 μM 25727400
Ba/F3 NA G1202R Growth Inhibition Assay 72 h IC50=0.277 μM 25727400
Ba/F3 NA G1269A Growth Inhibition Assay 72 h IC50=0.019 μM 25727400
Ba/F3 NA S1206Y Growth Inhibition Assay 72 h IC50=0.037 μM 25727400
Ba/F3 EA WT Growth Inhibition Assay 72 h IC50=0.021 μM 25727400
Ba/F3 EA C1156Y Growth Inhibition Assay 72 h IC50=0.026 μM 25727400
Ba/F3 EA L1196M Growth Inhibition Assay 72 h IC50=0.019 μM 25727400
Ba/F3 EA L1152R Growth Inhibition Assay 72 h IC50=0.099 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 S1206Y Growth Inhibition Assay 72 h IC50=0.038 μM 25727400
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.0107 μM. 29288940
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.015 μM. 26568289
NCI-H2228 Growth inhibition assay 3 days Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay, IC50 = 0.015 μM. 29627725
SU-DHL1 Growth inhibition assay 3 days Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay, IC50 = 0.015 μM. 29627725
DFCI114 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.018 μM. 26568289
HCC78 Cytotoxicity assay 72 hrs Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.018 μM. 27474925
KARPAS299 Cytotoxicity assay 2 to 3 days Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.0228 μM. 23742252
NCI-H3122 Function assay 72 hrs Inhibition of EML4 fused ALK in human NCI-H3122 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.025 μM. 27915169
BAF3 Function assay 2 to 3 days Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.026 μM. 23742252
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.026 μM. 29174809
NCI-H2228 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.026 μM. 30223120
KARPAS299 Cytotoxicity assay 72 hrs Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.027 μM. 27474925
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.033 μM. 26568289
NCI-H3122 Function assay 72 hrs Inhibition of EML4-ALK in human NCI-H3122 cells assessed as inhibition of cell proliferation after 72 hrs by SRB assay, CC50 = 0.038 μM. 26923695
NCI-H3122 Function assay 72 hrs Inhibition of EML4-ALK in human NCI-H3122 cells assessed as inhibition of cell proliferation after 72 hrs by SRB assay, CC50 = 0.038 μM. 26923695
NCI-H3122 Function assay 72 hrs Inhibition of EML4 fused ALK in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB assay, CC50 = 0.038 μM. 28385505
Ba/F3 Function assay 72 hrs Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.041 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.041 μM. 26568289
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.041 μM. 30223120
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.0549 μM. 29288940
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.057 μM. 26568289
HCC78 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.058 μM. 29174809
HCC78 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.058 μM. 30223120
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.064 μM. 26568289
DFCI76 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.072 μM. 26568289
BA/F3 Function assay 72 hrs Inhibition of ALK L1196M mutant in mouse BA/F3 cells assessed as inhibition of cell proliferation after 72 hrs by WST1 assay, CC50 = 0.075 μM. 26923695
BA/F3 Function assay 72 hrs Inhibition of EML4 fused ALK L1196M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.075 μM. 27915169
BA/F3 Function assay 72 hrs Inhibition of EML4 fused ALK (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.075 μM. 27915169
BAF3 Function assay 72 hrs Inhibition of ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by WST-1 assay, CC50 = 0.075 μM. 28385505
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.084 μM. 29288940
SMS-KCNR Antiproliferative assay 72 hrs Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.092 μM. 26568289
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.096 μM. 29288940
NCI-H2228 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.099 μM. 29174809
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.101 μM. 26568289
NCI-H2228 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H2228 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.1026 μM. 25644671
LAN5 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.122 μM. 26568289
SU-DHL1 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.122 μM. 29288940
Kelly Antiproliferative assay 72 hrs Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.142 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.164 μM. 26568289
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.186 μM. 26568289
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.234 μM. 29288940
SK-N-SH Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.303 μM. 26568289
BAF3 Function assay 2 to 3 days Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.3195 μM. 23742252
SK-N-FI Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.349 μM. 26568289
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.363 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.444 μM. 26568289
LAN1 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.549 μM. 26568289
SK-N-BE(2) Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.593 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.668 μM. 26568289
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.726 μM. 29288940
Ba/F3 Function assay 72 hrs Inhibition of human EGFR del19/T790M/C797S mutant expressed in mouse Ba/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo assay, GI50 = 0.7805 μM. 29136465
SK-N-AS Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.045 μM. 26568289
BAF3 Cytotoxicity assay 2 to 3 days Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 2.477 μM. 23742252
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 2.747 μM. 26568289
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 5.512 μM. 26568289
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay 29660984
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay 29660984
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
SU-DHL1 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL1 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
KARPAS299 Cytotoxicity assay Cytotoxicity against human KARPAS299 cells expressing NPM-ALK fusion gene assessed as growth inhibition, IC50 = 0.0228 μM. 23837797
BA/F3 Cytotoxicity assay Cytotoxicity against mouse BA/F3 cells expressing NPM-ALK fusion gene assessed as growth inhibition, IC50 = 0.026 μM. 23837797
NCI-H3122 Antiproliferative assay Antiproliferative activity against wild type human NCI-H3122 cells, CC50 = 0.038 μM. 26235945
BA/F3 Function assay Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells, IC50 = 0.0407 μM. 23837797
BAF3 Antiproliferative assay Antiproliferative activity against mouse BAF3 cells expressing ALK L1196M mutant, CC50 = 0.075 μM. 26235945
BA/F3 Cytotoxicity assay Cytotoxicity against mouse BA/F3 cells transfected with Tel-InsR gene assessed as growth inhibition, IC50 = 0.32 μM. 23837797
点击查看更多细胞系数据

