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RTS-V5

Cat. No. M10883
RTS-V5  Structure
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Biological Activity

RTS-V5 is an inhibitor of HDAC/proteasomes, against HDAC1, HDAC2, HDAC3, HDAC6, HDAC8IC50They were 6.9, 18, 15, 0.27, 0.53 μM, respectively.

Chemical Information
Molecular Weight 525.61
Formula C27H35N5O6
CAS Number 2285346-31-6
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] Kazuki Okubo, et al. Anticancer Res. The Dual Histone Deacetylase-Proteasome Inhibitor RTS-V5 Acts Synergistically With Ritonavir to Induce Endoplasmic Reticulum Stress in Bladder Cancer Cells

[2] Kazuki Okubo, et al. Anticancer Res. Ubiquitin-proteasome System Is a Promising Target for Killing Cisplatin-resistant Bladder Cancer Cells

[3] Sanil Bhatia, et al. J Med Chem. Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor

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