HPB is a cell-permeable, non-cytotoxic N-hydroxybenzamide derivative that acts as a HDAC6-selective deacetylase inhibitor (IC50 = 31/376/677/842/1133 nM against HDAC6/8/10/1/7, >2 μM against HDAC2/3/4/11/9/5). HPB treatment results in reduced growth, but not viability (up to 64 μM and 72 hrs), of LNCaP prostate cancer cells and non-cancer human foreskin fibroblasts (IC50 = 8 and 16-32 μM, respectively), causing upregulated acetylation levels of alpha-tubulin and peroxiredoxin, but not histones, both in cultures and in mice in vivo. Intraperitoneal injection is efficacious in suppressing the expansion of prostate cancer CWR22 xenograft-derived tumors in mice (by 73% in 4 wks; Five daily 300 mg/kg i.p. dosings a week) without detectable weight loss.
| Molecular Weight | 328.36 |
| Formula | C18H20N2O4 |
| CAS Number | 1800066-24-3 |
| Solubility (25°C) | DMSO: 5 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[1] No authors listed. HPB Surg. HPB News
[2] Martin de Santibaes, et al. Combined liver and multivisceral resections
[3] M P Senthil Kumar, et al. Klatskin-like lesions
[4] A N Kingsnorth. Major HPB procedures must be undertaken in high volume quaternary centres?
[5] G Gozzetti, et al. HPB surgery: an independent speciality or a branch of digestive surgery?
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