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patient-derived

" in MedChemExpress (MCE) Product Catalog:

36

Inhibitors & Agonists

1

Peptides

6

Inhibitory Antibodies

1

Natural
Products

1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-128350A
    FGTI-2734 mesylate
    1 Publications Verification

    		 Farnesyl Transferase γ-Glutamyl Transferase (GGT) Cancer
    FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
    FGTI-2734 mesylate
  • HY-128350
    FGTI-2734
    1 Publications Verification

    		 Farnesyl Transferase Cancer
    FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
    FGTI-2734
  • HY-153268
    Silevertinib
    1 Publications Verification

    BDTX-1535; EGFR-IN-76

    		 EGFR Cancer
    BDTX-1535 (EGFR-IN-76) is an orally available, blood-brain permeable, selective EGFR inhibitor with anti-tumor activity. BDTX-1535 is indicated in a variety of models including non-small cell lung cancer, glioblastoma patient-derived tumors, and intracranial tumors .
    Silevertinib
  • HY-P99268
    Seribantumab

    SAR 256212; MM 121; Anti-Human ERBB3/ErbB 3 Recombinant Antibody

    		 EGFR Apoptosis Cancer
    Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models .
    Seribantumab
  • HY-149556
    MTX-241F

    		EGFR PI3K Cancer
    MTX-241F is a selective small molecule inhibitor targeting EGFR and PI3 kinase family members. MTX-241F is able to penetrate the blood-brain barrier and control tumor growth over the long term. MTX-241F exhibits radiosensitizing activity in patient-derived DIPG neurospheres and may be used in the study of diffuse intrinsic pontine glioma (DIPG) .
    MTX-241F
  • HY-N10365
    6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine

    		Autophagy Neurological Disease
    6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine, a alkaloid, significantly perturbates the features of cellular organelles including early endosomes, mitochondria and autophagosomes (Parkinson’s Disease patient-derived olfactory cells) .
    6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine
  • HY-P991433
    BIIB036

    		TNF Receptor Cancer
    BIIB036 is a human IgG1 monoclonal antibody (mAb) targeting TNFRSF12A/Fn14. BIIB036 inhibits the growth of patient-derived primary colorectal tumors in SCID mice .
    BIIB036
  • HY-175212
    PDGFRA-IN-1

    		PDGFR Cancer
    PDGFRA-IN-1 (Compound 4p) is a Platelet-derived growth factor receptor A (PDGFRA) inhibitor with an IC50 of 1.25  μM. PDGFRA-IN-1 has a significant anticancer activity and potently kills cancer cells including primary patient-derived glioma cells .
    PDGFRA-IN-1
  • HY-163301
    Antitumor agent-139

    		Reactive Oxygen Species (ROS) Cancer
    Antitumor agent-139 (compound 9b) is a liver - and mitochondria-targeting gold(I) complexe, and produces reactive oxygen species (ROS) and facilitates DNA excretion. Antitumor agent-139 inhibits tumor growth in a patient-derived xenograft model of hepatocellular carcinoma .
    Antitumor agent-139
  • HY-173320
    HEMTAC WEE1 degrader-1

    		Wee1 HSP Cancer
    HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .
    HEMTAC WEE1 degrader-1
  • HY-144670
    ALDH3A1-IN-1

    		Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of ALDH3A1 with an IC50 of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination research with docetaxel .
    ALDH3A1-IN-1
  • 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-150072
    DS89002333

    		PKA Cancer
    DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC) .
    DS89002333
  • HY-147165
    VT02956

    		YAP Cancer
    VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VT02956
  • HY-147165A
    VT02956 hydrochloride

    		YAP Cancer
    VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VT02956 hydrochloride
  • HY-156020
    Glucocerebrosidase-IN-2

    		Glycosidase Metabolic Disease
    Glucocerebrosidase-IN-2 (compound 12) is a quinazoline analogue and an inhibitor of glucocerebrosidase (GC). Glucocerebrosidase-IN-2 has the potential to improve GC translocation to lysosomes in Gaucher disease patient-derived cells (mostly carrying the N370S mutation). Glucocerebrosidase-IN-2 inhibits the hydrolysis of 4-methylumbelliferone β-D-glucopyranoside (4MU) and fluorescent glycosylceramide (FlourGC) in N370S mutant tissues with an AC50 of 25.29 μM .
    Glucocerebrosidase-IN-2
  • HY-P99623
    Flotetuzumab

    MGD006; S80880

    		 CD3 Cancer
    Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
    Flotetuzumab
  • HY-155246
    PARP1-IN-15

