Search Result
Results for "
B cell malignancy
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-15582
-
|
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Microtubule/Tubulin
ADC Payload
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Cancer
|
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Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
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-
-
- HY-15771
-
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ONO-4059; GS-4059
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Btk
Apoptosis
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Inflammation/Immunology
Cancer
|
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Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies .
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-
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- HY-129390
-
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ICP-022
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Btk
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Cancer
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Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK .
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-
-
- HY-132844
-
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HL-085
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MEK
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Cancer
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Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .
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-
-
- HY-160141
-
|
BGB-16673; BTK-IN-29
|
PROTACs
Btk
NF-κB
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Inflammation/Immunology
Cancer
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BGB-16673 (BGB-16673) is an orally active, selective BTK PROTAC degrader (IC50=0.69 nM). BGB-16673 ligates BTK to E3 ubiquitin ligase, causing BTK to undergo polyubiquitination, which is then recognized and degraded by the proteasome, thereby exerting efficient BTK degradation activity. BGB-16673 can be used in the research of B-cell malignancies such as chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma .
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-
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- HY-150105
-
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BMF-219; Menin-MLL inhibitor 21
|
Epigenetic Reader Domain
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
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Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes .
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-
-
- HY-109068
-
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INCB050465; IBI-376
|
PI3K
|
Cancer
|
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Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies .
|
-
-
- HY-103019
-
|
(+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib
|
Drug Isomer
CDK
Apoptosis
DNA/RNA Synthesis
|
Inflammation/Immunology
Cancer
|
Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC50=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma .
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-
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- HY-109198
-
|
ME-401; PWT-143
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PI3K
Akt
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Cancer
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Zandelisib (ME-401) is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma .
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-
-
- HY-15771A
-
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ONO-4059 hydrochloride; GS-4059 hydrochloride
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Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies .
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-
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- HY-15999A
-
|
PRT062070 hydrochloride; PRT2070 hydrochloride
|
Syk
JAK
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Cancer
|
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Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies .
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-
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- HY-P990033
-
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CC-95251; BMS-986351
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CD47
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Cancer
|
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Anzurstobart is a CD47/SIRPα inhibitor with human SIRPα Kd of 0.0541 nM and human SIRPα IC50 of 100 nM. Anzurstobart binds SIRPα at a CD47-overlapping site, blocks CD47-SIRPα interactions, inhibits CD47-SIRPα axis signaling, and binds across 6 prevalent human SIRPα haplotypes. Anzurstobart binds SIRPγ and inhibits CD47-SIRPγ interactions. Anzurstobart can be used for the research of non-Hodgkin's lymphoma, colorectal cancer, squamous cell carcinoma of the head and neck, diffuse large B-cell lymphoma, and advanced solid and hematologic malignancies .
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-
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- HY-142648
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MLT-985
1 Publications Verification
|
MALT1
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Cancer
|
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MLT-985 is a selective allosteric and orally active MALT1 inhibitor with an IC50 value of 3 nM. MLT-985 can suppress cell growth and aberrant CARD11/BCL10/MALT1 complex signaling. MLT-985 can be used for the research of cancer, such as B cell malignancies .
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-
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- HY-139481
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TL-895
1 Publications Verification
|
Btk
BMX Kinase
Interleukin Related
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor. TL-895 is active against recombinant BTK (average IC50: 1.5 nM) and inhibits only three additional kinases BLK, BMX (IC50 = 1.6 nM) and TXK with IC50 within tenfold of BTK activity. TL-895 inhibits BTK auto-phosphorylation at the Y223 phosphorylation site (IC50: 1-10 nM). The TL-895 effectively inhibits the production of inflammatory factors such as IL-8, IL-1β, MCP-1 and TNF-α by monocytes or macrophages, and reduces the chemotactic migration of MF cells towards SDF-1. TL-895 is used be for studies of chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and B-cell malignancies .
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-
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- HY-154860
-
|
|
PROTACs
Btk
Apoptosis
Caspase
Bcl-2 Family
NF-κB
Akt
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Inflammation/Immunology
Cancer
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PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease .
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-
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- HY-114256
-
|
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PSMA
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Cancer
|
|
EC1169 is a cytotoxic maytansinoid conjugate that specifically binds to prostate-specific membrane antigen (PSMA). EC1169 precisely delivers the maytansinoid B hydrazide payload to PSMA-positive cells to exert antitumor activity. EC1169 only inhibits the growth of PSMA-positive cells but has no effect on PSMA-negative cells, and enables complete recovery in mice bearing PSMA-positive tumors. EC1169 exhibits safety with no body weight loss or major organ damage induced. EC1169 is used in studies of prostate cancer and other PSMA-expressing malignancies .
