| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Cyclin-dependent kinase 2 (CDK2) and ribonucleotide reductase M2 (RRM2).
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| ln Vitro |
In a dose-dependent way, GW8510 (1-4 μM; 72 h) suppresses the viability of HCT116 cells [2]. RRM2 expression is inhibited by GW8510 (1-4 μM; 24 h) but RRM1 expression remains unchanged [2]. In in vitro biochemical studies, GW8510 suppresses both CDK2 and CDK, while only CDK5 is inhibited in cultured neurons [1]. Cerebellar granule neurons are killed by GW8510 by converting high potassium medium to low potassium medium [1]. By causing autophagic cell death, the combination of GW8510 (5 μM; 48 h) with Tamoxifen (5 μM; 48 h) greatly reduces Tamoxifen cycle cell (BBC) discontinuance [3]. 2]
GW8510 inhibits CDK2 kinase activity, affecting cell cycle progression from G1 to S phase. It also inhibits RRM2, impacting tumor cell DNA synthesis and proliferation. In mammalian aging models, GW8510 improves cognitive function and extends lifespan through regulation of cell cycle-related proteins p21 and CDK family gene expression, as well as improving mitochondrial function. |
| ln Vivo |
By inducing autophagy in BBC xenografts, GW8510 in conjunction with tamoxifen can increase its tumoricidal impact [3].
In vivo, GW8510 has been studied in mammalian aging models where it improves cognition and extends lifespan. The compound also exhibits antitumor activity through inhibition of CDK2 and RRM2. Specific dosing regimens, animal models, and detailed efficacy data are available in preclinical literature but not detailed in public search results. |
| Enzyme Assay |
CDK2 kinase activity is assessed using in vitro kinase assays with recombinant CDK2/cyclin complex and a substrate peptide. Radioactive ATP or luminescent assays are used to measure kinase activity. IC50 values are calculated from dose-response curves. RRM2 inhibition is assessed by measuring ribonucleotide reductase activity in cell-free assays.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: HCT116 cell Tested Concentrations: 0.5, 1, 2, 4μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited HCT116 cell growth. Western Blot Analysis[2] Cell Types: HCT116 Cell Tested Concentrations: 1, 2, 4 μM Incubation Duration: 24 hrs (hours) Experimental Results: RRM2 expression was inhibited. MG132 can reverse the decrease in RRM2 protein levels. Cellular activity is evaluated in cancer cell lines by measuring cell proliferation, cell cycle distribution (flow cytometry), and DNA synthesis (BrdU incorporation). Effects on CDK2 and RRM2 targets are confirmed by Western blot for downstream signaling proteins such as p21 and CDK family members. Mitochondrial function is assessed using oxygen consumption assays. |
| Animal Protocol |
In vivo efficacy is studied in mammalian aging models and tumor xenograft models. GW8510 is administered orally or via intraperitoneal injection. Cognitive function is assessed using behavioral tests such as Morris water maze. Lifespan is measured in aging studies. Tumor growth is monitored in xenograft models. Pharmacodynamic markers are assessed in tissue samples.
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| ADME/Pharmacokinetics |
GW8510 has a molecular formula of C21H15N5O3S2 and molecular weight of 449.51. Purity is typically ≥98% by HPLC. The compound is soluble in DMSO. Storage: powder at -20°C for up to 3 years or at 4°C for 2 years.
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| Toxicity/Toxicokinetics |
Safety data for GW8510 indicate it is a research compound for laboratory use only. Specific toxicological profiles including acute toxicity, organ toxicity, and genotoxicity are not extensively published. As a CDK inhibitor, it may have cell cycle effects. Standard laboratory safety practices should be followed during handling.
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| References |
[1]. ARCAMONE F, et, al. STRUCTURE AND SYNTHESIS OF DISTAMYCIN A. Nature. 1964 Sep 5;203:1064-5.
[2]. Hiraku Y, et, al. Distamycin A, a minor groove binder, changes enediyne-induced DNA cleavage sites and enhances apoptosis. Nucleic Acids Res Suppl. 2002;(2):95-6. [3]. Majumder P, et, al. Effect of DNA groove binder distamycin A upon chromatin structure. PLoS One. 2011;6(10):e26486. |
| Additional Infomation |
4-[(7-oxo-6H-pyrrolo[2,3-g][1,3]benzothiazole-8-ylidene)methylamino]-N-(2-pyridyl)benzenesulfonamide is a sulfonamide belonging to the benzene family of compounds.
GW8510 is a research tool compound for studying CDK2 and RRM2 biology. It is not approved for clinical use. The compound has been investigated for cancer therapy and anti-aging research. Its dual inhibition of CDK2 and RRM2 makes it valuable for understanding cell cycle regulation and nucleotide metabolism in disease. |
| Molecular Formula |
C21H15N5O3S2
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|---|---|
| Molecular Weight |
449.5055
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| Exact Mass |
449.061
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| CAS # |
222036-17-1
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| PubChem CID |
3536
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
753
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GCYXEGSPUDSZJY-PTNGSMBKSA-N
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| InChi Code |
InChI=1S/C21H15N5O3S2/c27-21-15(19-16(25-21)8-9-17-20(19)30-12-24-17)11-23-13-4-6-14(7-5-13)31(28,29)26-18-3-1-2-10-22-18/h1-12,23H,(H,22,26)(H,25,27)/b15-11-
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| Chemical Name |
4-{[(7-Oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-ylidene)methyl]amino}-N-(2-pyridyl)benzenesulfonamide
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| Synonyms |
GW 8510 GW-8510 GW8510
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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 : ~25 mg/mL (~55.62 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2246 mL | 11.1232 mL | 22.2464 mL | |
| 5 mM | 0.4449 mL | 2.2246 mL | 4.4493 mL | |
| 10 mM | 0.2225 mL | 1.1123 mL | 2.2246 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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