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Olmutinib

Names

[ CAS No. ]:
1353550-13-6

[ Name ]:
Olmutinib

[Synonym ]:
N-{3-[(2-{[4-(4-Methyl-1-piperazinyl)phenyl]amino}thieno[3,2-d]pyrimidin-4-yl)oxy]phenyl}acrylamide
2-Propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]-
Olmutinib
N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino) thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide
HM71224

Biological Activity

[Description]:

Olmutinib (HM61713; BI-1482694) is an irreversible EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain.

[Related Catalog]:

Research Areas >> Cancer

[Target]

EGFRExon 19 deletion:9.2 nM (IC50, Cell Assay)

EGFRL858R/T790M:10 nM (IC50, Cell Assay)


[In Vitro]

Olmutinib potently inhibits EGFR in HCC827 cells expressing EGFRDEL19 (IC50=9.2 nM) and H1975 cells expressing EGFRL858R/T790M (IC50=10 nM). In contrast, the IC50 of olmutinib against cells expressing EGFRWT is 2225 nM[1].

[References]

[1]. Kim ES, et al. Olmutinib: First Global Approval. Drugs.?2016 Jul;76(11):1153-7.


[Related Small Molecules]

Osimertinib (AZD9291) | Tyrphostin B42 (AG-490) | Neratinib (HKI-272) | Genistein | (-)-Epigallocatechin gallate | AG-1478 | Dacomitinib (PF-00299804) | Irbinitinib | Poziotinib | Sapitinib | AZD-3759 | Pyrotinib | Canertinib dihydrochloride | BMS-690514 | Pelitinib

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C26H26N6O2S

[ Molecular Weight ]:
486.589

[ Exact Mass ]:
486.183807

[ PSA ]:
110.86000

[ LogP ]:
4.95

[ Index of Refraction ]:
1.706

[ Storage condition ]:
-20℃

Related Compounds