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Cat. No. M13437
ASK120067  Structure
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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).

Chemical Information
Molecular Weight 546.07
Formula C29H32ClN7O2
CAS Number 1934259-00-3
Solubility (25°C) DMSO : 41.67 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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.


[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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Abmole Inhibitor Catalog

Keywords: ASK120067 supplier, EGFR/HER2, inhibitors, activators

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