HMPL-309

Name	(3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide
Synonyms	HMPL309 HMPL 309 HMPL-309 EOS-61583 Theliatinib Theliatinib (HMPL-309) ThTheliatinib (HMPL-309) (3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide
CAS	1353644-70-8

Molecular Formula	C25H26N6O2
Molar Mass	442.51
Storage Condition	2-8℃
In vitro study	Compared with erlotinib or gefitnib,theliatinib has a stronger binding affinity with wild-type EGFR and is more difficult to be replaced by ATP, which makes theliatinib have a better target binding effect, stronger antitumor activity in tumors with wild-type EGFR activation. In A431 cells, theliatinib inhibited phosphorylation of EGFR with an IC50 of 0.007 μm; In tumor cells A431, H292, FaDu cells with wild-type EGFR, it inhibited cell survival.
In vivo study	In several patient-derived esophageal cancer xenograft models, Theliatinib has concentration-dependent antitumor activity. However, abnormal activation or gene mutation of other targets such as PI3K and FGFR can weaken the anti-tumor activity of EGFR inhibitors, especially theliatinib.

biological activity	thelitinib (HMPL-309) is a highly potent EGFR inhibitor with a Ki value of 0.05 nM for EGFR, the IC50 values for EGFR and EGFR T790M/L858R mutant were 3 nM and 22 nM, respectively. It is 50 times more selective for EGFR than the other 72 kinases.
Target	Value
WT EGFR (Cell-free assay)	3 nM
EGFR T790M/L858R (Cell-free assay)	22 nM

Last Update：2024-04-09 19:05:18