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XRP44X

Cat. No. M7496
XRP44X Structure
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Biological Activity

XRP44X is a ras-Net (Elk-3) pathway inhibitor (IC50 = 10 - 20 nM). Indirectly inhibits Net phosphorylation upstream of Erk1/2 activation. Mediates G2-M cell cycle arrest, suppresses growth of multiple cell types (IC50 ~ 2 nM), inhibits angiogenesis and acts as a microtubule depolymerizing agent in vitro.

Chemical Information
Molecular Weight 380.87
Formula C21H21ClN4O
CAS Number 729605-21-4
Solubility (25°C) DMSO 38.09 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] Bonanno, et al. Eur J Pharmacol. GABAB receptors as potential targets for drugs able to prevent excessive excitatory amino acid transmission in the spinal cord.

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