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ASK120067

Cat. No. M13437
ASK120067  Structure
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

ASK120067 is the third generation EGFR-TKI for non-small cell lung cancer (NSCLC) studies and is an effective oral EGFRT790M inhibitor (IC50 = 0.3 nM) with EGFRWT selectivity (IC50 = 6.0 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 546.07
Formula C29H32ClN7O2
CAS Number 1934259-00-3
Purity >98%
Solubility DMSO : 41.67 mg/mL
Storage at -20°C
References

[1] Yuankai Shi, et al. J Thorac Oncol. Efficacy and Safety of Limertinib (ASK120067) in Patients With Locally Advanced or Metastatic EGFR Thr790Met-Mutated NSCLC: A Multicenter, Single-Arm, Phase 2b Study

[2] Xinge Cui, et al. J Chromatogr B Analyt Technol Biomed Life Sci. Development of an LC-MS/MS method for quantifying ASK120067, a novel mutant-selective inhibitor of the epidermal growth factor receptor (EGFR) as well as its main metabolite in human plasma and its application in a pharmacokinetic study

[3] Tao Zhang, et al. Mol Cancer. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance

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Keywords: ASK120067 supplier, EGFR/HER2, inhibitors

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