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-
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- HY-124645
-
|
|
Flavivirus
Dengue Virus
Btk
MNK
|
Infection
Cancer
|
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QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC50s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies .
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-
-
- HY-15582S
-
|
|
Isotope-Labeled Compounds
Microtubule/Tubulin
ADC Payload
|
Cancer
|
|
Auristatin E-d8 is the deuterium labeled Auristatin E (HY-15582). Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
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-
-
- HY-P991176
-
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RO7443904
|
CD19
CD28
|
Cancer
|
|
RG-6333 is a bispecific agonist targeting CD19 and CD28. RG-6333 specifically recognizes and binds to the CD19 antigen on the surface of B-cell malignancies to locate tumor cells. RG-6333 activates T cells by binding to CD28, overcoming activation barriers to enhance anti-tumor immunity. RG-6333 can be used in the study of relapsed/refractory non-Hodgkin's lymphoma. The recommended isotype control is human IgG1 kappa, isotype control (HY-P99001) .
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-
-
- HY-10984A
-
|
(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 .
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-
-
- HY-174366
-
|
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c-Fms
PI3K
|
Cancer
|
|
JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity .
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-
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- HY-150638
-
|
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PI3K
Apoptosis
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Cancer
|
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PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research .
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-
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- HY-175541
-
|
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PROTACs
Btk
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Cancer
|
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TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .
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-
-
- HY-P991671
-
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JNJ-80948543
|
CD3
CD20
Transmembrane Glycoprotein
|
Cancer
|
|
Anafiltamig is a trivalent monoclonal antibody inhibitor targeting CD79B, CD3E and MS4A1. Anafiltamig consists of a humanized IgG1κ anti-CD79B arm and a bispecific scFv-based arm targeting CD3E and MS4A1. Anafiltamig simultaneously bridges T and B cells, activating T cells and specifically killing B cell tumors. Anafiltamig can be used for B cell malignancies such as non-Hodgkin lymphoma research .
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-
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- HY-153536
-
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PROTACs
Btk
|
Cancer
|
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PROTAC BTK Degrader-3 is a potent BTK degrader with a DC50 value of 10.9 nM of BTK degradation in Mino cells. PROTAC BTK Degrader-3 has the potential for B-cell malignancies, including chronic lymphoid malignancies research .
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-
-
- HY-168983
-
|
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Bcl-2 Family
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Cancer
|
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Lonitoclax is a B-cell lymphoma 2 (Bcl-2) inhibitor. Lonitoclax has comparable anti-tumor efficacy to Venetoclax (HY-15531) in both B cell and myeloid malignancy models. Lonitoclax is promising for research of relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas .
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-
-
- HY-P991542
-
|
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CD19
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Cancer
|
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GBR-401 is a humanized anti-CD19 monoclonal antibody with high affinity for FcγRIIIa. GBR-401 exerts a potent in vitro and in vivo cytotoxic activity against various B-cell malignancies. GBR-401 induces cell death by antibody dependent cellular cytotoxicity (ADCC) and direct killing effect. GBR-401 demonstrates potent activity of depleting malignant B cells and prolongs mice survival in multiple xenograft severe combined immunodeficiency (SCID) mice models .
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-
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- HY-178683
-
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Others
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Cancer
|
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ALV-05-077-01 is a BLC6/BLC6B degrader. ALV-05-077-01 depletes endogenous BCL6 levels in SuDHL4 cells (high BCL6 expression) and BCL6B levels in KYO1 cells (high BCL6B expression). ALV-05-077-01 can be used for the study of hematological malignancies .
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-
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- HY-178700
-
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Others
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Cancer
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ALV-05-151-02 is a BLC6/BLC6B degrader. ALV-05-151-02 depletes endogenous BCL6 levels in SuDHL4 cells (high BCL6 expression) and BCL6B levels in KYO1 cells (high BCL6B expression). ALV-05-151-02 can be used for the study of hematological malignancies .
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-
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- HY-P991562
-
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Transmembrane Glycoprotein
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Cancer
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MDX-1411 is a fully human monoclonal antibody targeting CD70. MDX-1411 is capable of inducing antibody-dependent cellular cytotoxicity (ADCC). MDX-1411 can be used in the research of B-cell malignancies .
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-
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- HY-109068A
-
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INCB050465 hydrochloride; IBI-376 hydrochloride
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PI3K
|
Cancer
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Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies .
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-
-
- HY-173499
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) .
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-
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- HY-158618
-
|
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Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia .
