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Results for "

tumor+regression

" in MedChemExpress (MCE) Product Catalog:

103

Inhibitors & Agonists

1

Fluorescent Dyes

12

Inhibitory Antibodies

3

Click Chemistry

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-136927
    MSA-2
    25+ Cited Publications

    		 STING Inflammation/Immunology Cancer
    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
    MSA-2
  • HY-156498
    RMC-7977
    10+ Cited Publications

    		 Ras ERK Raf Ribosomal S6 Kinase (RSK) AMPK Apoptosis PARP Cancer
    RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
    RMC-7977
  • HY-145483
    KT-474
    1 Publications Verification

    KYM-001; PROTAC IRAK4 degrader-7

    		 PROTACs IRAK Apoptosis Cancer
    KT-474 (KYM-001; PROTAC IRAK4 degrader-7) is an orally active PROTAC IRAK4 degrader with anti-tumor effects. KT-474 inhibits the cell cycle and induces apoptosis. KT-474 induces tumor regression in a xenograft model of MYD88-mutated ABC DLBCL. KT-474 is a click chemistry reagent, containing an alkyne group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups .
    KT-474
  • HY-12885
    2’3’-c-di-AM(PS)2 (Rp,Rp)
    Maximum Cited Publications
    87 Publications Verification

    ADU-S100; MIW815; ML RR-S2 CDA

    		 STING Inflammation/Immunology Cancer
    2’3’-c-di-AM(PS)2 (Rp,Rp) (ADU-S100), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity .
    2’3’-c-di-AM(PS)2 (Rp,Rp)
  • HY-12885B
    2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt
    Maximum Cited Publications
    87 Publications Verification

    ADU-S100 ammonium salt; MIW815 ammonium salt; ML RR-S2 CDA ammonium salt

    		 STING Inflammation/Immunology Cancer
    2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt (ADU-S100 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity .
    2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt
  • HY-129602
    SD-36
    Maximum Cited Publications
    9 Publications Verification

    		 PROTACs STAT Apoptosis Cancer
    SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SD-36
  • HY-156681
    Tersolisib
    1 Publications Verification

    STX-478; STX-478-101; LY4064809

    		 PI3K Cancer
    STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .
    Tersolisib
  • HY-147250
    Lirafugratinib
    1 Publications Verification

    RLY-4008

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib
  • HY-157228
    ACBI3

    		PROTACs Ras Cancer
    ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
    ACBI3
  • HY-175749
    BMS-986463

    		Molecular Glues Wee1 Inflammation/Immunology Cancer
    BMS-986463, a CRBN E3 ligase modulator (CELMoD), is a WEE1 kinase molecular glue degrader. BMS-986463 significantly inhibits tumor regression and reduces the level of phospho-CDK2. BMS-986463 can be used for advanced malignant solid tumors like non-small cell lung cancer (NSCLC) research .
    BMS-986463
  • HY-164992
    Trastuzumab vedotin
    2 Publications Verification

    MRG002; Trastuzumab MMAE

    		 Antibody-Drug Conjugates (ADCs) EGFR Microtubule/Tubulin Cancer
    Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
    Trastuzumab vedotin
  • HY-141523
    Vociprotafib

    RMC-4630; SHP2-IN-7

    		 SHP2 Phosphatase Cancer
    Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
    Vociprotafib
  • HY-P9933
    Dinutuximab

    APN-311; Ch14.18; MAb-14.18

    		 Apoptosis PERK mTOR Cancer
    Dinutuximab (APN-311) is a chimeric human-mouse anti-GD2 monoclonal antibody. Dinutuximab can bind to GD2 on the cell surface, triggering antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity, and promoting tumor regression. Dinutuximab can inhibit the growth, invasion, and migration and induce apoptosis of tumor cells. Dinutuximab can be used in the research of tumors such as neuroblastoma and breast cancer .
    Dinutuximab
  • HY-163410
    AU-24118
    1 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .
    AU-24118
  • HY-148807
    Zavondemstat

    QC8222 free base; TACH 101 free base

    		 Histone Demethylase Apoptosis Cancer
    Zavondemstat (QC8222 free base; TACH 101 free base) is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
    Zavondemstat
  • HY-148813
    AK-2292
    2 Publications Verification

    		 PROTACs STAT Cancer
    AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AK-2292
  • HY-161952
    Sitneprotafib

    JAB-3312

    		 SHP2 Cancer
    Sitneprotafib (JAB-3312) is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. Sitneprotafib has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
    Sitneprotafib
  • HY-P99948
    Etevritamab

    AMG-596

    		 EGFR CD3 Neurological Disease Cancer
    Etevritamab (AMG-596) is a bispecific T-cell engager that targets EGFRvIII and CD3. Etevritamab simultaneously binds CD3 on T cells and EGFRvIII on glioblastoma multiforme cells, thereby forming a bridge structure. Etevritamab triggers T-cell activation, proliferation, secretion of cytotoxic substances, and tumor cell lysis. Etevritamab extends overall survival and induces tumor regression in mouse models of glioblastoma multiforme. Etevritamab can be used for research related to glioblastoma .
    Etevritamab
  • HY-147250A
    Lirafugratinib hydrochloride
    1 Publications Verification

