SML2914
EMI1
≥98% (HPLC)
别名:
3-(1,3-benzoxazol-2-yl)-7-(diethylamino)-2H-chromen-2-one, 3-(2-Benzoxazolyl)-7-(diethylamino)coumarin, 3-(Benzoxazol-2-yl)-7-diethylamino-2H-benzopyran-2-one
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
N(CC)(CC)c1cc2[o][c](c(cc2cc1)c3nc4c([o]3)cccc4)=O
InChI
1S/C20H18N2O3/c1-3-22(4-2)14-10-9-13-11-15(20(23)25-18(13)12-14)19-21-16-7-5-6-8-17(16)24-19/h5-12H,3-4H2,1-2H3
InChI key
UJOQSHCJYVRZKJ-UHFFFAOYSA-N
生化/生理作用
EMI1 (ChemBridge 5213777) is a call penetrant and potent inhibitor of EGFR signaling in EGFR L858R/T790M/C797S and ex19del/T790M/C797S triple mutants associated with drug-resistant NSCLC. Additionally, EMI1 potently depolymerized interphase microtubules, disrupts spindle formation and induced mitotic block in PC9 EGFR ex19del/T790M/C797S cells. EMI1 exhibits potent anti-proliferative activity against various cancer cell lines.
call penetrant and potent inhibitor of EGFR signaling in EGFR L858R/T790M/C797S triple mutants associated with drug-resistant NSCLC
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Su-Nam Kim et al.
Biochemical pharmacology, 77(12), 1773-1779 (2009-05-12)
Microtubules are a proven target for anticancer drug development because they are critical for mitotic spindle formation and the separation of chromosomes at mitosis. We here report a novel synthetic microtubule inhibitor 7-diethylamino-3(2'-benzoxazolyl)-coumarin (DBC). DBC causes destabilization of microtubules, leading
Punit Saraon et al.
Nature chemical biology, 16(5), 577-586 (2020-02-26)
Receptor tyrosine kinases (RTKs) are transmembrane receptors of great clinical interest due to their role in disease. Historically, therapeutics targeting RTKs have been identified using in vitro kinase assays. Due to frequent development of drug resistance, however, there is a
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