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-
-
- HY-175261
-
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CDK
Wee1
Checkpoint Kinase (Chk)
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Cancer
|
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DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies .
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-
-
- HY-176701
-
|
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Histone Methyltransferase
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Cancer
|
|
PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma .
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-
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- HY-176172
-
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Btk
|
Cancer
|
|
BTK-IN-44 (Compound 10) is a potent noncovalent inhibitor of Bruton’s tyrosine kinase (BTK) with an IC50 value of 24.7 nM. BTK-IN-44 interferes with signaling pathways of B cell malignancies, showing antitumor effects in lymphoma cells. BTK-IN-44 is promising for research of B cell malignancies (such as lymphoma) .
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-
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- HY-142648A
-
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MALT1
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Cancer
|
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(R)-MLT-985 is the R configuration of MLT-985 (HY-142648). MLT-985 is a selective allosteric and orally active MALT1 inhibitor with an IC50 value of 3 nM. MLT-985 can suppress cell growth and aberrant CARD11/BCL10/MALT1 complex signaling. MLT-985 can be used for the research of cancer, such as B cell malignancies .
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-
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- HY-109198A
-
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ME-401 hydrochloride; PWT-143 hydrochloride
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PI3K
Akt
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Cancer
|
|
Zandelisib (ME-401) hydrochloride is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib hydrochloride can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib hydrochloride can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma .
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-
-
- HY-149051
-
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Btk
|
Inflammation/Immunology
Cancer
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BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research .
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- HY-P5472
-
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Transmembrane Glycoprotein
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Others
|
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Tumour-associated MUC1 epitope is a biological active peptide. (This sequence is the hallmark of MUC1 mucin. MUC1 is a highly glycosylated type I transmembrane glycoprotein with a unique extracellular domain consisting of a variable number of tandem repeats (VNTR) of this 20 amino acid peptide. It is overexpressed on the cell surface of many human adenocarcinomas and hematological malignancies, including multiple myeloma and B-cell lymphoma, making MUC1 broadly applicable target for immunotherapeutic strategies.)
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-
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- HY-146789
-
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PI3K
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Cancer
|
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PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies .
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-
-
- HY-143472
-
|
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PI3K
Akt
Apoptosis
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Cancer
|
|
PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .
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-
-
- HY-P99911
-
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MEDI-6383
|
Orexin Receptor (OX Receptor)
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Inflammation/Immunology
Cancer
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|
Efizonerimod alfa (MEDI-6383) is a recombinant human OX40L IgG4P Fc fusion protein that assembles into a hexameric structure and exerts potent agonist activity upon binding to OX40. The activity of Efizonerimod alfa is enhanced by Fcγ receptor-mediated aggregation. Efizonerimod alfa binds to OX40 on the surface of activated T cells, induces NF-κB promoter activity in OX40-expressing T cells, and triggers the production of Th1-type cytokines, T cell proliferation, and resistance to regulatory T cell (Treg)-mediated suppression. Efizonerimod alfa enhances the cytolytic activity of tumor-reactive T cells and slows tumor growth in immunodeficient mice. Efizonerimod alfa induces the proliferation of CD4, CD8, and B cells in the peripheral blood of healthy non-human primates. Efizonerimod alfa can be used in the research of advanced solid malignancies and melanoma .
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-
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- HY-P991935
-
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Apoptosis
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Cancer
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ANT1034 is humanized anti-CD52 antibody. ANT1034 directs antibody dependent and complement dependent cell cytotoxicity, induces Apoptosis when cross-linked or in the presence of a cross-linking antibody. ANT1034 leads to increased survival in a SCID CD52 tumour xenograft model. ANT1034 can be used for the research of B cell malignancies .
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-
-
- HY-117499
-
-
-
- HY-P991912
-
-
-
- HY-182293
-
|
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Btk
Src
BMX Kinase
FLT3
Pim
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-48 is a BTK inhibitor with an IC50 of 1.14 μM. BTK-IN-48 inhibits recombinant BTK and c-Src, and exerts moderate inhibitory effects on LCK, BMX/ETK, FLT3 and PIM1. BTK-IN-48 can be used in the research of B-cell malignancies and autoimmune diseases .
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-
-
- HY-181050
-
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PROTACs
Src
Btk
Apoptosis
|
Cancer
|
|
DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor (HY-15805), inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies .
