2699877-43-3
Chemical Structure
EGFR-IN-60
- CAS 番号: 2699877-43-3
- Formula:C28H28Cl2N6O
- Molecular Weight:535.47
IUPAC Name: (E)-5-(2,3-dichlorophenyl)-3-((4-(dimethylamino)benzylidene)amino)-4-imino-8,8-dimethyl-4,5,7,8,9,10-hexahydropyrimido[4,5-b]quinolin-6(3H)-one
InChIKey: HFGBVNJPTHYXRL-ZSBAPAOWSA-N
SMILES: O=C1C2=C(NC(N=CN(/N=C/C3=CC=C(N(C)C)C=C3)C4=N)=C4C2C5=CC=CC(Cl)=C5Cl)CC(C)(C)C1
Biological Activity: EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio[1].
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EGFR-IN-60 | EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio. | |||||||||||||||||||||
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