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AST 1306 tosylate

Axon 1986
  • Parent CAS:  897383-62-9
Purity:  98%
  • Soluble in DMSO
  • MF:  C24H18ClFN4O2.C7H8O3S
  • MW:  621.08

Description

AST 1306 tosylate is a selective, irreversible EGFR/ErbB2 (HER2) inhibitor with reported IC50 values of 0.5 nM for EGFR and 3.0 nM for ErbB2. It also inhibits ErbB4 and the EGFR T790M/L858R mutant in reported assays.

ErbB receptor signaling drives proliferation and survival in multiple epithelial cancers, and EGFR resistance mutations are important oncology targets. AST 1306 is useful for studying irreversible ErbB blockade, HER2-driven growth and EGFR mutant pharmacology.

Key Features

  • Irreversible EGFR/ErbB2 kinase inhibitor
  • Reported IC50: 0.5 nM (EGFR) and 3.0 nM (ErbB2)
  • Active against EGFR T790M/L858R in reported assays
  • More potent in ErbB2-overexpressing cellular models

Applications

  • EGFR and HER2 kinase assays
  • ErbB-driven cancer model research
  • Resistance mutation pharmacology
  • Irreversible kinase inhibitor profiling

More Information

Parent CAS No. 897383-62-9
Chemical Name N-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)acrylamide 4-methylbenzenesulfonate
SMILES C(NC1C=CC2C(C=1)=C(NC1=CC=C(OCC3=CC=CC(F)=C3)C(Cl)=C1)N=CN=2)(=O)C=C.C1C=C(S(O)(=O)=O)C=CC=1C
MFCD MFCD17169993
InChi InChI=1S/C24H18ClFN4O2.C7H8O3S/c1-2-23(31)29-17-6-8-21-19(11-17)24(28-14-27-21)30-18-7-9-22(20(25)12-18)32-13-15-4-3-5-16(26)10-15;1-6-2-4-7(5-3-6)11(8,9)10/h2-12,14H,1,13H2,(H,29,31)(H,27,28,30);2-5H,1H3,(H,8,9,10)
InChiKey ZMUKJEHWLJBODV-UHFFFAOYSA-N
CID 25027665
Short Description EGFR/Erb2 inhibitor

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