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EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.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.
Brand: BCM
Target: EGFRL858R/T790M/C797S:18 nM
In Vitro Activity: EGFR-IN-11 (1 μM; 24 h) potently induces the apoptosis of HCC827 cells. EGFR-IN-11 (1 μM; 24 h) induces cell cycle arrests in HCC827 cell.EGFR-IN-11 ( 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. 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.
Solubility: Soluble in DMSO : 125 mg/mL (217.88 mM; Need ultrasonic)
InChi Key: RNEHWYIFHKBZAW-XMMPIXPASA-N
Attribute [Chem Name] (R)-9-(1-(cyclopropylsulfonyl)pyrrolidin-3-yl)-N2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine [Synonym] EGFR-IN-11; RXN00442; RXN-00442; RXN 00442; [CAS No.] 2463200-44-2 [Formula] C29H35N9O2S [Molecular] 573.71 [Form] White to yellow solid
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