TargetMol

Mavelertinib

Product Code:
 
TAR-T21322
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T21322-25mg25mg£656.00
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Further Information

Bioactivity:
Mavelertinib is an orally available inhibitor of the EGFR mutant form T790M, a secondarily acquired resistance mutation. Mavelertinib specifically binds to and inhibits EGFR T790M, which prevents EGFR-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells.
CAS:
1776112-90-3
Formula:
C18H22FN9O2
Molecular Weight:
415.433
Purity:
0.98
SMILES:
COc1nn(C)cc1Nc1nc(nc2n(C)cnc12)N1C[C@@H](F)[C@@H](C1)NC(=O)C=C

References

1. Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S, Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM, Edwards MP, Ferre RA, Gajiwala KS, Hemkens MD, Kania RS, Kath JC, Matthews J, Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin S, Zhang C, Lafontaine JA. Discovery of N-((3R,4R)-4-fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H- purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) Through Structure-Based Drug Design; A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants With Selectivity Over Wild-Type EGFR. J Med Chem. 2017 Mar 13. doi: 10.1021/acs.jmedchem.6b01894. [Epub ahead of print] PubMed PMID: 28287730. 2. Wang S, Cang S, Liu D. Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016 Apr 12;9:34. doi: 10.1186/s13045-016-0268-z. Review. PubMed PMID: 27071706; PubMed Central PMCID: PMC4830020.