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Antitumor+efficacy

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309

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13636
    Fulvestrant
    Maximum Cited Publications
    133 Publications Verification

    ICI 182780; ZD 9238; ZM 182780

    		 Estrogen Receptor/ERR Autophagy Apoptosis Inflammation/Immunology Cancer
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
    Fulvestrant
  • 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-112090
    ABBV-744
    5+ Cited Publications

    		 Epigenetic Reader Domain HIV Infection Inflammation/Immunology Cancer
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
    ABBV-744
  • 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-150233
    Cys-McMMAF

    		Microtubule/Tubulin Cancer
    Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models) .
    Cys-McMMAF
  • 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-13302
    CP-547632
    1 Publications Verification

    		 VEGFR FGFR Cancer
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .
    CP-547632
  • 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-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-164285
    MYX1715

    IMP1320

    		 ADC Payload N-myristoyltransferase Cancer
    MYX1715 is an inhibitor of N-Myristoyltransferase (NMT) with a KD value of 0.09 nM. MYX1715 inhibits the proliferation of LU0884 and LU2511 with IC50 values of 44 nM and 9 nM. MYX1715 exhibits antitumor efficacy against neuroblastoma and gastric cancer in mouse models. MYX1715 can be used as ADC toxin .
    MYX1715
  • HY-141606
    Anetumab ravtansine

    BAY 94-9343

    		 Microtubule/Tubulin Antibody-Drug Conjugates (ADCs) Cancer
    Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models .
    Anetumab ravtansine
  • 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-50672
    MK-0731

    		Kinesin Apoptosis Lipoxygenase Cancer
    MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy .
    MK-0731
  • 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-W014395
    Dithiodipropionic acid

    		Reactive Oxygen Species (ROS) Apoptosis Cancer
    Dithiodipropionic acid can interact with CPUL1 (HY-151802) (a TrxR inhibitor) to form nanoaggregates (CPUL1-DA NAs). CPUL1-DA NAs generates more abundant ROS to induce cell apoptosis than that of free CPUL1, and improves antitumor efficacy against HUH7 cancer cells .
    Dithiodipropionic acid
  • 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-P99320
    Tarextumab

    OMP 59R5; Anti-Human NOTCH2 Recombinant Antibody

    		 Notch Cancer
    Tarextumab (OMP-59R5) is a cross-reactive, fully human IgG2 antibody that selectively inhibits Notch2 and Notch3 signaling. Tarextumab demonstrates broad-spectrum antitumor efficacy in xenograft models of epithelial tumors. Tarextumab can be used for the study of pancreatic cancer .
    Tarextumab
  • HY-13636S
    Fulvestrant-d3

    ICI 182780-d3; ZD 9238-d3; ZM 182780-d3

    		 Isotope-Labeled Compounds Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
    Fulvestrant-d3
  • HY-P99493
    Cantuzumab ravtansine
    1 Publications Verification

    IMGN242; huC242-DM4

    		 Antibody-Drug Conjugates (ADCs) Microtubule/Tubulin Cancer
    Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (HY-12454). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
    Cantuzumab ravtansine
  • HY-130115
    IACS-8803

    		STING Cancer
    IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy .
    IACS-8803
  • 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-P990902
    Atigotatug

    BMS-986012

    		 Transmembrane Glycoprotein Cancer
    Atigotatug (BMS-986012) is a fully human IgG1 antibody binds specifically to FucGM1 with an EC50 of 0.15 nmol/L for FucGM1. Atigotatug is a FcγRIIIa ligand with a Kd of 21 nmol/L. Atigotatug demonstrates antitumor efficacy in multiple mouse small cell lung cancer models .
    Atigotatug
  • HY-13302B
    CP-547632 hydrochloride
    1 Publications Verification

    		 VEGFR FGFR Cancer
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .
    CP-547632 hydrochloride
  • HY-121522
    SD-70

    		Histone Demethylase Cancer
    SD-70 is an inhibitor for histone demethylase JMJD2C and exhibits antitumor efficacy. SD-70 inhibits viability of cancer cells CWR22Rv1 (9% cell survival at 10 μM), PC3 (14% cell survival at 2 μM) and DU145 (26% cell survival at 2 μM) .
    SD-70
  • HY-159886
    MG-C-30

    		TNF Receptor Inflammation/Immunology
    MG-C-30 is an orally active agonist for CD27 with an EC50 of 0.84 μM. MG-C-30 activates NK cells and T cell co-stimulatory signals, and enhances immune response. MG-C-30 exhibits antitumor efficacy in mouse EG7-OVA model .
    MG-C-30
  • 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-160649
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan

    		Drug-Linker Conjugates for ADC Topoisomerase Cancer
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo .
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
  • 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-164397
    XMU-MP-5

    		Anaplastic lymphoma kinase (ALK) Apoptosis Cancer
    XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC50s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice .
    XMU-MP-5
  • 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-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-128778
    Gozanertinib

    DBPR112

    		 EGFR Cancer
    Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy .
    Gozanertinib
  • HY-164955
    TTK/PLK1-IN-1

    		Mps1 Polo-like Kinase (PLK) Cancer
    TTK/PLK1-IN-1 (Formula I) is the inhibitor for threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1) with IC50 of 7 nM and 72 nM. TTK/PLK1-IN-1 regulates spindle assembly checkpoint (SAC), and exhibits antitumor efficacy against TNBC .
    TTK/PLK1-IN-1
  • HY-144614
    JH-XVII-10

    		DYRK Apoptosis Neurological Disease Cancer
    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .
    JH-XVII-10
  • HY-170434
    Bfl-1-IN-6

    		Bcl-2 Family Caspase Cancer
    Bfl-1-IN-6 (Compound 20) is an orally active inhibitor for Bcl-2 related protein A1 (BFL1) with an IC50 of 19 nM. Bfl-1-IN-6 stabilizes BFL1 protein, activates cleaved caspase 3, and exhibits antitumor efficacy in mouse models .
    Bfl-1-IN-6
  • 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-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-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-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-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-146697
    IHMT-TRK-284

    		Trk Receptor c-Fms PDGFR Bcr-Abl c-Kit Apoptosis Cancer
    IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
    IHMT-TRK-284

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