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antitumor efficacy

" in MedChemExpress (MCE) Product Catalog:

449

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GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13442A
    Eribulin mesylate
    5+ Cited Publications

    B1939 mesylate; E7389 mesylate; ER-086526 mesylate

    		 Microtubule/Tubulin Apoptosis Cancer
    Eribulin mesylate is an inhibitor for microtubule. Eribulin mesylate inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate exhibits antitumor efficacy in mouse model .
    Eribulin mesylate
  • HY-10977
    Tivozanib
    5+ Cited Publications

    AV-951; KRN951

    		 VEGFR Cancer
    Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy .
    Tivozanib
  • HY-132166
    Velzatinib
    1 Publications Verification

    M4205; IDRX-42

    		 c-Kit PDGFR c-Fms FLT3 Src Cancer
    Velzatinib (M4205) is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. Velzatinib exhibits antitumor efficacy in xenograft mouse models .
    Velzatinib
  • HY-139782
    SKLB325
    2 Publications Verification

    		 Histone Demethylase Apoptosis Cancer
    SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis . SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .
    SKLB325
  • HY-N7128
    Flavanone
    1 Publications Verification

    		 Cytochrome P450 ERK p38 MAPK NF-κB MMP PAI-1 Cancer
    Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). Flavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy .
    Flavanone
  • HY-111458
    GSK2643943A
    5+ Cited Publications

    		 Deubiquitinase Cancer
    GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
    GSK2643943A
  • HY-133117
    BAY-985
    4 Publications Verification

    		 IKK Cancer
    BAY-985, a chemical probe, is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy .
    BAY-985
  • HY-130115A
    IACS-8803 disodium
    1 Publications Verification

    		 STING Cancer
    IACS-8803 disodium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 disodium has a robust systemic antitumor efficacy .
    IACS-8803 disodium
  • HY-17547
    NMS-E973
    2 Publications Verification

    		 HSP Cancer
    NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy .
    NMS-E973
  • HY-115400
    1V209
    4 Publications Verification

    TLR7 agonist T7

    		 Toll-like Receptor (TLR) Cancer
    1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity .
    1V209
  • HY-100510
    RAF709
    5+ Cited Publications

    		 Raf Cancer
    RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively . Antitumor efficacy .
    RAF709
  • HY-101096
    Suvecaltamide

    MK-8998; CX-8998; JZP385

    		 Calcium Channel Neurological Disease Cancer
    Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
    Suvecaltamide
  • HY-N8342
    Rhamnazin
    1 Publications Verification

    		 VEGFR Inflammation/Immunology Cancer
    Rhamnazin is an orally active inhibitor of VEGFR2 signaling with an IC50 of 4.68 μM against VEGFR2 kinase. Rhamnazin shows potent antiangiogenic activity and antitumor efficacy . Rhamnazin shows antioxidant and anti-inflammatory properties .
    Rhamnazin
  • HY-P99833
    Cosibelimab

    CK-301; TG-1501

    		 PD-1/PD-L1 Cancer
    Cosibelimab (CK-301) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab exhibits antitumor efficacy .
    Cosibelimab
  • HY-10977A
    Tivozanib hydrochloride hydrate
    5+ Cited Publications

    AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate

    		 VEGFR Cancer
    Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy .
    Tivozanib hydrochloride hydrate
  • HY-150228
    MitoCur-1
    1 Publications Verification

    		 TrxR Cancer
    MitoCur-1, a curcumin analogue, is an inhibitor of mitochondrial antioxidative thioredoxin reductase 2 (TrxR2). MitoCur-1 has electrophilic and mitochondrial-targeting properties. MitoCur-1 induces reactive oxygen species (ROS) generation, exerts specifically antitumor efficacy .
    MitoCur-1
  • HY-130115
    IACS-8803

    		STING Cancer
    IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy .
    IACS-8803
  • HY-146034
    NOD1/2 antagonist-1

    		NOD-like Receptor (NLR) Inflammation/Immunology Cancer
    NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX) .
    NOD1/2 antagonist-1
  • HY-161078
    QP5038

    		Amyloid-β Cancer
    QP5038 (compound 28) is an inhibitor of QPCTL with an IC50 value of 3.8 nM. QP5038 has antitumor efficacy .
    QP5038
  • HY-116447
    Antitumor agent-159

    		Mitochondrial Metabolism Apoptosis Cancer
    Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
    Antitumor agent-159
  • HY-163767
    Antitumor agent-171

    		β-catenin Inflammation/Immunology Cancer
    Antitumor agent-171 (Compound 35) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 1.61 μM. Antitumor agent-171 exhibits high affinity to β-catenin with Kd of 0.63 μM. Antitumor agent-171 inhibits the gene expression of axin2 with IC50 of 0.84 μM. Antitumor agent-171 inhibits cell viability of HCT116 with IC50 of 4.39 μM. Antitumor agent-171 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
    Antitumor agent-171
  • HY-161765
    iHSP110-33

    		HSP STAT Cancer
    iHSP110-33 is an inhibitor for heat shock protein 110 (HSP110). iHSP110-33 exhibits antitumor efficacy agaisnt large B-cell lymphoma and classical Hodgkin lymphoma. iHSP110-33 shows a synergistic effect with Selinexor (HY-17536), inhibits the STAT6 phosphorylation, and enhances its antitumor activity. .
    iHSP110-33
  • HY-10080
    Teglarinad chloride

    GMX1777; EB-1627

    		 NAMPT Cancer
    Teglarinad chloride (GMX1777) is a proagent of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis .
    Teglarinad chloride
  • HY-157029S
    KRASG12D-IN-1

    		Ras Cancer
    KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
    KRASG12D-IN-1
  • HY-163768
    Antitumor agent-172

    		β-catenin Inflammation/Immunology Cancer
    Antitumor agent-172 (Compound 28) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 3.92 μM. Antitumor agent-172 exhibits high affinity to β-catenin with Kd of 82 nM. Antitumor agent-172 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
    Antitumor agent-172
  • HY-146231
    SS47

    		PROTACs MAP4K Inflammation/Immunology Cancer
    SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy .
    SS47
  • HY-176508
    KDX1381

    		Casein Kinase Cancer
    KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models .
    KDX1381
  • HY-157031S
    KRASG12D-IN-2

    		Ras Cancer
    KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
    KRASG12D-IN-2
  • HY-130116
    IACS-8779

    		STING Cancer
    IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy .
    IACS-8779
  • HY-130115B
    IACS-8803 diammonium
    1 Publications Verification

    		 STING Cancer
    IACS-8803 diammonium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 diammonium has a robust systemic antitumor efficacy .
    IACS-8803 diammonium
  • HY-150256
    YTP-17

    		YAP Cancer
    YTP-17 is an orally active YAP-TEAD protein-protein interaction inhibitor with an IC50 of 4 nM. YTP-17 shows anti-tumor efficacy .
    YTP-17
  • HY-164386
    Defoslimod

    OM 174

    		 Toll-like Receptor (TLR) Inflammation/Immunology Cancer
    Defoslimod (OM 174) is an agonist for TLR4 receptor and acts as an immunomodulator. Defoslimod activates macrophages and dendritic cells, induces cytokines secretion, and exhibits antitumor efficacy in rats .
    Defoslimod
  • HY-146397
    TD-802

    		PROTACs Androgen Receptor Cancer
    TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .
    TD-802
  • HY-130628
    PAK4-IN-1

    		PAK Cancer
    PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions .
    PAK4-IN-1
  • HY-109084A
    Conteltinib tetrahydrochloride

    CT-707 tetrahydrochloride

    		 FAK Cancer
    Conteltinib tetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride salt form of Conteltinib (HY-109084). Conteltinib tetrahydrochloride is the inhibitor for FAK (IC50=1.6 nM), ALK, and Pyk2. Conteltinib tetrahydrochloride exhibits a synergistic anti-tumor efficacy with Cabozantinib (HY-13016) .
    Conteltinib tetrahydrochloride
  • HY-13752
    STA-1474

