產(chǎn)品屬性:
產(chǎn)品名稱
規(guī)格
CAS號(hào)
型號(hào)
EGFR-IN-11
10mM*1 mL in DMSO 5 mg 10 mg 25 mg 50 mg 100 mg
2463200-44-2
EY-Y0165574
Cas No.2463200-44-2
別名 N/A
化學(xué)名 N/A
分子式 C29H35N9O2S
分子量 573.71
溶解度 DMSO : 125 mg/mL (217.88 mM; Need ultrasonic)
儲(chǔ)存條件 Store at -20°C General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. Shipping Condition Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request 產(chǎn)品描述: EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1[1].
EGFR-IN-11 (Compound D9; 0.0001-10 μM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 μM, respectively[1]. EGFR-IN-11 (0.01-1.00 μM for HCC827 cells; 0.1-10.00 μM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line[1]. EGFR-IN-11 (1 μM; 24 h) potently induces the apoptosis of HCC827 cells.[1]EGFR-IN-11 (1 μM; 24 h) induces cell cycle arrests in HCC827 cell[1].
[1]. Lei H, et al. Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors. Eur J Med Chem. 2019 Nov 16:111888.
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