| Identification | Back Directory | [Name]
9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- | [CAS]
2463200-44-2 | [Synonyms]
EGFR-IN-11
9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl- | [Molecular Formula]
C29H35N9O2S | [MOL File]
2463200-44-2.mol | [Molecular Weight]
573.71 |
| Chemical Properties | Back Directory | [Boiling point ]
808.3±75.0 °C(Predicted) | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (217.88 mM; Need ultrasonic) | [form ]
Solid | [pka]
7.88±0.42(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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]. | [IC 50]
EGFRL858R/T790M/C797S: 18 nM (IC50) | [References]
[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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