G-749
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.
G-749是Fms样酪氨酸受体激酶3(FLT3)的选择性抑制剂,对野生型FLT3的IC50值为0.4 nM。
G-749是一种合成的、高效的和ATP竞争性的野生型FLT3抑制剂。G-749抑制FLT3的自磷酸化,在RS4-11白血病细胞中的IC50值≤ 8 nM。G-749还对各种FLT3突变体具有抑制活性。在稳定表达FLT3-ITD/N676D、FLT3-ITD/F691L,FLT3-D835Y或FLT3-D835Y/N676DBaF3的细胞系中,G-749有效抑制所测试FLT3突变体的自磷酸化,其IC50值小于10 nM。在嗜FLT3-ITD的MV4-11和MOLM-14细胞系中,G-749显著抑制细胞增殖,增加活性caspase 3/7的水平,以及呈剂量依赖性地切割PARP。此外,即使处于高浓度的FLT3配体环境中,G-749可以有效抑制p-FLT3、p-ERK1/2和p-AKT。
参考文献:
1. Lee H K, Kim H W, Lee I Y, et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood, 2014, 123(14): 2209-2219.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 521.41 |
Cas No. | 1457983-28-6 |
Formula | C25H25BrN6O2 |
Solubility | ≥26.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1NC=C(Br)C2=C1C(NC3=CC=C(OC4=CC=CC=C4)C=C3)=NC(NC5CCN(C)CC5)=N2 |
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。 |
质量控制和MSDS
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