1. Cell Cycle/DNA Damage
  2. CDK
  3. GW8510

GW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities.

For research use only. We do not sell to patients.

GW8510 Chemical Structure

GW8510 Chemical Structure

CAS No. : 222036-17-1

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Based on 1 publication(s) in Google Scholar

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Description

GW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities[1][2][3].

IC50 & Target[1][2]

CDK2

 

CDK5

 

RRM2

 

In Vitro

GW8510 (0.5-4 μM; 72 h) inhibits viability of HCT116 cells in a dose-dependent manner[2].
GW8510 (1-4 μM; 24 h) inhibits RRM2 expression without alteration of RRM1 expression[2].
GW8510 inhibits CDK2 and other CDKs when tested in in vitro biochemical assays, when used on cultured neurons it only inhibits CDK5[1].
GW8510 inhibits the death of cerebellar granule neurons caused by switching them from high potassium medium to low potassium medium[1].
Combination with GW8510 (5 μM; 48 h) and Tamoxifen (5 μM; 48 h) significantly inhibits survival of the Tamoxifen-resistant breast cancer cells (BBCs) through induction of autophagic cell death[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: HCT116 cells
Concentration: 0.5, 1, 2, 4 μM
Incubation Time: 72 hours
Result: Inhibited HCT116 cells growth.

Western Blot Analysis[2]

Cell Line: HCT116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 24 hours
Result: Inhibited RRM2 expression.
The reduction of RRM2 protein level can be reversed by MG132.
In Vivo

Combination with GW8510 and Tamoxifen enhances tumoricidal effect on Tamoxifen-resistant BBC xenograft through autophagy induction[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

449.51

Formula

C21H15N5O3S2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=CC=C(N/C=C(C2=C(SC=N3)C3=CC=C2N4)\C4=O)C=C1)(NC5=NC=CC=C5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2246 mL 11.1232 mL 22.2464 mL 55.6161 mL
5 mM 0.4449 mL 2.2246 mL 4.4493 mL 11.1232 mL
10 mM 0.2225 mL 1.1123 mL 2.2246 mL 5.5616 mL
15 mM 0.1483 mL 0.7415 mL 1.4831 mL 3.7077 mL
20 mM 0.1112 mL 0.5562 mL 1.1123 mL 2.7808 mL
25 mM 0.0890 mL 0.4449 mL 0.8899 mL 2.2246 mL
30 mM 0.0742 mL 0.3708 mL 0.7415 mL 1.8539 mL
40 mM 0.0556 mL 0.2781 mL 0.5562 mL 1.3904 mL
50 mM 0.0445 mL 0.2225 mL 0.4449 mL 1.1123 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GW8510
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