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GW8510

Cat. No. M7820
GW8510 Structure
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Biological Activity

GW8510 is an inhibitor of cyclin kinase 2 (CDK2). It prevents and/or reduces the side effects of chemotherapy (alopecia, plantar-palmar syndrome and mucositis).

Chemical Information
Molecular Weight 449.51
Formula C21H15N5O3S2
CAS Number 222036-17-1
Solubility (25°C) DMSO: soluble
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Duygu Genalp Rstem, et al. Synergistic Interactions between GW8510 and Gemcitabine in an In Vitro Model of Pancreatic Cancer

[2] Zhen-Nan Li, et al. Acquired tamoxifen resistance is surmounted by GW8510 through ribonucleotide reductase M2 downregulation-mediated autophagy induction

[3] Ping Chen, et al. Gemcitabine resistance mediated by ribonucleotide reductase M2 in lung squamous cell carcinoma is reversed by GW8510 through autophagy induction

[4] Nivanthika K Wimalasena, et al. Gene Expression-Based Screen for Parkinson's Disease Identifies GW8510 as a Neuroprotective Agent

[5] Dina Fomina-Yadlin, et al. GW8510 increases insulin expression in pancreatic alpha cells through activation of p53 transcriptional activity

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