首页 Angiogenesis ALK LDK378
LDK378
编号 T1791     别名: Ceritinib
CAS 1032900-25-6     分子式 C28H36ClN5O3S     分子量 558.14
靶点: ALK; FLT3; IGF-1R; Insulin Receptor; STK22D;
Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).
选择批次  
规格 库存 单价 数量
5 mg 上海现货 489.00
10 mg 上海现货 698.00
50 mg 上海现货 2152.00
100 mg 上海现货 3102.00
200 mg 上海现货 5192.00
1 mL * 10 mM (in DMSO) 上海现货 611.00
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生物活性

产品描述

Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).

靶点活性

ALK,0.2 nM (cell free)

FLT3,60nM

IGF-1R,8 nM (cell free)

Insulin Receptor,7 nM (cell free)

STK22D,23 nM (cell free)

体外活性

Ceritinib (LDK378) also inhibits RET (IC50: 400 nM), FGFR3 (IC50: 430 nM), LCK (IC50: 560 nM), JAK2 (IC50: 610 nM), Aurora (IC50: 660 nM), LYN (IC50: 840 nM), EGFR (IC50: 900 nM), and FGFR4 (IC50: 950 nM) [1]. In ALK-positive cell line models, ceritinib was able to effectively inhibit ALK harboring the crizotinib-resistant mutations L1196M, G1269A, I1171T, and S1206Y, but it was ineffective at inhibiting ALK containing the G1202R and F1174C mutations.49 Among a panel of 46 other tested kinases, ceritinib showed strong activity only against IGF-1R (IC50: 8 nM), INSR (IC50: 7 nM), and STK22D (IC50: 23 nM) [2].

体内活性

Mice treated with ceritinib at 50 mg/kg remained in complete remission with no discernible tumor growth for 4 months. In the mice treated with ceritinib at 25 mg/kg, tumor re-growth was observed in 4 out of 8 animals after 1 month, whereas complete remission was maintained in the other 4 animals for 4 months. In a primary explant model derived from a crizotinib-naïve NSCLC tumor MGH006, treatment with 25 mg/kg ceritinib also led to tumor regressions [3].

激酶实验

All kinases were expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which was produced in E. coli. The kinase activity was measured in the LabChip mobility-shift assay. The assay was performed at 30°C for 60 min. The effect of the compound on the enzymatic activity was obtained from the linear progress curves in the absence and presence of compound and routinely determined from one reading (end point measurement) [1].

细胞实验

Luciferase-expressing cells were incubated with serial dilutions of compounds or DMSO for 2–3 days. Luciferase expression was used as a measure of cell proliferation/survival and was evaluated with the Bright-Glo Luciferase Assay System. IC50 values were generated by using XLFit software [1].

细胞系: Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 cells

动物实验

SCID beige mice for crizotinib-resistant H2228 xenograft tumor models, nude mice for MGH006 primary explants and MGH045 cells were randomized into groups of 5, 6 or 8 mice with an average tumor volume of ~150 mm^3 and received Crizotinib or ceritinib daily treatments by oral gavage as indicated in each study. Tumor volumes were determined by using caliper measurements and calculated with the formula (Length × Width × Height)/2 [3].

动物模型:RNU nude rats bearing the Karpas299/H2228 tumors

化学信息

分子量

558.14

分子式

C28H36ClN5O3S

CAS

1032900-25-6

溶解度

DMSO: 16 mg/mL (28.7 mM)

Ethanol: 3 mg/mL (5.37 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.792 ml 8.958 ml 17.917 ml
5 mM 0.358 ml 1.792 ml 3.583 ml
10 mM 0.179 ml 0.896 ml 1.792 ml
50 mM 0.036 ml 0.179 ml 0.358 ml
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