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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
TAE684 (NVP-TAE684), ALK 受体酪氨酸激酶抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
TAE684 (NVP-TAE684)是一种有效的，选择性的ALK抑制剂，IC50为3 nM，作用于ALK比作用于InsR选择性高100倍。A selective NPM-ALK phosphorylation inhibitor which also inhibits ALK and LRRK2 Kinase
Information
TAE684 (NVP-TAE684) TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis .
In vitro
TAE684 does not exhibit significant cross-reactivity against other kinases. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. TAE684 also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. Molecular modeling reveals that L258 may be one of the major kinase-selectivity determinants for TAE684. TAE684 treatment results in a rapid and sustained inhibition of phosphorylation of NPM-ALK. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines. TAE684 markedly overcomes Crizotinib-resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis. Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by TAE684 at 30 nM.
In vivo
After 4 weeks of treatment with TAE684 at 3 and 10 mg/kg, there is a significant delay in lymphoma development and 100- to 1,000-fold reduction in luminescence signal, without any signs of compound- or disease-related toxicity in Karpas-299 lymphoma model. TAE684 treatment also induces disease regression in established Karpas-299 lymphomas and down-regulates CD30 expression. TAE684 also shows impressive antitumor activity against H3122 CR xenograft tumors. Furthermore, treatment with TAE684 improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q, whereas Crizotinib has little effect on either phenotype.
Cell Data
cell lines：
Concentrations：1 nM-10 μM
Incubation Time：2–3 days
Powder Purity:≥97%
规格
英文别名
5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine
规格或纯度
Moligand™, 2mM in DMSO
英文名称
TAE684 (NVP-TAE684)
生化机理
TAE684（NVP-TAE684）是一种强效的选择性 ALK 抑制剂，在无细胞实验中的 IC50 为 3 nM，对 ALK 的敏感性是 InsR 的 100 倍。TAE684 (NVP-TAE684) 可诱导细胞周期停滞和细胞凋亡。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
ALK 受体酪氨酸激酶抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC
PubChem CID
分子量
614.2
技术文档
高级数据
关联靶点（人）
CDS2
Tbio
磷脂酰胞苷酸转移酶2(Phosphatidate cytidylyltransferase 2)
(0 活性数据)
ERBB4
Tclin
受体酪氨酸蛋白激酶 erbB-4(Receptor tyrosine-protein kinase erbB-4)
(1 活性数据)
EGFR
Tclin
表皮生长因子受体(Epidermal growth factor receptor)
(3 活性数据)
PTK2
Tclin
粘着斑激酶1(Focal adhesion kinase 1)
(1 活性数据)
PTK6
Tchem
蛋白酪氨酸激酶 6(Protein-tyrosine kinase 6)
(1 活性数据)
SRC
Tclin
原癌基因酪氨酸蛋白激酶Src(Proto-oncogene tyrosine-protein kinase Src)
(1 活性数据)
ROS1
Tclin
原癌基因酪氨酸蛋白激酶ROS(Proto-oncogene tyrosine-protein kinase ROS)
(2 活性数据)
FLT4
Tclin
血管内皮生长因子受体 3(Vascular endothelial growth factor receptor 3)
(1 活性数据)
YES1
Tclin
酪氨酸蛋白激酶 是(Tyrosine-protein kinase Yes)
