AZD-9291 mesylate

For research use only. Not for therapeutic Use.

  • CAT Number: I001623
  • CAS Number: 1421373-66-1
  • Molecular Formula: C₂₉H₃₇N₇O₅S
  • Molecular Weight: 595.71
  • Purity: ≥95%
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AZD-9291 mesylate (CAT: I001623) is a potent and selective inhibitor of mutated forms of the epidermal growth factor receptor (EGFR). Specifically, it targets EGFR mutations such as T790M, which is associated with resistance to traditional EGFR inhibitors. AZD-9291 mesylate acts by irreversibly binding to the mutant EGFR, inhibiting its tyrosine kinase activity and preventing downstream signaling pathways involved in tumor growth and survival. This targeted therapy has shown promising results in the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations, offering a potential treatment option for patients with resistance to standard EGFR inhibitors.


Catalog Number I001623
CAS Number 1421373-66-1
Synonyms

(Z)-N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylimidic acid compound with methanesulfonic acid (1:1)

Molecular Formula C₂₉H₃₇N₇O₅S
Purity ≥95%
Target EGFR
Solubility 10 mM in DMSO
Storage Store at -20°C
Related CAS 1421373-65-0(free base)    
IC50 12.92 nM(Exon 19 deletion EGFR); 11.44 nM(L858R/T790M EGFR)
InChI InChI=1S/C28H33N7O2.CH4O3S/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24;1-5(2,3)4/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32);1H3,(H,2,3,4)
InChIKey FUKSNUHSJBTCFJ-UHFFFAOYSA-N
SMILES CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC.CS(=O)(=O)O
Reference

1: Stinchcombe TE. AZD9291 in epidermal growth factor receptor
inhibitor-resistant non-small-cell lung cancer. Transl Lung Cancer Res. 2016
Feb;5(1):92-4. doi: 10.3978/j.issn.2218-6751.2015.07.19. PubMed PMID: 26958499;
PubMed Central PMCID: PMC4758967. <br />
2: Gautschi O, Aebi S, Heukamp LC. Successful AZD9291 Therapy Based on
Circulating T790M. J Thorac Oncol. 2015 Dec;10(12):e122-3. doi:
10.1097/JTO.0000000000000676. PubMed PMID: 26709490. <br />
3: Remon J, Planchard D. AZD9291 in EGFR-mutant advanced non-small-cell lung
cancer patients. Future Oncol. 2015 Nov;11(22):3069-81. doi: 10.2217/fon.15.250.
Epub 2015 Oct 9. Review. PubMed PMID: 26450446. <br />
4: J&#228;nne PA, Yang JC, Kim DW, Planchard D, Ohe Y, Ramalingam SS, Ahn MJ, Kim SW,
Su WC, Horn L, Haggstrom D, Felip E, Kim JH, Frewer P, Cantarini M, Brown KH,
Dickinson PA, Ghiorghiu S, Ranson M. AZD9291 in EGFR inhibitor-resistant
non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1689-99. doi:
10.1056/NEJMoa1411817. PubMed PMID: 25923549.

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