2730430-08-5
2730430-08-5
Chemical Structure
ALK/EGFR-IN-1
- CAS. Nr.: 2730430-08-5
- Formula:C27H34ClN7O3S
- Molecular Weight:572.12
InChIKey: AMMOSDRENOSFIO-UHFFFAOYSA-N
SMILES: O=S(CC)C1=C(NC2=NC(NC3=C(OC)C=C(N(CCN(C)C)C)C(NC(C=C)=O)=C3)=NC=C2Cl)C=CC=C1
Biological Activity: ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research[1].
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ALK/EGFR-IN-1 | ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research. | |||||||||||||||||||||
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ALK/EGFR-IN-1-d5 | ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment | |||||||||||||||||||||
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