egfrl858r/t790m/c797s

EGFR-IN-11 is a selective inhibitor of EGFR-tyrosine kinase and induces cell apoptosis. EGFR-IN-11 inhibits triple mutant EGFRL858R T790M C797S with an IC50 of 18 nM and arrests cell cycle at G0 G1.

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R T790M C797S and BaF3–C797S Del19 T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.

EGFR-IN-120 (Compound 11eg) is an orally effective EGFR inhibitor. It exhibits potency against the EGFR L858R T790M C797S mutant with an IC50 of 0.053 μM, and displays weaker activity against EGFRWT, with an IC50 of 1.05 μM. EGFR-IN-120 inhibits the phosphorylation of EGFR as well as key downstream effectors including STAT3, AKT, and Erk. This compound induces cell cycle arrest and apoptosis in cells harboring the EGFR mutation. Additionally, EGFR-IN-120 inhibits the proliferation of NSCLC cells containing the EGFR L858R T790M C797S mutation, with an IC50 value of 0.052 μM.

EGFR mutant-IN-2 (Compound D51) is an inhibitor of EGFR mutants, specifically targeting EGFR L858R T790M C797S and EGFR del19 T790M C797S mutants with IC50 values of 14 nM and 62 nM, respectively. This compound exhibits favorable pharmacokinetic (PK) parameters, safety properties, in vivo stability, and demonstrates antitumor activity [1].

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-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R T790M C797S and 0.06 nM for EGFR Del19 T790M C797S. It lacks significant inhibitory effects on EGFR WT. Demonstrating anti-proliferative properties, EGFR-IN-82 also inhibits tumor growth in nude mice, rendering it applicable in non-small cell lung cancer research [1].

EGFR-IN-22 is a highly effective inhibitor targeting wild type EGFR and its mutant form, EGFR L858R T790M C797S, displaying IC50 values of 4.91 nM and 0.54 nM, respectively.

EGFR-IN-126 (compound 9d) is an effective inhibitor of EGFR L858R T790M C797S, displaying an IC50 value of 0.005 μM. It exhibits antitumor activity both in vivo and in vitro.

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].

JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R T790M C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858

Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19 T790M C797S TK and 113 nM for EGFRL858R T790M C797S TK. It effectively suppresses EGFR phosphorylation, induces G1 phase arrest, and triggers apoptosis in KC-0116 (BaF3-EGFRDel19 T790M C797S) cells. Moreover, Os30 demonstrates strong antitumor activity in non-small cell lung cancer (NSCLC) harboring the EGFmRC797S mutation [1].

EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R T790M), and EGFR(L858R T790M C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.

JBJ-09-063 is a mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR), with potent inhibitory activity demonstrated by half-maximal inhibitory concentrations (IC50s) of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R T790M, 0.083 nM for EGFR L858R T790M C797S, and 0.396 nM for EGFR L747S. This compound effectively decreases phosphorylation of EGFR, Akt, and ERK1 2, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 holds potential for research into EGFR-mutant lung cancer.

EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R T790M C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect.

EGFR-IN-104 (Compound A23) acts as a potent EGFR inhibitor, demonstrating IC50 values of 0.33 μM for EGFR L858R T790M and 0.133 μM for EGFR Del19 T790M C797S. It exhibits anticancer properties, effective both in vitro and in vivo [1].

LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del T790M C797S and EGFRL858R T790M C797S, with IC50 values of 2.4 nmol L and 3.1 nmol L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del T790M C797S, and results in significant tumor reduction in a C797S mutant xenograft model.

EGFR-IN-101 (I-10), a 2-phenylamino pyrimidine derivative, is an EGFR inhibitor with IC50 values of 33.26 nM for EGFR L858R T790M C797S and 106.4 nM for Ba F3-EGFR L858R T790M C797S. It is applicable in the study of non-small cell lung cancer (NSCLC) [1].

JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R T790M C797S, EGFRWT and EGFRL858R T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.

EGFR-IN-47 is a potent, orally active inhibitor of EGFRL858R T790M C797S (IC50: 0.01 μM). EGFR-IN-47 is capable of blocking the cell cycle and inducing apoptosis. EGFR-IN-47 has potential for NSCLC studies.

EGFR-IN-69 is a potent inhibitor of the EGFR enzyme, demonstrating IC50 values of 4.3 nM for EGFR L858R T790M C797S, 6.6 nM for EGFR L858R T790M, and 25.6 nM for EGFR 19del T790M C797S. This compound is utilized in the research of non-small-cell lung cancer (NSCLC).

JBJ-09-063 hydrochloride is an EGFR inhibitor selective for mutants, demonstrating IC50 values of 0.147 nM, 0.063 nM, 0.083 nM, and 0.396 nM against EGFR L858R, EGFR L858R T790M, EGFR L858R T790M C797S, and EGFR L747S, respectively. It effectively inhibits EGFR, Akt, and ERK1 2 phosphorylation, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and -resistant models. This compound holds potential for research on EGFR-mutant lung cancer.

JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R T790M, 0.083 nM for EGFR L858R T790M C797S, and 0.396 nM for EGFR L747S mutations. It effectively reduces phosphorylation of EGFR, Akt, and ERK1 2, demonstrating efficacy in models both sensitive and resistant to EGFR tyrosine kinase inhibitors (TKI). JBJ-09-063 TFA holds potential for research in EGFR-mutant lung cancer [1].

EGFR-IN-140 (Compound 31) is an inhibitor of EGFR, effectively targeting both wild-type EGFR and the EGFRL858R T790M C797S mutant, with Ki values of 0.95 nM and 2.1 nM, respectively. Additionally, it inhibits EGFRdel19 T790M C797S in Ba F3 cells with an IC50 of 56.9 nM and demonstrates antitumor activity in mouse models.

LSD1 EGFR-IN-1 (compound L-1) is an effective inhibitor of LSD1, EGFRT790M L858R, and EGFRL858R T790M C797S, with IC50 values of 6.24, 2.06, and 5.01 μM, respectively. This compound plays a significant role in cancer research.