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Results for "

H1975 xenograft model

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109061B
    Lazertinib mesylate
    1 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 EGFR Akt ERK Cancer
    Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor that can penetrate the blood-brain barrier. Lazertinib (mesylate) inhibits p-EGFR, p-AKT and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) has anti-tumor activity in the mouse H1975-luc BM xenograft model. Lazertinib (mesylate) can be used in the study of non-small cell lung cancer .
    Lazertinib mesylate
  • HY-151563A
    OTUB1/USP8-IN-1 TFA
    1 Publications Verification

    		 Deubiquitinase Cancer
    OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
    OTUB1/USP8-IN-1 TFA
  • HY-15772S
    Osimertinib-d6

    AZD-9291-d6; Mereletinib-d6

    		 EGFR Cancer
    Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
    Osimertinib-d6
  • HY-15772AR
    Osimertinib mesylate (Standard)

    AZD-9291 mesylate (Standard); Mereletinib mesylate (Standard)

    		 Reference Standards EGFR Cancer
    Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
    Osimertinib mesylate (Standard)
  • HY-15772R
    Osimertinib (Standard)

    AZD-9291 (Standard); Mereletinib (Standard)

    		 Reference Standards EGFR Cancer
    Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
    Osimertinib (Standard)
  • HY-123891
    NS-062

    		EGFR Cancer
    NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .
    NS-062
  • HY-156457
    EGFR-IN-90

    		EGFR Cancer
    EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
    EGFR-IN-90
  • HY-170968
    EGFR-IN-150

    		EGFR Apoptosis Cancer
    EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
    EGFR-IN-150
  • HY-164392
    TAS-121

    		EGFR Apoptosis Cancer
    TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .
    TAS-121
  • HY-163396
    EGFR-IN-107

    		EGFR Apoptosis Cancer
    EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
    EGFR-IN-107
  • HY-15772
    Osimertinib
    Maximum Cited Publications
    151 Publications Verification

    AZD-9291; Mereletinib

    		 EGFR Cancer
    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
    Osimertinib
  • HY-15772A
    Osimertinib mesylate
    Maximum Cited Publications
    151 Publications Verification

    AZD-9291 mesylate; Mereletinib mesylate

    		 EGFR Cancer
    Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
    Osimertinib mesylate
  • HY-157526
    EGFR-TK-IN-1

    		EGFR Apoptosis Cancer
    EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
    EGFR-TK-IN-1
  • HY-150774
    HDAC6/HSP90-IN-2

    		HDAC HSP Apoptosis Cancer
    HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
    HDAC6/HSP90-IN-2
  • HY-172795
    EGFR-IN-158

    		EGFR Apoptosis Cancer
    EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .
    EGFR-IN-158

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