    RLY-4008 hydrochloride

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib hydrochloride
  • HY-114440
    Belapectin

    GR-MD-02

    		 Galectin Apoptosis Cancer
    Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM .
    Belapectin
  • HY-172429
    Enozertinib

    ORIC-114

    		 EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
    Enozertinib
  • HY-128481
    SB24011

    		STING Inflammation/Immunology Cancer
    SB24011 is a STING modulator and a TRIM29-STING protein-protein interaction inhibitor. SB24011 blocks TRIM29-induced K48-linked specific ubiquitination by binding to STING, thereby upregulating intracellular STING protein levels. SB24011 enhances inflammatory cytokine expression and STING-mediated immune responses, and exhibits abscopal antitumor activity that promotes tumor regression and activates T cell infiltration. When combined with STING agonists or anti-PD1 antibodies, SB24011 synergistically enhances antitumor responses. SB24011 is suitable for research related to colon cancer and melanoma .
    SB24011
  • HY-153358
    TNG260

    		HDAC Cancer
    TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .
    TNG260
  • HY-17493
    MI-773
    5+ Cited Publications

    		 MDM-2/p53 Apoptosis Neurological Disease Cancer
    MI-773 is an orally active, selective MDM2-p53 interaction inhibitor with a Ki of 0.88 nM for MDM2. MI-773 blocks the MDM2-TP53 interaction. MI-773 potently activates p53. MI-773 induces Apoptosis. MI-773 causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma .
    MI-773
  • HY-169360
    SD-436

    		PROTACs STAT Cancer
    SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma (Pink: STAT3 ligand (HY-169361); Blue: E3 ligase ligand (HY-43722); Black: linker (HY-147052) .
    SD-436
  • HY-157229
    STX-721
    1 Publications Verification

    		 EGFR ERK Cancer
    STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
    STX-721
  • HY-132234
    M-1211

    		Epigenetic Reader Domain Cancer
    M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression .
    M-1211
  • HY-136447
    ASP4132
    1 Publications Verification

    		 AMPK Cancer
    ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
    ASP4132
  • HY-P99776
    Plamotamab

    XmAb-13676

    		 CD20 CD3 Cancer
    Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 + expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .
    Plamotamab
  • HY-172429A
    Enozertinib hemihydrate

    ORIC-114 hemihydrate

    		 EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
    Enozertinib hemihydrate
  • HY-148274
    KTX-582

    		PROTACs IRAK Apoptosis Cancer
    KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88 MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model .
    KTX-582
  • HY-13479
    EC144

    		HSP Cancer
    EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases . EC144 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EC144
  • HY-175743
    TYRA-200

    		FGFR Cancer
    TYRA-200 is a potent and orally active FGFR2 inhibitor. TYRA-200 inhibits the kinase activity of wild-type FGFR2 and its mutants. TYRA-200 induces significant tumor regression in FGFR2-driven cancer models. TYRA-200 can be used for the research of FGFR2-altered advanced solid tumors, intrahepatic cholangiocarcinoma, and endometrial cancer .
    TYRA-200
  • HY-148511
    Vidutolimod

    CMP-001

    		 Toll-like Receptor (TLR) IFNAR PD-1/PD-L1 Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Vidutolimod (CMP-001) is a virus-like particle containing a TLR9 activator . Vidutolimod induces human peripheral blood mononuclear cells to secrete IFNα, and upregulates the gene expression of CXCL10, PDL1, IDO and CD80. Vidutolimod activates TLR9, which in turn triggers plasmacytoid dendritic cell activation, production of IFNγ and TNFα, induction of CXCL10, and recruitment of antitumor T cells. Vidutolimod causes influenza-like symptoms, hypotension and tumor regression, and its activity depends on the presence of anti-Qβ antibodies. Vidutolimod modulates monocyte function, promotes CD4 T cell proliferation, and activates multiple immune cell types in an environment with anti-Qβ antibodies. Vidutolimod prolongs the survival of tumor-bearing mice. Vidutolimod is used in research related to advanced melanoma, head and neck squamous cell carcinoma, and advanced non-small cell lung cancer .
    Vidutolimod
  • HY-155537
    Pruvonertinib
    1 Publications Verification

    YK-029A

    		 EGFR Cancer
    YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFR T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models .
    Pruvonertinib
  • HY-172423
    Darlifarnib

    KO-2806

    		 Farnesyl Transferase mTOR VEGFR Cancer
    Darlifarnib (KO-2806) is an orally active farnesyl transferase inhibitor. Darlifarnib inhibits the mTORC1 signaling pathway, thereby enhancing the anti-angiogenic properties of tyrosine kinase inhibitors. When used in combination with anti-VEGFR tyrosine kinase inhibitors, Darlifarnib promotes renal cell carcinoma tumor regression and inhibits tumor neovascularization. Darlifarnib sensitizes renal cell carcinoma tumors that progress after anti-VEGFR TKI treatment .
    Darlifarnib
  • HY-155356
    YN14

