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PJ34 hydrochloride

Cat. No. M2056
PJ34 hydrochloride Structure
Synonym:

PJ34 hcl

Size Price Availability Quantity
5mg USD 35  USD35 In stock
10mg USD 58  USD58 In stock
25mg USD 100  USD100 In stock
50mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

PJ34 hydrochloride is a potent, selective PARP-1 inhibitor. PJ34 displays activity at Pim-1 and Pim-2 kinases at higher concentrations (IC50 values are 3.7 and 16 μM respectively). PJ34 significantly suppresses HepG2 cell growth in a dose-dependent manner, and inhibits HepG2 cell-derived tumor growth in nude mice.

Chemical Information
Molecular Weight 331.8
Formula C17H17N3O2.HCl
CAS Number 344458-15-7
Solubility (25°C) DMSO 56 mg/mL
Water 56 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] Antolín AA, et al. ACS Chem Biol. Identification of pim kinases as novel targets for PJ34 with confounding effects in PARP biology.

[2] Huang SH, et al. Oncol Rep. PJ34, an inhibitor of PARP-1, suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells.

[3] Abdelkarim GE, et al. Int J Mol Med. Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke.

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