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TAS6417

Cat. No. M9534
TAS6417 Structure
Synonym:

TAS-6417

Size Price Availability Quantity
5mg USD 450  USD450 In stock
10mg USD 750  USD750 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

TAS6417 is a novel EGFR inhibitor targeting exon 20 insertion mutations, with IC50 values range from 1.1-8.0 nM. TAS6417 inhibited EGFR phosphorylation and downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions, resulting in caspase activation. TAS6417 suppresses the growth of cells expressing exon 20 insertion mutations of the EGFR gene, with a GI50 value of 86.5±28.5 nM for LXF 2478L cells and 45.4±2.6 nM for NCI-H1975 EGFR D770_N771insSVD cells. TAS6417 also potently inhibits proliferation in other cell lines harboring activating mutations or acquired resistance mutations, with mean GI50 values of 1.92±0.21 nM to 7.12±0.60 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 396.44
Formula C23H20N6O
CAS Number 1661854-97-2
Purity >98.5%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Shinichi Hasako, et al. Mol Cancer Ther. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations.

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