egfr in 8

EGFR-IN-8, a dual inhibitor targeting both EGFR and c-Met, shows potential as a promising candidate for further development in treating EGFR TKI-resistant NSCLC.

EGFR HER2-IN-8 (compound 34) is an inhibitor of EGFR, HER2, and DHFR with IC50 values of 0.45 μM, 0.244 μM, and 5.669 μM, respectively. It demonstrates anticancer activity against several cancer cell lines, exhibiting a high safety profile and selectivity indices, making it useful for cancer research [1].

Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) is a potent GTPase inhibitor that inhibits EGFR kinase with an IC50 of 560 μM.Tyrphostin 8 inhibits protein serine threonine calmodulin phosphatases (IC50=21 μM), enhances transferrin receptor-mediated transcytosis in Caco-2 cells, and increases the hypoglycemic effect of oral insulin-transferrin. hypoglycemic effect.

EGFR-IN-50 is a potent EGFR inhibitor targeting L858R resistance mutations, acting on TEL-EGFR-L858R-BaF3 and TEL-EGFR-T790M-L858R-BaF3 with GI50 values of 8 nM and 6.03 μM, respectively. EGFR-IN-50 exhibits anti-proliferative effects on cancer cells. .

PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells, and inhibits the growth of cell lines H1975, PC-9, and HCC827 with IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is used primarily for cancer research, particularly in the context of non-small cell lung cancer (NSCLC) [1].

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

Petosemtamab (FUT8-KO) is a variant of Petosemtamab with the fucosyltransferase 8 gene (FUT8) knocked out. Petosemtamab is a monoclonal antibody (mAb) targeting EGFR (with a Kd of 0.22 nM) and LGR5 (with a Kd of 0.86 nM). This antibody disrupts EGFR signaling and causes receptor degradation in LGR5+ cancer cells. It is applicable in research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

Anticanceragent 231 (compound P5) is a tyrosine kinase inhibitor with an IC50 value of 3.95 μM. It targets the EGFR-ERK1 2 signaling pathway, reducing cell viability, proliferation, migration, and cancer stemness in triple-negative breast cancer (TNBC) cells, potentially playing a significant role in the treatment of TNBC.

EGFR-IN-134 (compound 3f) is a triazolo[3,4-a]quinoline derivative and functions as a potent EGFR inhibitor with an IC50 of 0.023 µM. It induces apoptosis and necrosis in cells, and causes cell cycle arrest in the G2 M and pre-G1 phases. EGFR-IN-134 modulates the expression of apoptosis-regulating proteins by downregulating anti-apoptotic protein Bcl2 and upregulating pro-apoptotic proteins p53, Bax, and caspases 3, 8, and 9, demonstrating significant antiproliferative and anticancer activities.

HER2-IN-13 (Compound 33) is an effective HER2 inhibitor with an IC50 value of 8 nM and also inhibits wt-EGFR with an IC50 of 0.40 μM [1].

EGFR-IN-23, identified as compound 8 in WO2021244502A1, is a potent EGFR tyrosine kinase inhibitor (TKI) demonstrating an inhibitory concentration (IC50) of 8.05 nM against the BaF3 EGFR-DEL19 T790M C797S cell line.

BMX-IN-1 (BMX kinase inhibitor) is a selective inhibitor of bone marrow tyrosine kinase on chromosome X (BMX, IC50 = 8 nM) and the related Bruton's tyrosine kinase (BTK, IC50 = 10.4 nM), but BMX-IN-1 is more than 47-656 fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

EGFRT790M L858R-IN-9 (Compound 8) is an inhibitor targeting the EGFR-L858R T790M mutations. It effectively inhibits the phosphorylation of the EGFR-L858R T790M mutant kinase, demonstrating an IC50 value of 0.0064 µM. Additionally, EGFRT790M L858R-IN-9 can suppress the proliferation of non-small cell lung cancer (NSCLC) cells, making it useful for cancer research.

PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR, ErbB2, ErbB3, and ErbB4 (IC50s: 8μM, 49 nM, 52 nM, and 52 nM in cell assay).