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Purity: ≥98%
GSK621 is a novel, potent and selective activator of AMP-activated protein kinase (AMPK) with potential antitumor activity. It spares healthy hematopoietic progenitors while selectively killing acute myeloid leukemia (AML) cells. Both in vitro and in vivo tests revealed strong antiproliferative activity and high antitumor efficacy.
| Targets |
AMPK
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|---|---|
| ln Vitro |
GSK621 significantly increases AMPKα T172 phosphorylation, a sign of AMPK activation, in both AML cell lines and primary AML samples. GSK621 inhibits the proliferation of all 20 cell lines in the study, with IC50 values ranging from 13 to 30 μM, and increases apoptosis in 17 (85%) of the lines. Additionally, GSK621 activates autophagy, which also plays a role in AML cell death.[1]
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| ln Vivo |
GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly increases survival in nude mice with MOLM-14 xenografts by increasing AMPK activity and inducing apoptosis.[1]
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| Enzyme Assay |
HEPG2 cells are exposed to increasing doses of A-769662 or GSK621, and the phosphorylation of ACC S79 is measured using a commercial ELISA kit as a stand-in for the activation of AMPK.
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| Cell Assay |
Twenty AML cell lines are subjected to log10 dilutions of GSK621, and CellTiter-Glo?assay is used to assess relative viability. Using the Prism software, the IC50 of GSK621 for each of these 20 cell lines is calculated and shown as log[C], where [C] is expressed in mol/l (M). Five different cell lines are represented in the results for each panel.
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| Animal Protocol |
NUDE Mice bearing MOLM-14 Xenografts
30 mg/kg, twice daily i.p. |
| References |
| Molecular Formula |
C26H20N3O5CL
|
|---|---|
| Molecular Weight |
489.907
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| Exact Mass |
489.109
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| Elemental Analysis |
2934.99.9001
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| CAS # |
1346607-05-3
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| Related CAS # |
1346607-05-3
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| PubChem CID |
54577153
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.674
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| LogP |
4.04
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
778
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1C=CC=C(N2C(=O)NC3=C(N(C(=C3)Cl)C3=CC=C(C4=CC=CC(OC)=C4O)C=C3)C2=O)C=1
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| InChi Key |
KURYSXLJGKKDHT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H20ClN3O5/c1-34-18-6-3-5-17(13-18)30-25(32)23-20(28-26(30)33)14-22(27)29(23)16-11-9-15(10-12-16)19-7-4-8-21(35-2)24(19)31/h3-14,31H,1-2H3,(H,28,33)
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| Chemical Name |
6-chloro-5-[4-(2-hydroxy-3-methoxyphenyl)phenyl]-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4-dione
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| Synonyms |
GSK-621; GSK621; GSK 621
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~97 mg/mL (~198.0 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (2.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL Solubility in Formulation 5: 10 mg/mL (20.41 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0412 mL | 10.2060 mL | 20.4119 mL | |
| 5 mM | 0.4082 mL | 2.0412 mL | 4.0824 mL | |
| 10 mM | 0.2041 mL | 1.0206 mL | 2.0412 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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