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HUHS015

Cat. No. M9246
HUHS015 Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 100  USD100 In stock
50mg USD 290  USD290 In stock
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Quality Control & Documentation
Biological Activity

HUHS015 is a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo. The bioavailability (BA) of HUHS015 was 7.2% in rats after oral administration. As expected, continuously administering HUHS015 significantly suppressed the growth of DU145 cells, which are human hormone-independent prostate cancer cells, in a mouse xenograft model without untoward effects.

Chemical Information
Molecular Weight 318.37
Formula C19H18N4O
CAS Number 1453097-13-6
Solubility (25°C) DMSO: ≥ 25 mg/mL
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] Nakao S, et al. Bioorg Med Chem Lett. Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer dru gs.

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  Catalog
Abmole Inhibitor Catalog




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