    		PROTACs Ras Cancer
    YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
    YN14
  • HY-174850
    CFON-026

    		Btk Cancer
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
    CFON-026
  • HY-P991358
    XOMA-213

    LFA-102; X213

    		 Estrogen Receptor/ERR STAT Akt Cancer
    XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer .
    XOMA-213
  • HY-159643
    NDI-101150

    		MAP4K IFNAR Interleukin Related Inflammation/Immunology Cancer
    NDI-101150 is an orally active, potent and selective hematopoietic progenitor cell kinase 1 (HPK1) inhibitor with an IC50 of 0.7 nM. NDI-101150 blocks HPK1-mediated negative regulation of immune receptor signaling, inhibits immunosuppression of T cell activation, enhances antigen-specific antibody production and augments B-cell activation. NDI-101150 inhibits tumor growth in syngeneic tumor models, establishes durable antitumor immune memory, and synergizes with anti-PD1 to enhance exhausted T cell activity and drive tumor regressions. NDI-101150 can be used for the research of cancer, such as breast cancer and colon cancer .
    NDI-101150
  • HY-178238
    LD2-3

    		ADC Payload Topoisomerase Cancer
    LD2-3 is a cytotoxic compound derived from Exatecan (HY-13631), designed to be conjugated with anti-FGFR2b or anti-CEA antibodies to form intact antibody-drug conjugate (ADC) molecules. LD2-3 exhibits a remarkable bystander killing effect: it not only effectively kills FGFR2b-positive tumor cells, but also eliminates surrounding FGFR2b-negative cells in co-culture and mixed tumor xenograft models, thereby inducing complete tumor regression. LD2-3 can be used for anti-tumor research in relevant fields such as gastric cancer and lung cancer .
    LD2-3
  • HY-10984A
    (S)-Pomalidomide

    (S)-CC-4047

    		 Endogenous Metabolite Cancer
    (S)-Pomalidomide ((S)-CC-4047) is an angiogenesis-inhibiting drug with growth-inhibitory activity against B-cell tumors. (S)-Pomalidomide can induce complete tumor regression in BurKitt lymphoma cells. (S)-Pomalidomide serves as an immunomodulator with potential applications in inhibiting hematological malignancies .
    (S)-Pomalidomide
  • HY-111965
    PF-06647263

    anti-EFNA4-ADC

    		 Antibody-Drug Conjugates (ADCs) DNA Alkylator/Crosslinker Antibiotic Apoptosis Cancer
    PF-06647263 is an ADC targeting EFNA4, consisting of EFNA4 Antibody (HY-P991109), ADC toxin Calicheamicin (HY-19609) and a linker. PF-06647263 exhibits anti-tumor activity and induces significant tumor regression in TNBC xenografts .
    PF-06647263
  • HY-100765
    BI-0252

    		MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis .
    BI-0252
  • HY-126850
    4-Epidoxycycline

    		EGFR Cancer
    4-Epidoxycycline is a liver metabolite of the antibiotic doxycycline (doxycycline, HY-N0565) and doesn't have antibiotic properties in mice. 4-Epidoxycycline’s ability to regulate HER2 gene expression in vitro and in live mouse models is similar to that of doxycycline, and it shows comparable high efficacy in tumor tissues, achieving over 95% tumor regression rates .
    4-Epidoxycycline
  • HY-174458
    MD-4251

    		PROTACs MDM-2/p53 IKZF Family Casein Kinase Cancer
    MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
    MD-4251
  • HY-118899
    XR5944

    		Endogenous Metabolite Cancer
    XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
    XR5944
  • HY-155847
    LYP-IN-3

    		Phosphatase PD-1/PD-L1 Inflammation/Immunology Cancer
    LYP-IN-3 is a selective, orally active and reversible lymphoid-tyrosine phosphatase (LYP) inhibitor (IC50 = 2.55 μM, Ki = 0.93 μM). D34 exhibits high selectivity of PTP1B, PTPN12, PTPN5 and SSH2. LYP-IN-3 regulates the T-cell receptor (TCR) signaling by specifically inhibiting LYP. LYP-IN-3 does not significantly inhibit MC38 cell viability; its anti-tumor effect stems from immune regulation. LYP-IN-3 can significantly upregulate PD-L1 or PD-1 expression in different immune cells. LYP-IN-3 facilitates T-cell infiltration and enhances T-cell functions. LYP-IN-3 synergizes with PD-L1 blockade can significantly improve colorectal tumor regression. LYP-IN-3 can be used for the study of colorectal cancer .
    LYP-IN-3
  • HY-114228
    PROTAC BET degrader-2
    2 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
    PROTAC BET degrader-2
  • HY-169327
    MD-265

    		PROTACs MDM-2/p53 Cancer
    MD-265 is a PROTAC degrader that can break down MDM2, leading to activation of p53 in cancer cells carrying wild-type p53. MD-265 achieves complete tumor regression and improves long-term survival of mice with leukemia. (Pink: MI-1063 (HY-133754); Black: linker; Blue: Lenalidomide (HY-A0003) .
    MD-265

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