NVP-TNKS656
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NVP-TNKS656是Wnt通路的口服活性拮抗剂。Wnt信号通路参与许多控制发育的过程,该通路的失调可导致癌变[1]。
体外实验:针对TNKS2、PARP1、PARP2和STF NVP-TNKS656的IC50值分别为0.006、>19、32、和0.0035 μM[1]。
在体实验:小鼠静脉内给药NVP-TNKS656后,NVP-TNKS656的清除率和容积分布分别为10 mL/min/kg和0.6 L/kg。暴露度和口服生物利用度分别为32%和53%。在小鼠乳腺肿瘤病毒(MMTV)-Wnt1转基因模型中,口服350 mg/kg 的NVP-TNKS656超过24小时后,会激活Wnt信号。NVP-TNKS656使肿瘤中Wnt/β-连环蛋白靶基因Axin2的mRNA水平减少70至80%[1]。
参考文献:
Shultz M D, Cheung A K, Kirby C A, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor[J]. Journal of medicinal chemistry, 2013, 56(16): 6495-6511.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 494.58 |
Cas No. | 1419949-20-4 |
Formula | C27H34N4O5 |
Solubility | Soluble in DMSO |
Chemical Name | N-(cyclopropylmethyl)-N-((4-hydroxy-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)methyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)acetamide |
SDF | Download SDF |
Canonical SMILES | COC1=CC=C(C(C2CCN(CC(N(CC3=NC4=C(C(O)=N3)COCC4)CC5CC5)=O)CC2)=O)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |