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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
52 Results for "
EGFR inhibition
" in MedChemExpress (MCE) Product Catalog:
Products (52)
52 Results for "EGFR inhibition" in MCE Product Catalog:
2
2 Cited Publications
Synonyms: EKI-785; WAY-EKI 785
Research Areas:
CL-387785 (EKI-785; WAY-EKI 785) is an orally active EGFR inhibitor with an IC50 of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC50 of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease .
2
2 Cited Publications
Synonyms: EGFR mutant-IN-3
Target:
Research Areas:
NT-1 (EGFR mutant-IN-3) is a potent mutant EGFR inhibitor and an analog of Osimertinib (HY-15772). This mutant EGFR inhibitor suppresses FGFR WT with an IC50 of 0.4 nM. NT-1 also inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M. NT-1 exerts deeper inhibition on p-EGFR and p-ERK, and induces tumor cell apoptosis. NT-1 can be used in colorectal cancer research .
2
2 Cited Publications
Target:
Research Areas:
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2
2 Cited Publications
Target:
Research Areas:
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
1
Cat. No.: HY-172429
CAS No.: 2489185-38-6
Synonyms: ORIC-114
Target:
Research Areas:
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
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Acid-PEG3-C2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs for the degradation of EGFR and inhibition of mTOR .
Cat. No.: HY-172429A
Synonyms: ORIC-114 hemihydrate
Target:
Research Areas:
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research .
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors .
Cat. No.: HY-117852
CAS No.: 173458-56-5
Synonyms: TRX-13
Target:
Research Areas:
CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (IC50=0.027 μM). CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers .
Cat. No.: HY-129510
CAS No.: 1346601-52-2
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
Cat. No.: HY-112806
CAS No.: 2247025-63-2
Research Areas:
ST8155AA1 is a part of antibody agent conjugates (ADCs) charged with HDAC inhibitor. ST8155AA1 induces α-tubulin, histone H3/H4 acetylation via direct enzymatic inhibition. ST8155AA1 recognizes and binds EGFR, undergoes internalization into EGFR-expressing tumor cells. ST8155AA1 inhibits cancer cell proliferation and exerts activity in mouse tumor models. ST8155AA1 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-178955
EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
Cat. No.: HY-174231
EGFR-IN-163 (Compound 13) is a competitive epidermal growth factor receptor (EGFR) inhibitor (IC50=0.079 μM, selective for HER-2 inhibition). EGFR-IN-163 induces tumor cell apoptosis and cell cycle arrest at G₂/M phase. EGFR-IN-163 is promising for research of estrogen receptor-positive (ER+) breast cancer .
Cat. No.: HY-178942
CAS No.: 3123724-88-6
EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). EGFR/VEGFR2-IN-9 significantly inhibits the proliferation of multiple cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 upregulates the expression levels of Bax, caspase-3, and p53, while downregulating the expression of Bcl-2. EGFR/VEGFR2-IN-9 induces apoptosis and arrests the cell cycle in the G1 phase. EGFR/VEGFR2-IN-9 can be used to investigate anti-tumor angiogenesis and multi-drug resistant cancers .
Cat. No.: HY-150552
CAS No.: 2366264-18-6
Target:
Research Areas:
JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor with IC50 values of >100, >100, 0.25 µM for JNK1, JNK2, JNK3, respectively. JNK3 inhibitor-2 shows DDR1 and EGFR (T790M, L858R) inhibition .
Cat. No.: HY-131710
CAS No.: 2538149-57-2
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PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity .
Cat. No.: HY-147802
CAS No.: 2529891-44-7
EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer .
Cat. No.: HY-128633
CAS No.: 2269470-35-9
PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research .
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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
