EMI1 (EGFR MaMTH Inhibitor 1)|ChemBridge 5213777|DC Chemicals

Cas No.:	35773-42-3
Synonyms:	EMI-1,EMI 1,ChemBridge-5213777,ChemBridge5213777,ChemBridge 5213777
SMILES:	CCN(CC)C1=CC2=C(C=C1)C=C(C(=O)O2)C3OC4=C(C=CC=C4)N=3
Formula:	C₂₀H₁₈N₂O₃
M.Wt:	334.36852
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor[1].
Target:	EGFRdel19 T790M C797S EGFRL858R/T790M/C797S
In Vitro:	EMI1 inhibits PC9 EGFR ex19del/T790M/C797S organoid growth with the EC50 of 131 nM[1]. EMI1 (1 nM-10 μM) potently reduces the interaction of EGFR triple mutant with Shc1[1]. EMI1 (1 nM-100μM) strongly inhibits the viability and increase the caspase 3/7 activity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells[1]. Cell Viability Assay[1] Cell Line: PC9 EGFR ex19del/T790M/C797S and HBE bronchial epithelial lung EGFR-WT control cells. Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Time: 72 hours Result: Strongly inhibited the viability.
References:	[1]. Punit Saraon, et al. A drug discovery platform to identify compounds that inhibit EGFR triple mutants. Nat Chem Biol. 2020 May;16(5):577-586

Cat. No.	Product name	Field of application
DC28032	EMI1 (EGFR MaMTH Inhibitor 1)	EMI1 (EGFR MaMTH Inhibitor 1) is a novel EGFR ex19del/T790M/C797S inhibitor.EMI1, while potently reducing the interaction of EGFR triple mutant with Shc1 in our MaMTH-DS assay, did not behave as a TKI and displayed no inhibition of the kinase activity of EGFR triple-mutant protein invitro.EMI1 did, however, more strongly inhibit the viability and increase the caspase 3/7 activ-ity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells, as well as potently reduce PC9 EGFR ex19del/T790M/C797S organ-oid viability.EMI1 had a similar inhibi-tory effect on microtubule plus-end growth in both EGFR-WT and EGFR-C797S triple-mutant cells at 50–100 nM concentration. At 1 µM concentration, EMI1 strongly depolymerized inter-phase microtubules, perturbed spindle formation and induced strong mitotic block in PC9 EGFR ex19del/T790M/C797S cells after 20 h of treatment. EMI1 inhibited interaction of both proteins with EGFR at a level similar to that observed with Shc1, indicating it is not a specific inhibitor of the EGFR-Shc1 PPI interface. Rather, the loss of interaction mediated by EMI1 appears to be due to a more general alteration in EGFR activity.EMI1 induced EGFR degradation, and inhibited the activation of EGFR, ERK, AKT and S6 in PC9-ex19del and PC9-ex19del/T790M cells.
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