GW 610 (Synonyms: NSC 721648) |
Catalog No.GC10616 |
GW 610 (NSC 721648), un agente antitumoral, muestra una actividad anticancerÍgena potente y selectiva contra lÍneas celulares de cÁncer de pulmÓn, colon y mama.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 872726-44-8
Sample solution is provided at 25 µL, 10mM.
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 | |
Sinónimos | NSC 721648 | ||
Chemical Name | 2-(3,4-dimethoxyphenyl)-5-fluorobenzo[d]thiazole | ||
Canonical SMILES | FC1=CC2=C(SC(C3=CC=C(OC)C(OC)=C3)=N2)C=C1 | ||
Formula | C15H12FNO2S | M.Wt | 289.32 |
Solubility | DMF: 10 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 0.5 mg/ml | 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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
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