    		Apoptosis PARP Cancer
    PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .
    PARP1-IN-15
  • HY-114162B
    VTP50469 mesylate

    		Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
    VTP50469 mesylate
  • HY-172902
    RNA binder 1

    		DNA/RNA Synthesis Neurological Disease
    RNA binder 1 (Compound 4b) is a blood-brain permeable RNA binder. RNA binder 1 can selectively bind to the G-quadruplex structure of the G4C2 repeat sequence RNA of the C9orf72 gene. RNA binder 1 significantly reduces the levels of toxic polypeptides poly(GA) and poly(GP) produced by the G4C2 repeat sequence in amyotrophic lateral sclerosis (ALS) patient-derived cells. RNA binder 1 has no significant effect on the antisense polypeptide poly(PR), showing selectivity for sense RNA. RNA binder 1 can be used in the study of ALS and frontotemporal dementia (FTD) .
    RNA binder 1
  • HY-116504
    WB-308

    		EGFR Akt ERK Apoptosis Cancer
    WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
    WB-308
  • HY-168555
    YJ1206

    		CDK PROTACs Apoptosis Cancer
    YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
    YJ1206
  • HY-159834
    Progerinin

    SLC-D011

    		 DNA/RNA Synthesis Others
    Progerinin (SLC-D011) is an orally active progerin-lamin A binding inhibitor. Progerinin selectively binds to the C-terminal region of progerin, disrupting its interaction with lamin A and promoting progerin degradation while sparing wild-type lamin A, B, and C. Progerinin ameliorates nuclear deformation, increases H3K9me3 levels, and reduces progerin expression in HGPS patient-derived fibroblasts. Progerinin extends lifespan in Lmna G609G/G609G mice and Lmna G609G/+ mice, improves body weight, hair morphology, cardiac function, and histological phenotypes. Progerinin can be used for the study of Hutchinson-Gilford progeria syndrome (HGPS) .
    Progerinin
  • HY-131374
    TN14003

    		CXCR Cancer
    TN14003 is a CXCR4 inhibitor. TN14003 has antitumor activity .
    TN14003
  • HY-132283
    PF-9363
    3 Publications Verification

    CTx-648

    		 Histone Acetyltransferase Cancer
    PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer .
    PF-9363
  • HY-162713
    MTX-531

    		EGFR PI3K PPAR Cancer
    MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors .
    MTX-531
  • HY-112816A
    MA242 free base

    		MDM-2/p53 Apoptosis Cancer
    MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
    MA242 free base
  • HY-112816
    MA242

    		MDM-2/p53 Apoptosis Cancer
    MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
    MA242
  • HY-117548
    UNC1062
    2 Publications Verification

    		 TAM Receptor Apoptosis p38 MAPK ERK PI3K Akt JAK STAT Cardiovascular Disease Cancer
    UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis .
    UNC1062
  • HY-178061
    APS03118

    		ERK RET Cancer
    APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
    APS03118
  • HY-175785
    X15695

    		Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Apoptosis MDM-2/p53 Cancer
    X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer .
    X15695
  • HY-178944
    CDC25-IN-1

    		Phosphatase Apoptosis Caspase Cancer
    CDC25-IN-1 (Compound D11b) is a potent inhibitor of cell division cycle 25 (CDC25) phosphatase. CDC25-IN-1 exerts strong inhibitory effects on leukemia and colorectal cancer cells. CDC25-IN-1 blocks CDC25 mediated CDK1 Tyr15 dephosphorylation, delays G2/M progression, and induces caspase-dependent apoptosis with DNA damage. CDC25-IN-1 can be used for researches of leukemia and colorectal cancer .
    CDC25-IN-1
  • HY-153967
    BLU0588
    1 Publications Verification

    		 PKA Cancer
    BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research .
    BLU0588
  • HY-P99011
    Cibisatamab
    1 Publications Verification

    		 CD3 Cancer
    Cibisatamab, a T cell bispecific antibody, binds Carcino-Embryonic Antigen (CEA) on cancer cells and CD3 on T cells. Cibisatamab triggers T cell killing of cancer cell lines expressing moderate to high levels of CEA at the cell surface. Cibisatamab can be used for colorectal cancer research .
    Cibisatamab
  • HY-P99215
    Parsatuzumab

    Anti-EGFL7; RG 7414

    		 VEGFR Cancer
    Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition .
    Parsatuzumab
  • HY-153356
    MRT-2359

    		Apoptosis Cancer
    MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
    MRT-2359

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