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Dasatinib Monohydrate

カタログ番号GC15884

ダサチニブ (BMS-354825) 一水和物は、強力な抗腫瘍活性を有する、非常に強力な ATP 競合性経口活性デュアル Src/Bcr-Abl 阻害剤です。 Kis は、Src と Bcr-Abl でそれぞれ 16 pM と 30 pM です。ダサチニブ一水和物は、Bcr-Abl および Src をそれぞれ <1.0 nM および 0.5 nM の IC50 で阻害します。ダサチニブ一水和物は、アポトーシスとオートファジーも誘導します。

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Dasatinib Monohydrate 化学構造

Cas No.: 863127-77-9

サイズ 価格 在庫数 個数
100mg
$38.00
在庫あり
500mg
$65.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 863127-77-9 SDF
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
Canonical SMILES CC1=C(/N=C(O)/C(S2)=CN=C2NC3=CC(N4CCN(CCO)CC4)=NC(C)=N3)C(Cl)=CC=C1.O
Formula C22H28ClN7O3S M.Wt 506.02
溶解度 ≥ 25.3mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9762 mL 9.881 mL 19.7621 mL
5 mM 0.3952 mL 1.9762 mL 3.9524 mL
10 mM 0.1976 mL 0.9881 mL 1.9762 mL
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レビュー

Review for Dasatinib Monohydrate

Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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