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Symadex

Cat. No. M8354
Symadex Structure
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Biological Activity

Symadex is an FMS-like tyrosine kinase 3 (FLT3) and topoisomerase-II inhibitor; ABCG2 substrate; cell cycle modulator.

Chemical Information
Molecular Weight 350.41
Formula C20H22N4O2
CAS Number 138154-39-9
Solubility (25°C) DMSO: 10 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] Tomasz Laskowski, et al. Intercalation complex of imidazoacridinone C-1311, a potential anticancer drug, with DNA helix d(CGATCG)2: stereostructural studies by 2D NMR spectroscopy

[2] N Isambert, et al. Evaluation of the safety of C-1311 (SYMADEX) administered in a phase 1 dose escalation trial as a weekly infusion for 3 consecutive weeks in patients with advanced solid tumours

[3] Eran E Bram, et al. Structural determinants of imidazoacridinones facilitating antitumor activity are crucial for substrate recognition by ABCG2

[4] N Alami, et al. Comparative cytotoxicity of C-1311 in colon cancer in vitro and in vivo using the hollow fiber assay

[5] Magdalena Hyzy, et al. Antitumour imidazoacridone C-1311 induces cell death by mitotic catastrophe in human colon carcinoma cells

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