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SBI-0087702

Cat. No. M8425
SBI-0087702 Structure
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Biological Activity

SBI-0087702 promotes the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε.

Chemical Information
Molecular Weight 321.41
Formula C21H23NO2
CAS Number 864431-36-7
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
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] Nanako Kitanaka, et al. ERK1/ATF-2 signaling axis contributes to interleukin-1β-induced MMP-3 expression in dermal fibroblasts

[2] Tal Varsano, et al. Inhibition of melanoma growth by small molecules that promote the mitochondrial localization of ATF2

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