生物活性

产品描述 Ceritinib是一种有效的ALK抑制剂,在无细胞试验中IC50为0.2 nM。Ceritinib (LDK378)还可抑制IGF-1RInsRSTK22DFLT3对应的IC50值分别为8 nM、7 nM、23 nM和60 nM。Phase 3。
特性 不与c-Met交叉反应,对体内葡萄糖稳态比TAE684效果好,有效作用于 Crizotinib复发的肿瘤。
靶点
ALK [1]
(Cell-free assay)
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
STK22D [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
0.2 nM 7 nM 8 nM 23 nM 60 nM
体外研究(In Vitro)
体外研究活性 LDK378作用于Ba/F3-NPM-ALK和Karpas290细胞,具有显著的抗增殖活性,IC50分别为26.0 nM 和 22.8 nM,作用于Ba/F3-Tel-InsR 和Ba/F3-WT细胞,IC50分别为319.5 nM 和 2477 nM。[1]
激酶实验 激酶分析
所有激酶使用杆状病毒表达技术表达为组氨酸或GST标签的融合蛋白,除了在大肠杆菌中产生的未标记的ERK2。在LabChip迁移实验中测量激酶活性。实验在30°C下进行60分钟。在有或无LDK378存在时,通过线性进展曲线,获得LDK378对酶活性的作用效果。
细胞实验 细胞系 Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 细胞
浓度 ~100 μM
孵育时间 2-3 天
方法 表达荧光素酶的细胞与连续稀释的LDK378 或 DMSO 温育2-3天。荧光素酶的表达用来衡量细胞增殖/存活,使用Bright-Glo萤光素酶检测系统来评估。使用 XLFit软件获得 IC50值。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-ALK / ALK / p-AKT / AKT / p-ERK / ERK pROS1 / ROS1 / pSTAT3 / STAT3 28425916
Growth inhibition assay Cell viability 29067644
体内研究(In Vivo)
体内研究活性 LDK378 用于降低形成反应代谢的可能性,在肝微粒体几乎检测不到谷胱甘肽(GSH)加合物的水平(<1%)。LDK378具有相对良好的代谢稳定性,中度抑制CYP3A4(Midazolam底物)和抑制hERG。LDK378处理动物,与肝脏血流量相比,具有低的血浆清除率(小鼠,大鼠,狗和猴),处理小鼠,大鼠,狗和猴的口服生物利用度都在55%以上。LDK378 处理Karpas299 和H2228 大鼠移植瘤模型,抑制肿瘤生长,诱导肿瘤衰退,这种作用具有剂量依赖性,体重没有降低。LDK378处理小鼠,剂量高达100 mg/kg,对胰岛素水平或血浆葡萄糖的利用无影响。[1]
动物实验 Animal Models 携带 Karpas299/H2228肿瘤的 RNU裸鼠
Dosages ~50 mg/kg
Administration 口服饲喂
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02450903 Completed
Non-Small-Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
August 21 2015 Phase 2
NCT02040870 Completed
Non-Small Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
March 7 2014 Phase 1|Phase 2
NCT01950481 Completed
Normal Hepatic Function|Impaired Hepatic Function
Novartis Pharmaceuticals|Novartis
January 2014 Phase 1
NCT01772797 Completed
Anaplastic Lymphoma Kinase (ALK)|Non-small Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
June 2013 Phase 1
NCT01685060 Completed
Non-Small Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
November 26 2012 Phase 2
NCT01634763 Completed
Tumors Characterized by Genetic Alterations in Anaplastic Lymphoma Kinase (ALK)
Novartis Pharmaceuticals|Novartis
June 2012 Phase 1

化学信息&溶解度

分子量 558.14 分子式

C28H36ClN5O3S

CAS号 1032900-25-6 SDF Download Ceritinib SDF
Smiles CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 4 mg/mL ( (7.16 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

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操作手册

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常见问题及建议解决方法

问题 1:
how to reconstitute the inhibitor for oral administration to mice?

回答:
You can resuspend LDK378 in 30% PEG400/0.5% Tween 80/5% propylene glycol and use the suspension for oral gavage feeding.

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