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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
28 Results for "
EGFR (L858R/T790M/C797S mutant)
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "EGFR (L858R/T790M/C797S mutant)" in MCE Product Catalog:
Cat. No.: HY-135805
CAS No.: 2060610-53-7
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
TQB-3804 is a potent, selective and orally active EGFR kinase inhibitor. TQB-3804 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. TQB-3804 can be used for the research of various cancers .
Cat. No.: HY-161536
CAS No.: 2992670-33-2
Research Areas:
PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)) .
Cat. No.: HY-175252
PROTAC EGFR degrader 14 is a EGFR PROTAC degrader, with a DC50 of 2.9 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 forms a stable ternary complex by bridging the ATP-binding pocket of the target protein EGFR with VHL E3 ubiquitin ligase, induces efficient and specific degradation of EGFR mutants via the ubiquitin-proteasome system, and ultimately induces cell cycle arrest and apoptosis. PROTAC EGFR degrader 14 can be used in studies related to non-small cell lung cancer carrying the EGFR C797S drug-resistant mutation .
Cat. No.: HY-139997
CAS No.: 2140806-84-2
DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .
Cat. No.: HY-147183A
Purity: 99.64%
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
Cat. No.: HY-147183B
Purity: 99.37%
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
Cat. No.: HY-147183
CAS No.: 2820336-67-0
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
Cat. No.: HY-178057
CAS No.: 2754394-10-8
Research Areas:
EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .
Cat. No.: HY-138746
CAS No.: 2573869-16-4
EGFR-IN-15 is an EGFR inhibitor with an IC50 of 4 nM. EGFR-IN-15 exhibits an IC50 of 16 nM against Osimertinib (HY-15772)-resistant mutant EGFR such as L858R/T790M/C797S. EGFR-IN-15 can be used for research on oncological diseases .
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
Cat. No.: HY-174826
EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFR L858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research .
Cat. No.: HY-175864
EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
Cat. No.: HY-170497
EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .
EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
Cat. No.: HY-130608
CAS No.: 2375107-27-8
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively .
Cat. No.: HY-139884
CAS No.: 2765573-34-8
EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
Cat. No.: HY-164490
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
Cat. No.: HY-161785
CAS No.: 3035639-05-2
EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
