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Selatinib 

Cat. No. M28106
Selatinib  Structure
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Quality Control & Documentation
Biological Activity

Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.

Chemical Information
Molecular Weight 565.06
Formula C29H26ClFN4O3S
CAS Number 1275595-86-2
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light
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] Meng-Na Wang, et al. Invest New Drugs. First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects

[2] Jin-fang Jiang, et al. Yao Xue Xue Bao. [Metabolic research of domestically developed small molecule tyrosine kinase inhibitors]

[3] Long Zhang, et al. Eur J Med Chem. Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer

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  Catalog
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Keywords: Selatinib  supplier, EGFR/HER2, inhibitors, activators


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