AZD3229 Tosylate

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AZD3229 Tosylate  纯度: 98.54%

AZD3229 Tosylate 是一种有效的、广泛的突变型酪氨酸激酶受体 (KIT) 抑制剂,可用于开发研究胃肠道间质瘤。

AZD3229 Tosylate

AZD3229 Tosylate Chemical Structure

CAS No. : 2248003-71-4

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AZD3229 Tosylate 相关产品

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生物活性

AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

IC50 & Target

KIT[1].

体外研究
(In Vitro)

AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM). AZD3229 demonstrates potent single digit nM growth inhibition across a broad cell panel, with good margin to KDR-driven effects. Selectivity over KDR can be rationalised predominantly by the interaction of water molecules with the protein and ligand in the active site and its kinome selectivity is similar to the best of the approved GIST agents[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

651.71

Formula

C31H34FN7O6S

CAS 号

2248003-71-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (153.44 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5344 mL 7.6721 mL 15.3442 mL
5 mM 0.3069 mL 1.5344 mL 3.0688 mL
10 mM 0.1534 mL 0.7672 mL 1.5344 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Kettle JG, et al. Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Chem. 2018 Oct 11;61(19):8797-8810.

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