GZD824
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.
GZD824是一种Bcr-Abl的口服生物活性抑制剂, 对Bcr-AblWT和Bcr-AblT315I的IC50值分别为0.34 nM和0.68 nM[1].
Bcr-Abl是与白细胞介素-3受体β(c)亚基相互作用的融合蛋白,具有酪氨酸激酶活性.Abl激活细胞周期相关的蛋白和酶,并增加细胞分裂.Bcr-Abl抑制DNA修复,并导致基因组不稳定.
GZD824是一种具有口服生物利用度的Bcr-Abl抑制剂.GZD824对Bcr-AblWT和Bcr-AblT315I显示出高亲和性,Kd值分别为0.32 nM和0.71 nM.GZD824抑制Bcr-Abl活性,对 Bcr-AblWT\Bcr-AblT315I\Bcr-AblE255K\Bcr-AblG250E\Bcr-AblQ252H\Bcr-AblH396P\Bcr-AblM351T和Bcr-AblY253F的IC50值分别为:0.34\0.68\0.27\0.71\0.15\0.35\0.29和0.35 nM.在竞争性结合试验中,GZD824与天然Abl的ATP结合位点结合,对非磷酸化和磷酸化Abl的Kd值分别为0.32和0.34 nM.在稳定转化的Ba/F3细胞中,GZD824有效抑制表达Bcr-AblWT和Bcr-AblT315I1的细胞的生长,IC50值分别为1.0 nM和7.1 nM[1].
在小鼠异种移植肿瘤模型中,GZD824抑制肿瘤的生长.在小鼠异体移植白血病模型中,GZD824显著增加生存率[1].
参考文献：
Ren X, Pan X, Zhang Z, et al. Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem, 2013, 56(3): 879-894.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 724.77 |
| Cas No. | 1421783-64-3 |
| Formula | C29H27F3N6O·2CH4O3S |
| Solubility | ≥36.25 mg/mL in DMSO; ≥33.95 mg/mL in H2O with ultrasonic; ≥4.71 mg/mL in EtOH with ultrasonic |
| Chemical Name | 3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide dimethanesulfonate |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=C(C(NC2=CC=C(CN3CCN(C)CC3)C(C(F)(F)F)=C2)=O)C=C1C#CC4=CN=C5C(C=NN5)=C4.CS(=O)(O)=O.CS(=O)(O)=O |
| 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
- 批次:
化学结构
