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NSC745885

Cat. No. M11170
NSC745885 Structure
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Biological Activity

NSC745885 is a potent anti-tumor reagent that is selectively toxic to a variety of cancer cell lines but not to normal cells. NSC745885 is a potent downregulator of EZH2 through the proteasome degradation pathway. NSC745885 offers the possibility of research on advanced bladder cancer and oral squamous cell carcinoma.

Chemical Information
Molecular Weight 266.27
Formula C14H6N2O2S
CAS Number 4219-52-7
Solubility (25°C) DMSO Insoluble
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] Chia-Chi Kung, et al. Mol Biol Rep. Temporal expression patterns of distinct cytokines and M1/M2 macrophage polarization regulate rheumatoid arthritis progression

[2] Ahmed Atef Ahmed Ali, et al. PLoS One. Novel Anthra[1,2-c][1,2,5]Thiadiazole-6,11-Diones as Promising Anticancer Lead Compounds: Biological Evaluation, Characterization & Molecular Targets Determination

[3] Shou-Hung Tang, et al. Oncotarget. Pharmacologic down-regulation of EZH2 suppresses bladder cancer in vitro and in vivo

[4] Yuan-Wu Chen, et al. PLoS One. A novel compound NSC745885 exerts an anti-tumor effect on tongue cancer SAS cells in vitro and in vivo

[5] Yung-Lung Chang, et al. Int J Biochem Cell Biol. Different roles of p53 in the regulation of DNA damage caused by 1,2-heteroannelated anthraquinones and doxorubicin

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