(1 活性数据)
FER
Tclin
酪氨酸蛋白激酶Fer(Tyrosine-protein kinase Fer)
(1 活性数据)
FLT3
Tclin
受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3)
(8 活性数据)
GAK
Tchem
细胞周期蛋白G相关激酶(Cyclin-G-associated kinase)
(1 活性数据)
FGFR1
Tclin
成纤维细胞生长因子受体 1(Fibroblast growth factor receptor 1)
(2 活性数据)
FGFR4
Tclin
成纤维细胞生长因子受体 4(Fibroblast growth factor receptor 4)
(2 活性数据)
IGF1R
Tclin
胰岛素类生长因子 1 受体(Insulin-like growth factor 1 receptor)
(2 活性数据)
ITK
Tclin
酪氨酸蛋白激酶 ITK/TSK(Tyrosine-protein kinase ITK/TSK)
(1 活性数据)
JAK3
Tclin
酪氨酸蛋白激酶JAK3(Tyrosine-protein kinase JAK3)
(1 活性数据)
MERTK
Tchem
酪氨酸蛋白激酶(Tyrosine-protein kinase Mer)
(2 活性数据)
SIK1
Tchem
丝氨酸/苏氨酸蛋白激酶 SIK1(Serine/threonine-protein kinase SIK1)
(1 活性数据)
SIK2
Tchem
丝氨酸/苏氨酸蛋白激酶SIK2(Serine/threonine-protein kinase SIK2)
(1 活性数据)
TAOK1
Tchem
丝氨酸/苏氨酸蛋白激酶 TAO1(Serine/threonine-protein kinase TAO1)
(1 活性数据)
TEK
Tclin
血管生成素-1受体(Angiopoietin-1 receptor)
(1 活性数据)
SLK
Tchem
STE20 类丝氨酸/苏氨酸蛋白激酶(STE20-like serine/threonine-protein kinase)
(2 活性数据)
PLK4
Tchem
丝氨酸/苏氨酸蛋白激酶 PLK4(Serine/threonine-protein kinase PLK4)
(2 活性数据)
PLK1
Tchem
丝氨酸/苏氨酸蛋白激酶 PLK1(Serine/threonine-protein kinase PLK1)
(1 活性数据)
RPS6KA6
Tchem
核糖体蛋白 S6 激酶 α-6(Ribosomal protein S6 kinase alpha-6)
(1 活性数据)
LTK
Tclin
白细胞酪氨酸激酶受体(Leukocyte tyrosine kinase receptor)
(1 活性数据)
LRRK2
Tchem
富含亮氨酸重复丝氨酸/苏氨酸蛋白激酶 2(Leucine-rich repeat serine/threonine-protein kinase 2)
(5 活性数据)
BMPR1B
Tchem
骨形态发生蛋白受体 1B 型(Bone morphogenetic protein receptor type-1B)
(1 活性数据)
BTK
Tclin
酪氨酸蛋白激酶 BTK(Tyrosine-protein kinase BTK)
(1 活性数据)
AURKA
Tchem
极光激酶A(Aurora kinase A)
(1 活性数据)
ACVR1
Tchem
激活素受体 1 型(Activin receptor type-1)
(2 活性数据)
TNK2
Tclin
激活 CDC42 激酶 1(Activated CDC42 kinase 1)
(2 活性数据)
ABL1
Tclin
酪氨酸蛋白激酶ABL1(Tyrosine-protein kinase ABL1)
(3 活性数据)
ALK
Tclin
ALK 酪氨酸激酶受体(ALK tyrosine kinase receptor)
(8 活性数据)
CHEK2
Tchem
丝氨酸/苏氨酸蛋白激酶 Chk2(Serine/threonine-protein kinase Chk2)
(1 活性数据)
TIE1
Tchem
酪氨酸蛋白激酶受体 Tie-1(Tyrosine-protein kinase receptor Tie-1)
(1 活性数据)
CLK1
Tchem
双特异性蛋白激酶 CLK1(Dual specificity protein kinase CLK1)
(1 活性数据)
CLK2
Tchem
双特异性蛋白激酶 CLK2(Dual specificity protein kinase CLK2)
(1 活性数据)
CLK4
Tchem
双特异性蛋白激酶 CLK4(Dual specificity protein kinase CLK4)
(1 活性数据)
KIT
Tclin
肥大细胞/干细胞生长因子受体试剂盒(Mast/stem cell growth factor receptor Kit)
(1 活性数据)
INSR
Tclin
胰岛素受体(Insulin receptor)
(3 活性数据)
NUAK2
Tchem
NUAK 家族 SNF1 类激酶 2(NUAK family SNF1-like kinase 2)
(1 活性数据)
NUAK1
Tchem
NUAK 家族 SNF1 类激酶 1(NUAK family SNF1-like kinase 1)
(1 活性数据)
CAMK2D
Tchem
钙/钙调蛋白依赖性蛋白激酶 II 型亚基 delta(Calcium/calmodulin-dependent protein kinase type II subunit delta)
(1 活性数据)
JAK2
Tclin
酪氨酸蛋白激酶JAK2(Tyrosine-protein kinase JAK2)
(1 活性数据)
RPS6KA3
Tchem
核糖体蛋白 S6 激酶 α-3(Ribosomal protein S6 kinase alpha-3)
(2 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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