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Famitinib malate

Cat. No. M28063
Famitinib malate Structure
Synonym:

SHR1020 malate

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Quality Control & Documentation
Biological Activity

Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer.

Chemical Information
Molecular Weight 544.57
Formula C27H33FN4O7
CAS Number 1256377-67-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Xiaoran Zhang, et al. Clin Pharmacol Drug Dev. Effect of Dietary Intake on the Pharmacokinetics of the Multitargeted Receptor Tyrosine Kinase Inhibitor Famitinib: Results From a Phase 1 Study in Healthy Chinese Participants

[2] Federica Grillo, et al. Endocr Relat Cancer. Emerging multitarget tyrosine kinase inhibitors in the treatment of neuroendocrine neoplasms

[3] Aiping Zhou, et al. Cancer Chemother Pharmacol. Phase I study of the safety, pharmacokinetics and antitumor activity of famitinib

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Keywords: Famitinib malate, SHR1020 malate supplier, VEGFR/PDGFR, inhibitors, activators


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