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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。 |
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. The fusion protein NPM-ALK, which is generated from a hybrid gene consisting of the intracellular domain of the ALK tyrosine kinase receptor juxtaposed with nucleophosmin, has constitutive tyrosine kinase activity and is associated with 50–60% of cases of anaplastic large-cell lymphomas. NVP-TAE 684 is a potent and selective NPM-ALK kinase inhibitor without exhibiting significant cross-reactivity against other kinases tested, including the highly homologous InsR. Consistent with this, NVP-TAE 684 exhibited inhibitory concentrations (IC50) between 2 and 5nM in NPM-ALK-dependent cells, Ba/F3 NPM-ALK, SU-DHL-1 and Karpas-299, but not the parent Ba/F3-WT cells, with a dose-dependent reduction of NPM-ALK auto-phosphorylation. Through the inhibition of NPM-ALK kinase activity, the downstream signaling events, pSTAT3-Y705 and pSTAT5-Y694, were inhibited in a concentration- (>50nM) and time (50nM, >15min)-dependent manner in Ba/F3 NPM-ALK and Karpas-299 cells. Also, NVP-TAE 684 (>50nM) can lead a dose-dependent reduction in phosphorylation of both ERK and Akt in Karpas-299 cells after 4h of treatment. The G1 phase arrest and apoptosis induced by treatment with 50nM NVP-TAE 684 for 48h can be observed in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines. Oral administration of NVP-TAE 684 at dose of 3 and 10mg/kg once daily for 4 weeks significantly delayed lymphoma development in Karpas-299 xenograft mice. Daily oral administration of NVP-TAE 684 at dose of 5 or 10mg/kg for 2 weeks initiated 12 days after Karpas-299 inoculation induced disease regression in mice. Reduction of p-ALK and p-STAT3, as well as CD30 expression (present as the ALCLs) can be observed at day 3 after dose[1]. |
作用机制 | NVP-TAE 684 is expected to bind with the ATP-binding site of ALK.[1] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
697 | Growth Inhibition Assay | IC50=0.43215 μM | SANGER | ||
8-MG-BA | Growth Inhibition Assay | IC50=2.65414 μM | SANGER | ||
A101D | Growth Inhibition Assay | IC50=1.57113 μM | SANGER | ||
A388 | Growth Inhibition Assay | IC50=2.9617 μM | SANGER | ||
Dose | Mice: 1 mg/kg - 20 mg/kg[1] (p.o.), 0.5 mg/kg[2] (p.o.) | ||||||||||||
Administration | p.o. | ||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.63mL 0.33mL 0.16mL |
8.14mL 1.63mL 0.81mL |
16.28mL 3.26mL 1.63mL |
CAS号 | 761439-42-3 |
分子式 | C30H40ClN7O3S |
分子量 | 614.202 |
别名 | TAE 684 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 6 mg/mL(9.77 mM),配合低频超声助溶,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 |