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Tesevatinib

Cat. No. M14143
Tesevatinib Structure
Synonym:

XL-647; EXEL-7647; KD-019

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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 491.39
Formula
CAS Number 781613-23-8
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

[1] Sani H Kizilbash, et al. In Vivo Efficacy of Tesevatinib in EGFR-Amplified Patient-Derived Xenograft Glioblastoma Models May Be Limited by Tissue Binding and Compensatory Signaling

[2] Eric J Rubin, et al. Audio Interview: Covid-19 in South Africa and a New SARS-CoV-2 Variant

[3] Anjay Rastogi, et al. Autosomal dominant polycystic kidney disease: updated perspectives

[4] William E Sweeney, et al. Tesevatinib ameliorates progression of polycystic kidney disease in rodent models of autosomal recessive polycystic kidney disease

[5] Lin Tao, et al. Co-targeting cancer drug escape pathways confers clinical advantage for multi-target anticancer drugs

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Keywords: Tesevatinib, XL-647; EXEL-7647; KD-019 supplier, EGFR/HER2, inhibitors

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