Olmutinib (BI 1482694) is a novel EGFR mutation-specific tyrosine kinase inhibitor and Bruton's tyrosine kinase inhibitor.

 

Brand: BCM

 

Target: EGFR; BTK

 

Signaling Pathways: Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors

 

In Vitro: HM61713 causes potent inhibition in cell lines H1975 (L858R and T790M) and HCC827 (exon 19 deletion). It has a low potency for NSCLC cell line H358 harboring wild-type EGFR (GI50 of 2225 nM).

 

In Vivo: HM61713 has a half-life of over 24 h for EGFR inhibition. In the in vivo studies of xenograft models with grafts of H1975 and HCC827, HM61713 is active against the tumors without showing any side effects.

 

pKa: 12.87±0.70(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4  

 

InChIKey: FDMQDKQUTRLUBU-UHFFFAOYSA-N  

 

InChI: InChI=1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)

 

Attribute
[Chem Name]	N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]thieno[3,2-d]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
[Synonym]	Olmutinib;BI 1482694; HM61713
[CAS No.]	1353550-13-6
[MDL No.]	MFCD29918158
[Formula]	C26H26N6O2S
[Molecular]	486.59
[Form]	Solid Powder
[Storage]	Keep in dark place. Inert atmosphere, 2-8°C

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