AMG319
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.
AMG 319是磷酸肌醇3-激酶p110δ亚型(PI3Kδ)的高选择性抑制剂[1],IC50值小于10 nM[2]。
PI3Kδ在B细胞受体(BCR)的信号传导中发挥重要作用。PI3Kδ在淋巴样恶性肿瘤中显现,包括慢性淋巴细胞白血病(CLL)和非霍奇金淋巴瘤(NHL)[1]。
C-Akt是一种丝氨酸-苏氨酸激酶,是PI39K的靶标。C-Akt蛋白是哺乳动物Akt亚型家族的原型成员。对Akt的调控可能是磷酸化或直接结合PI39K脂质的Akt pleckstrin同源结构域。不依赖于PI39K的Akt刺激已被确定[3]。AMG 319抑制淋巴瘤细胞中基础AKT磷酸化和增殖[1]。
28例患者接受了AMG 319治疗,在1剂量后的CLL患者中,25 mg的AMG 319引起了3级溶血性贫血。 所有CLL样品都伴有60%的诱导性信号,其展现了BCR诱导的pAKT(离体IgD的刺激)的剂量依赖性范围。当剂量在400 mg时,可观测到长达24小时的近完整抑制。CLL患者中T调节性细胞的基线百分比升高(14.4%±7.6%)。但在19例患者中的14例接受治疗过程中,T调节细胞的升高趋于正常化,这表明该药物可能会产生免疫修复。通过体检,所有20个被评估的患者都表现出大于50%的淋巴结(LN)减少,其中15个患者(75%)表现出大于90%的LN减少。此反应存在于所有的细胞遗传学亚型中[1]。
参考文献:
[1]. Glenn M, Mato AR, Allgood SD, et al. First-in-human study of AMG 319, a highly selective, small molecule inhibitor of PI3Kδ, in adult patients with relapsed or refractory lymphoid malignancies. Blood, 2013, 122(21): 678-678.
[2]. Brana I, Siu LL. Clinical development of phosphatidylinositol 3-kinase inhibitors for cancer treatment. BMC medicine, 2012, 10(1): 1.
[3]. Datta SR, Dudek H, Tao X, et al. Akt phosphorylation of BAD couples survival signals to the cell-intrinsic death machinery. Cell, 1997, 91(2): 231-241.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 385.4 |
Cas No. | 1608125-21-8 |
Formula | C21H16FN7 |
Solubility | Soluble in DMSO |
Chemical Name | (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine |
SDF | Download SDF |
Canonical SMILES | C[C@@](NC1=NC=NC2=C1N=CN2)([H])C(C=C3C=CC(F)=CC3=N4)=C4C5=CC=CC=N5 |
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。 |