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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-EMI1
EMI1

Chemical Structure : EMI1

CAS No.: 35773-42-3

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EMI1 (EGFR MaMTH Inhibitor 1, EMI-1, ChemBridge 5213777)

货号: PC-72416Not For Human Use, Lab Use Only.

EMI1 (EGFR MaMTH Inhibitor 1, ChemBridge 5213777) is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S activating mutant inhibitor, inhibits viability of PC9 EGFR ex19del/T790M/C797S with EC50 of 115 nM, potently reducing the interaction of EGFR triple mutant with Shc1 in MaMTH-DS assays.

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10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3480 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

EMI1 (EGFR MaMTH Inhibitor 1, ChemBridge 5213777) is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S activating mutant inhibitor, inhibits viability of PC9 EGFR ex19del/T790M/C797S with EC50 of 115 nM, potently reducing the interaction of EGFR triple mutant with Shc1 in MaMTH-DS assays.
EMI1 binds to Coatomer Protein Complex Beta 2 (COPB2) with KD of 3.98 uM.
EMI1 strongly inhibit the viability and increase the caspase 3/7 activity of PC9 EGFR ex19del/T790M/C797S triple mutant cells than non-cancerous human bronchial epithelial (HBE) cells.
EMI1 inhibited PC9 EGFR ex19del/T790M/C797S organoid growth with EC50 of 131 nM.
EMI1 exerts an inhibitory effect on the uptake and distribution of activated, mutant EGFR receptor in early endosomes.
EMI1 attenuates RTK expression and signalling and alters the electrophoretic mobility of Coatomer Protein Complex Beta 2 (COPB2) in lung cancer cells.

物理化学性质&存储条件

分子量 334.375
分子式 C20H18N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(Benzo[d]oxazol-2-yl)-7-(diethylamino)-2H-chromen-2-one

参考文献

1. Punit Saraon, et al. Nat Chem Biol. 2020 May;16(5):577-586.

2. Saraon P, et al. J Mol Biol. 2021 Nov 19;433(23):167294.

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