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EGFR inhibition

" in MedChemExpress (MCE) Product Catalog:

28

Inhibitors & Agonists

3

Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147826
    EGFR-IN-60

    		EGFR Apoptosis Cancer
    EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
    EGFR-IN-60
  • HY-162881
    DS06652923

    		EGFR Cancer
    DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
    DS06652923
  • HY-171252
    EGFR-IN-145

    		EGFR Cancer
    EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase .
    EGFR-IN-145
  • HY-169568
    EGFR-IN-147

    		EGFR Cancer
    EGFR-IN-147 (compound ID-5841161) is a potent inhibitor of EGFR, with the inhibition rate of 14% at 1 μM. EGFR-IN-147 has the potential for the research of cancer .
    EGFR-IN-147
  • HY-145823
    EGFR-IN-42

    		EGFR Cancer
    EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity .
    EGFR-IN-42
  • HY-145824
    EGFR-IN-43

    		EGFR Cancer
    EGFR-IN-43 (Compound 17c) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity .
    EGFR-IN-43
  • HY-147967
    EGFR-IN-63

    		EGFR Cancer
    EGFR-IN-63 is an EGFR inhibition (IC50: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC50: 2.49 μM).
    EGFR-IN-63
  • HY-142512
    EGFR-IN-24

    		EGFR Cancer
    EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively .
    EGFR-IN-24
  • HY-160682
    EGFR/HER2-IN-12

    		EGFR Others
    EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
    EGFR/HER2-IN-12
  • HY-151158
    EGFR/HER2-IN-7

    		EGFR Cancer
    EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
    EGFR/HER2-IN-7
  • HY-129510
    4-Methyl erlotinib

    		EGFR Cancer
    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 .
    4-Methyl erlotinib
  • HY-158178
    EGFR T790M/L858R-IN-7

    		EGFR Cancer
    EGFR T790M/L858R-IN-7 (Compound 72) is a novel pyrimidine compound that inhibits the EGFR T790M and L858R mutation with a high efficacy (93% inhibition rate at 0.05 μM). EGFR T790M/L858R-IN-7 functions by specifically binding to the kinase domain of EGFR, thereby inhibiting its phosphorylation activity .
    EGFR T790M/L858R-IN-7
  • HY-158176
    EGFR T790M/L858R-IN-5

    		EGFR Cancer
    EGFR T790M/L858R-IN-5 (example 52) is a potent inhibitor of EGFR T790M/L858R with the inhibition percentage of 92.9% in the concerntration of 0.05 μM .
    EGFR T790M/L858R-IN-5
  • HY-158177
    EGFR T790M/L858R-IN-6

    		EGFR Cancer
    EGFR T790M/L858R-IN-6 (compound 53), a pyrimidine compound, is a potent EGFR T790M/L858R inhibitor. EGFR T790M/L858R-IN-6 shows 90.88% enzyme activity inhibition with 0.05 μM .
    EGFR T790M/L858R-IN-6
  • HY-112293
    GW2974

    		EGFR Cancer
    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 .
    GW2974
  • HY-129510R
    4-Methyl erlotinib (Standard)

    		EGFR Cancer
    4-Methyl erlotinib (Standard) is the analytical standard of 4-Methyl erlotinib. This product is intended for research and analytical applications. 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 .
    4-Methyl erlotinib (Standard)
  • HY-130549
    Acid-PEG3-C2-Boc

    		PROTAC Linkers Cancer
    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 .
    Acid-PEG3-C2-Boc
  • HY-147862
    EGFR-IN-62

    		EGFR Apoptosis Cancer
    EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
    EGFR-IN-62
  • HY-164413
    CLM3

    		VEGFR EGFR RET Apoptosis Cancer
    CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
    CLM3
  • HY-150552
    JNK3 inhibitor-2

    		JNK Discoidin Domain Receptor Inflammation/Immunology Cancer
    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 .
    JNK3 inhibitor-2
  • HY-164702
    BL-B01D1

    		Antibody-Drug Conjugates (ADCs) EGFR Cancer
    BL-B01D1 is a bispecific ADC, which targets EGFR and HER3 through bispecific antibody Izalontamab (HY-P99676), and exhibits cytotoxicity against various cancer cells via inhibition of DNA replication and DNA synthesis by its ADC toxin ED04 (HY-153891) .
    BL-B01D1
  • HY-111553
    TAS0728

    		EGFR Cancer
    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 .
    TAS0728
  • HY-131710
    PDE5-IN-3

    		Phosphodiesterase (PDE) EGFR Wnt Apoptosis Cancer
    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 .
    PDE5-IN-3
  • HY-18957C
    Lifirafenib hydrochloride

    BGB-283 hydrochloride

    		 Endogenous Metabolite Cancer
    Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
    Lifirafenib hydrochloride
  • HY-146325
    HSP90-IN-11

    		HSP Cancer
    HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
    HSP90-IN-11
  • HY-135699
    TD52
    1 Publications Verification

    		 Apoptosis Phosphatase Akt Cancer
    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.
    TD52
  • HY-135699A
    TD52 dihydrochloride
    1 Publications Verification

    		 Akt Phosphatase Apoptosis Cancer
    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.
    TD52 dihydrochloride
  • HY-147802
    EGFR-IN-59

    		EGFR Apoptosis Cancer
    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 .
    EGFR-IN-59

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