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Befotertinib

Cat. No. M28940
Befotertinib Structure
Synonym:

D-0316

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Quality Control & Documentation
Biological Activity

Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).

Chemical Information
Molecular Weight 567.61
Formula C29H32F3N7O2
CAS Number 1835667-63-4
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic and warming and heat to 60°C)
Storage Powder -20°C
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] Shun Lu, et al. Lancet Respir Med. Befotertinib (D-0316) versus icotinib as first-line therapy for patients with EGFR-mutated locally advanced or metastatic non-small-cell lung cancer: a multicentre, open-label, randomised phase 3 study

[2] Jessica Menis, et al. Lancet Respir Med. Befotertinib-a viable alternative in EGFR-mutant advanced NSCLC?

[3] Hua Li, et al. J Chromatogr B Analyt Technol Biomed Life Sci. Simultaneous quantitation of befotertinib (D-0316) and its metabolite D-0865 in human plasma by LC-MS/MS method

[4] Sally C M Lau, et al. J Thorac Oncol. And Still They Come Over Troubled Waters: Can Asia's Third-Generation EGFR Tyrosine Kinase Inhibitors (Furmonertinib, Aumolertinib, Rezivertinib, Limertinib, Befotertinib, SH-1028, and Lazertinib) Affect Global Treatment of EGFR+ NSCLC

[5] Shun Lu, et al. J Thorac Oncol. Efficacy and Safety of Befotertinib (D-0316) in Patients With EGFR T790M-Mutated NSCLC That Had Progressed After Prior EGFR Tyrosine Kinase Inhibitor Therapy: A Phase 2, Multicenter, Single-Arm, Open-Label Study

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Keywords: Befotertinib, D-0316 supplier, EGFR/HER2, inhibitors, activators


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