egfr-in-9

EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor 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.

EGFR-IN-91 (compound 9) is an orally active EGFR inhibitor capable of crossing the blood-brain barrier. It effectively inhibits EGFRL858R/C797S and EGFRexon 19del/C797S, leading to tumor regression in patient-derived xenograft (PDX) mouse models. EGFR-IN-91 shows potential for inhibiting locally advanced and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutations.

EGFR/HER2-IN-9, a compound inhibiting both EGFR and HER2, demonstrates potency with IC50 values of 3.2 nM for EGFR, 14 nM for HER2, and 8.3 nM against the EGFR T790M mutation.

EGFR-IN-95 is a derivative of 2,4-diaminonicotinamide. It effectively inhibits the activity of EGFRdel19/T790M/C797S and L858R/T790M/C797S.

EGFR-IN-94 (compound 5a) is an EGFR inhibitor with an IC50 of 0.086 μM. It exhibits IC50 values of 0.107 μM for VEGFR-2 and 2.52 μM for Topo II. In HepG-2 cells, EGFR-IN-94 induces apoptosis and causes cell cycle arrest at the S phase.

EGFR-IN-92 (compound 15) is an allosteric inhibitor targeting both T790M and L858R double-mutated EGFR. It exhibits antiproliferative activity against H1975 non-small cell lung cancer (NSCLC) cells expressing these double mutations.

EGFR-IN-93 (compound 18) is an allosteric inhibitor of the T790M/L858R double mutant EGFR. It is applicable for research in non-small cell lung cancer (NSCLC).

EGFR-IN-96 (compound 7a) is a thiophene[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. It causes HepG2 cells to arrest in the S and G2/M phases and inhibits the growth of cancer cells with wild-type EGFR and EGFRT790M.

EGFR-IN-98 (Compound 4c) is an EGFR inhibitor, exhibiting IC50 values of 0.277 μM for L858R/T790M/C797S and 0.089 μM for Del19/T790M/C797S enzymes. It is applicable in tumor research.

EGFR-IN-99 (JBJ-03-142-02) is an EGFR and HER2 Exon 20 insertion mutation inhibitor with antiproliferative activity for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-90 (compound 34), an orally active EGFR inhibitor, demonstrates potent activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and effectively inhibits the proliferation of the H1975-TM cell line carrying EGFRL858R/T790M/C797S mutations with an IC50 of 0.05 μM. Additionally, EGFR-IN-90 suppresses tumor growth in the H1975-TM xenograft tumor model [1].

EGFR-IN-97 (compound 6q), an EGFR inhibitor, demonstrates effectiveness in inhibiting Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, exhibiting IC 50 values of 0.42 μM and 0.41 μM, respectively. Additionally, at a concentration of 0.8 μM, EGFR-IN-97 is capable of inducing apoptosis in NCI-H1975-EGFR L858R/T790M/C797S cells [1].

EGFR/VEGFR2-IN-3 (compound 9) is an effective inhibitor of EGFR and VEGFR-2, demonstrating IC50 values of 0.129 µM for EGFR, 0.142 µM for VEGFR-2, and 3.428 µM for COX-2. This compound exhibits cytotoxic properties and induces cell apoptosis (apoptosis) as well as cell cycle arrest at the G2/M phase.

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.

SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for prostate cancer, effectively suppressing downstream effector molecules through the inhibition of SOS1 and EGFR. It induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. In prostate cancer cells PC-3, it demonstrates significant antitumor activity with an IC50 of 0.45±0.03 μM.

Lenalidomide-C6-Br is a conjugate of an E3 ligase ligand and a linker. It is utilized in the synthesis of PROTAC EGFR degrader 9.

7-Bromoheptanoyl chloride is the link (ligand) in the formation of PROTACEGFR degrader 9.

7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.

Ensartinib (X-396) is a potent and orally active dual ALK/MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

Canertinib (CI-1033) is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.

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

ProMMP-9 inhibitor-3c is a potent and specific proMMP-9 inhibitor which disrupts f MMP-9 homodimerization and prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR.

EGFR-IN-25, an efficacious EGFR inhibitor, demonstrates IC50 values of 9 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and 60 nM for A431 cells (WT), respectively.