    		HSP Cancer
    STA-1474 is an orally active and highly selective HSP90 inhibitor. STA-1474 can trigger tumor cell apoptosis. STA-1474 demonstrates significant antitumor efficacy in spontaneous canine cancer models (e.g., osteosarcoma, thyroid carcinoma). STA-1474 is promising for research of solid tumors (e.g., osteosarcoma, breast cancer) and HSP90-driven cancers .
    STA-1474
  • HY-162449
    GIC-20

    		Apoptosis Ferroptosis Cancer
    GIC-20 is a dual inducer for apoptosis and ferroptosis. GIC-20 exhibits antitumor efficacy against fibrosarcoma .
    GIC-20
  • HY-133117A
    (Rac)-BAY-985

    		IKK Cancer
    (Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy .
    (Rac)-BAY-985
  • HY-155313
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE

    		Drug-Linker Conjugates for ADC Cancer
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE
  • HY-124615
    ST-162

    		p38 MAPK PI3K Cancer
    ST-162 is a MAPK/PI3K dual antagonist. ST-162 exhibits antitumor activity and can increase the efficacy of immune checkpoint blockers. ST-162 can be used for the research of cancer, such as melanoma .
    ST-162
  • HY-129331
    Neothramycin A

    		Antibiotic Bacterial Fungal Infection Cancer
    Neothramycin A is an antibiotic, which can be isolated from Streptomyces. Neothramycin A exhibits board spectrum antimicrobial activity, inhibits Staphylococcus aureus, Klebsiella pneumoniae, Escherichia coli W677, and Saccharomyces cerevisia with MIC of 25-50 μg/mL. Neothramycin A exhibits antitumor efficacy against leukemia in mouse models .
    Neothramycin A
  • HY-161774
    ST80

    		CD73 Cancer
    ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC) .
    ST80
  • HY-170570
    PFM046

    		LXR Stearoyl-CoA Desaturase (SCD) Fatty Acid Synthase (FASN) Cancer
    PFM046 is the antagonist for liver X receptor (LXR), that inhibits the activation of LXRα and LXRβ with IC50 of 2.04 μM and 1.58 μM. PFM046 inhibits the expression of SCD1 and FASN, upregulates the expression of ABCA1, and exhibits antitumor efficacy in mouse models .
    PFM046
  • HY-P10239A
    Tyr3-Octreotate acetate

    		Radionuclide-Drug Conjugates (RDCs) Cancer
    Tyr3-Octreotate acetate is a somatostatin analog. Tyr3-Octreotate acetate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate acetate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
    Tyr3-Octreotate acetate
  • HY-155647
    Microtubule stabilizing agent-1

    		Microtubule/Tubulin Cancer
    Microtubule stabilizing agent-1 (compound 3l) is a Paclitaxel derivative that efficiently promotes tubulin polymerization. Microtubule stabilizing agent-1 shows antitumor efficacy .
    Microtubule stabilizing agent-1
  • HY-164484
    IHMT-RAF-128

    		Raf Cancer
    IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities .
    IHMT-RAF-128
  • HY-173065
    CDK9-IN-36

    		CDK Apoptosis Cancer
    CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model .
    CDK9-IN-36
  • HY-147695
    c-Met-IN-12

    		c-Met/HGFR Cancer
    c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy .
    c-Met-IN-12
  • HY-121349
    Aerothionin

    		Bacterial Fungal Antibiotic Infection Cancer
    Aerothionin is an antibiotic with potent antimicrobial efficacy against bacteria and fungi. Aerothionin exhibits antitumor efficacy against adrenal pheochromocytomas and extra-adrenal paragangliomas (PPGLs) .
    Aerothionin
  • HY-161077
    QP5020

    		Amyloid-β Cancer
    QP5020 (compound 28) is an inhibitor of QPCTL with an IC 50 value of 15 nM. QP5020 has antitumor efficacy .
    QP5020

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