Dasatinib Monohydrate

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

863127-77-9

包装与价格：

包装	价格(元)
100mg	电议
500mg	电议

产品介绍

Dasatinib (BMS-354825) 一水合物是一种高效的、ATP 竞争性的、具有口服活性的双重 Src/Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。 Src 和 Bcr-Abl 的 Kis 分别为 16 pM 和 30 pM。 Dasatinib monohydrate 抑制 Bcr-Abl 和 Src，IC50 分别为<1.0 nM 和 0.5 nM。达沙替尼一水合物还诱导细胞凋亡和自噬。

Cas No.	863127-77-9
别名	达沙替尼一水合物,BMS-354825 monohydrate
化学名	(Z)-N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carbimidic acid hydrate
Canonical SMILES	CC1=C(/N=C(O)/C(S2)=CN=C2NC3=CC(N4CCN(CCO)CC4)=NC(C)=N3)C(Cl)=CC=C1.O
分子式	C₂₂H₂₈ClN₇O₃S
分子量	506.02
溶解度	≥ 25.3mg/mL in DMSO
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Description: IC50: 0.55 and 3.0 nM for Src and Bcr-Abl tyrosine kinases, respectively Chronic Myeloid Leukemia (CML) is a disease characterized by the presence of the Philadelphia (Ph+) chromosome and its oncogenic product, BCR-ABL, that is present in >90% of the patients. Dasatinib (BMS-354825) is a novel, potent, and multitargeted kinase inhibitor that targets ABL, SRC, KIT, PDGFR, and other tyrosine kinases. In vitro: Dasatinib is a potent ATP-competitive inhibitor in biochemical assays with broad-spectrum antiproliferative activities against hematological and solid tumor cell lines. Dasatinib was more potent than imatinib at inhibiting nonmutated BCR-ABL kinase activity. In addition, the kinase activity of 14 out of 15 different clinically relevant, imatinib-resistant BCR-ABL isoforms was successfully inhibited [1]. In vivo: Mice were dosed with Dasatinib or vehicle alone by gavage for 2 weeks, beginning 3 days after injection of Ba/F3 cells. All vehicle-treated mice developed progressive disease. In contrast, Dasatinib–treated mice harboring nonmutant BCR-ABL or the clinically common imatinib-resistant mutation M351T appeared healthy with no evidence of weight loss, lethargy, or ruffled fur and showed more than one log lower levels of bioluminescent activity after 2 weeks of therapy [2]. Clinical trial: Dasatinib has been evaluated in clinical trials in adult patients with Ph-positive leukemias after imatinib failure or intolerance when it was proven to be effective in the chronic, accelerated and blast phases of CML. It was approved by FDA in 2006 for the treatment of CML in the three phases and also for Ph-positive ALL [2]. Reference: [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.