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GW 583340 dihydrochloride

Potent dual EGFR/ErbB2 inhibitor; orally active CAS# 1173023-85-2

GW 583340 dihydrochloride

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Catalog No. BCC7300----Order now to get a substantial discount!

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Quality Control of GW 583340 dihydrochloride

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GW 583340 dihydrochloride

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Chemical Properties of GW 583340 dihydrochloride

Cas No. 1173023-85-2 SDF Download SDF
PubChem ID 16219404 Appearance Powder
Formula C28H27Cl3FN5O3S2 M.Wt 671.03
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO with gentle warming
Chemical Name N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[(2-methylsulfonylethylamino)methyl]-1,3-thiazol-4-yl]quinazolin-4-amine;dihydrochloride
SMILES CS(=O)(=O)CCNCC1=NC(=CS1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl.Cl.Cl
Standard InChIKey WIMITXDBYLKRKB-UHFFFAOYSA-N
Standard InChI InChI=1S/C28H25ClFN5O3S2.2ClH/c1-40(36,37)10-9-31-14-27-35-25(16-39-27)19-5-7-24-22(12-19)28(33-17-32-24)34-21-6-8-26(23(29)13-21)38-15-18-3-2-4-20(30)11-18;;/h2-8,11-13,16-17,31H,9-10,14-15H2,1H3,(H,32,33,34);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GW 583340 dihydrochloride

DescriptionPotent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 values are 0.01 and 0.014 μM respectively). Selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 values are 0.11 μM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μM for inhibition of non-tumor cell line HFF). Inhibits tumor growth in vivo by ~ 80% in a murine xenograft model following oral administration.

GW 583340 dihydrochloride Dilution Calculator

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Preparing Stock Solutions of GW 583340 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.4902 mL 7.4512 mL 14.9025 mL 29.8049 mL 37.2562 mL
5 mM 0.298 mL 1.4902 mL 2.9805 mL 5.961 mL 7.4512 mL
10 mM 0.149 mL 0.7451 mL 1.4902 mL 2.9805 mL 3.7256 mL
50 mM 0.0298 mL 0.149 mL 0.298 mL 0.5961 mL 0.7451 mL
100 mM 0.0149 mL 0.0745 mL 0.149 mL 0.298 mL 0.3726 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on GW 583340 dihydrochloride

Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines.[Pubmed:12639547]

Bioorg Med Chem Lett. 2003 Feb 24;13(4):637-40.

We have identified a novel class of 6-thiazolylquinazolines as potent and selective inhibitors of both ErbB-2 and EGFR tyrosine kinase activity, with IC(50) values in the nanomolar range. These compounds inhibited the growth of both EGFR (HN5) and ErbB-2 (BT474) over-expressing human tumor cell lines in vitro. Using xenograft models of the same cell lines, we found that the compounds given orally inhibited in vivo tumor growth significantly compared with control animals.

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