Dasatinib Monohydrate
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.
Dasatinib Monohydrate对Src和Bcr-Abl酪氨酸激酶的IC50值分别为0.55 nM和3.0 nM.
慢性粒细胞白血病(CML)以费城(Ph+)染色体及其致癌产物BCR-ABL(存在于> 90%的患者中)的存在为特征.Dasatinib(BMS-354825)是一种新型的\有效的以及多靶点的激酶抑制剂,靶向作用于ABL\SRC\KIT\PDGFR以及其它酪氨酸激酶.
体外:生化实验表明,在血液与实体瘤细胞系中,Dasatinib是一种有效的ATP竞争性抑制剂,具有广谱的抗增殖活性.Dasatinib较Imatinib更有效地抑制无突变BCR-ABL激酶的活性.此外,在临床相关的15种耐Imatinib BCR-ABL亚型中,Dasatinib有效地抑制其中14种的激酶活性[1].
体内:通过灌胃方式给予小鼠Dasatinib或赋形剂,持续2周,从注射Ba/F3细胞后的第3天开始.所有经赋形剂处理的小鼠逐渐发病.相比之下,携带非突变型BCR-ABL或耐Imatinib的突变型M351T(临床常见)小鼠经Dasatinib处理后,显得健康,没有出现体重减轻\嗜睡或皱皮.此外,于治疗2周后,上述小鼠的生物发光活性降低了1个log以上的水平[2].
临床试验:在Imatinib失效或不耐受的Ph阳性白血病成年患者中,进行Dasatinib临床评估.试验表明,Dasatinib对慢性期\加速期以及急变期的CML有效.于2006年,Dasatinib获FDA批准用于治疗3个时期的慢性粒细胞白血病以及Ph阳性白血病[2].
参考文献：
[1] Shah NP, Tran C, Lee FY, Chen P, Norris D, Sawyers CL. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science. 2004 Jul 16;305(5682):399-401.
[2] Monika Conchon, Carla Maria Boquimpani de Moura Freitas, Maria Aparecida do Carmo Rego, and José Wilson Ramos Braga Junior. Dasatinib - clinical trials and management of adverse events in imatinib resistant/intolerant chronic myeloid leukemia Rev Bras Hematol Hemoter. 2011; 33(2): 131–139.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 506.02 |
| Cas No. | 863127-77-9 |
| Formula | C22H28ClN7O3S |
| Solubility | ≥25.3 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | (Z)-N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carbimidic acid hydrate |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(/N=C(O)/C(S2)=CN=C2NC3=CC(N4CCN(CCO)CC4)=NC(C)=N3)C(Cl)=CC=C1.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
