GW 610
(Synonyms: NSC 721648) 目录号 : GC10616An antitumor benzothiazole
Cas No.:872726-44-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GI50: < 0.1 nM for MCF-7 and MDA 468 cancer cell lines
GW 610 is a potent antiproliferative agent with tyrosine kinase inhibitory properties.
Tyrosine kinases are important mediators of the signaling cascade, having critical roles in various biological processes such as growth, differentiation, metabolism as well as apoptosis in response to both internal and external stimuli.
In vitro: GW 610 was evaluated in vitro in four human cancer cell lines, and GW 610 was observed to display potent antiproliferative activity exquisitely (GI50 < 0.1 nM for both MCF-7 and MDA 468). Moreover, selective and potent activity was observed in the NCI 60 human cancer cell line panel as well. Structure-activity relationships (SARs) indicated that GW 610 exhibited a pinnacle of potent activity, with most structural variations with a deactivating in-vitro effect. Mechanistically, this noval compound contrasting with the previously reported 2-(4-aminophenyl)benzothiazoles, GW 610 was not dependent on induction of CYP1A1 expression for antitumor activity. An additional observation was that CYP1A1 protein was also expressed in MCF-7 and MDA 468 cells exposed to GW 610’s inactive analogues [1].
In vivo: Currently, there is no animal in vivo data reported.
Clinical trial: Up to now, GW 610 is still in the preclinical development stage.
Reference:
[1] Mortimer CG,Wells G,Crochard JP,Stone EL,Bradshaw TD,Stevens MF,Westwell AD. Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines. J Med Chem.2006 Jan 12;49(1):179-85.
Cas No. | 872726-44-8 | SDF | |
别名 | NSC 721648 | ||
化学名 | 2-(3,4-dimethoxyphenyl)-5-fluorobenzo[d]thiazole | ||
Canonical SMILES | FC1=CC2=C(SC(C3=CC=C(OC)C(OC)=C3)=N2)C=C1 | ||
分子式 | C15H12FNO2S | 分子量 | 289.32 |
溶解度 | DMF: 10 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 0.5 mg/ml | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.4564 mL | 17.2819 mL | 34.5638 mL |
5 mM | 0.6913 mL | 3.4564 mL | 6.9128 mL |
10 mM | 0.3456 mL | 1.7282 mL | 3.4564 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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