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antitumor potency

" in MedChemExpress (MCE) Product Catalog:

19

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12202
    MEK inhibitor
    1 Publications Verification

    		 MEK Cancer
    MEK inhibitor is a potent MEK inhibitor with antitumor potency.
    MEK inhibitor
  • HY-115568
    BETd-246
    1 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity .
    BETd-246
  • HY-139590
    Zeteletinib

    BOS-172738; DS-5010

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
    Zeteletinib
  • HY-155303
    DCLK1-IN-2

    		Ser/Thr Protease Cancer
    DCLK1-IN-2 (compound I-5) is a potent DCLK1 inhibitor with an IC50 of 171.3  nM. DCLK1-IN-2 shows remarkable antiproliferative effects on SW1990 cell lines (IC50 of 0.6 μM) and in vivo antitumor potency .
    DCLK1-IN-2
  • HY-144232
    Anticancer agent 28

    		Others Cancer
    Anticancer agent 28 showed good antitumor activity in H22 allogeneic mice in vivo. Its potency in K562 cells was 50 times that of oridonin, and its < b > IC < sub > 50 < / sub > < / b > value was 0.09 μ M。
    Anticancer agent 28
  • HY-139590A
    Zeteletinib hemiadipate

    BOS-172738 hemiadipate; DS-5010 hemiadipate

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
    Zeteletinib hemiadipate
  • HY-12457
    Rachelmycin

    CC-1065; NSC 298223

    		 Antibiotic DNA/RNA Synthesis Infection Cancer
    Rachelmycin (CC-1065) is an antitumor antibiotic and a DNA-alkylating agent. Rachelmycin has cytotoxic potency that can be used as a cytotoxin to synthesis ADC. Rachelmycin effectively inhibits DNA synthesis. Rachelmycin can be used for cancer and infection research .
    Rachelmycin
  • HY-146438
    PPARγ agonist 3

    		PPAR Cancer
    PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
    PPARγ agonist 3
  • HY-147656
    NAMPT degrader-1

    		NAMPT Autophagy Cancer
    NAMPT degrader-1 (Compound A3) is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency .
    NAMPT degrader-1
  • HY-146439
    PPARγ agonist 4

    		PPAR Cancer
    PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
    PPARγ agonist 4
  • HY-B0305A
    Roxatidine Acetate Hydrochloride

    HOE 760

    		 Histamine Receptor Metabolic Disease Inflammation/Immunology Cancer
    Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity .
    Roxatidine Acetate Hydrochloride
  • HY-B0305
    Roxatidine acetate

    Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity .
    Roxatidine acetate
  • HY-109189
    Rezivertinib

    BPI-7711

    		 EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
    Rezivertinib
  • HY-15656
    Ceritinib
    Maximum Cited Publications
    29 Publications Verification

    LDK378

    		 Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Endocrinology Cancer
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
    Ceritinib
  • HY-15656A
    Ceritinib dihydrochloride
    Maximum Cited Publications
    29 Publications Verification

    LDK378 dihydrochloride

    		 Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Endocrinology Cancer
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency .
    Ceritinib dihydrochloride
  • HY-146755
    TIY-7

    		Trk Receptor Cancer
    TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
    TIY-7
  • HY-151453
    Topoisomerase IIα-IN-4

    		Topoisomerase Apoptosis Cancer
    Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .
    Topoisomerase IIα-IN-4
  • HY-111790
    M3258
    1 Publications Verification

    		 Proteasome Apoptosis Cancer
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
    M3258
  • HY-145836
    FGFR4-IN-8

    		FGFR Cancer
    FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
    FGFR4-IN-8

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