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-
-
- HY-160167A
-
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(R,R)-DZD8586
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Btk
|
Cancer
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(R,R)-Birelentinib ((R,R)-DZD8586) (Compound 14) is a potent BTK inhibitor with IC50 values for BTK WT and BTK C481S of 0.7 and 0.86 nM, respectively. (R,R)-Birelentinib inhibits the self-phosphorylation of BTK and its IC50 is 24.3 nM. (R,R)-Birelentinib exhibits significant anti-proliferative activity against wild-type and C481S mutant HEK293 cells. (R,R)-Birelentinib can be used for the study of drug-resistant B-cell malignancies .
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-
-
- HY-109068R
-
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INCB050465 (Standard); IBI-376 (Standard)
|
Reference Standards
PI3K
|
Cancer
|
|
Parsaclisib (Standard) is the analytical standard of Parsaclisib (HY-109068). This product is intended for research and analytical applications. Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies .
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-
- HY-109068AR
-
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INCB050465 hydrochloride (Standard); IBI-376 hydrochloride (Standard)
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Reference Standards
PI3K
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Cancer
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Parsaclisib hydrochloride (Standard) is the analytical standard of Parsaclisib (hydrochloride) (HY-109068A). This product is intended for research and analytical applications. Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies .
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- HY-103019BR
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(R)-Enitociclib (Standard); (-)-BAY-1251152 (Standard); (-)-VIP152 (Standard)
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Reference Standards
Drug Isomer
CDK
Apoptosis
DNA/RNA Synthesis
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Cancer
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(-)-Enitociclib (Standard) is the analytical standard of (-)-Enitociclib (HY-103019B). This product is intended for research and analytical applications. (-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
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- HY-125585
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Syk
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Others
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Syk-IN-2 (Page 78; 35) is a spleen tyrosine kinase (Syk) inhibitor .
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- HY-103019R
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(+)-BAY-1251152 (Standard); (+)-VIP152 (Standard); (S)-Enitociclib (Standard)
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Reference Standards
Drug Isomer
Apoptosis
DNA/RNA Synthesis
CDK
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Cancer
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Enitociclib (Standard) is the analytical standard of Enitociclib (HY-103019). This product is intended for research and analytical applications. Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC50=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma .
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- HY-P991924
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P5472
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Transmembrane Glycoprotein
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Others
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Tumour-associated MUC1 epitope is a biological active peptide. (This sequence is the hallmark of MUC1 mucin. MUC1 is a highly glycosylated type I transmembrane glycoprotein with a unique extracellular domain consisting of a variable number of tandem repeats (VNTR) of this 20 amino acid peptide. It is overexpressed on the cell surface of many human adenocarcinomas and hematological malignancies, including multiple myeloma and B-cell lymphoma, making MUC1 broadly applicable target for immunotherapeutic strategies.)
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P990033
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CC-95251; BMS-986351
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CD47
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Cancer
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Anzurstobart is a CD47/SIRPα inhibitor with human SIRPα Kd of 0.0541 nM and human SIRPα IC50 of 100 nM. Anzurstobart binds SIRPα at a CD47-overlapping site, blocks CD47-SIRPα interactions, inhibits CD47-SIRPα axis signaling, and binds across 6 prevalent human SIRPα haplotypes. Anzurstobart binds SIRPγ and inhibits CD47-SIRPγ interactions. Anzurstobart can be used for the research of non-Hodgkin's lymphoma, colorectal cancer, squamous cell carcinoma of the head and neck, diffuse large B-cell lymphoma, and advanced solid and hematologic malignancies .
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(5)
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- HY-P991176
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RO7443904
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CD19
CD28
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Cancer
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RG-6333 is a bispecific agonist targeting CD19 and CD28. RG-6333 specifically recognizes and binds to the CD19 antigen on the surface of B-cell malignancies to locate tumor cells. RG-6333 activates T cells by binding to CD28, overcoming activation barriers to enhance anti-tumor immunity. RG-6333 can be used in the study of relapsed/refractory non-Hodgkin's lymphoma. The recommended isotype control is human IgG1 kappa, isotype control (HY-P99001) .
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(5)
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- HY-P991671
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JNJ-80948543
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CD3
CD20
Transmembrane Glycoprotein
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Cancer
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Anafiltamig is a trivalent monoclonal antibody inhibitor targeting CD79B, CD3E and MS4A1. Anafiltamig consists of a humanized IgG1κ anti-CD79B arm and a bispecific scFv-based arm targeting CD3E and MS4A1. Anafiltamig simultaneously bridges T and B cells, activating T cells and specifically killing B cell tumors. Anafiltamig can be used for B cell malignancies such as non-Hodgkin lymphoma research .
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(5)
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- HY-P991542
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CD19
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Cancer
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GBR-401 is a humanized anti-CD19 monoclonal antibody with high affinity for FcγRIIIa. GBR-401 exerts a potent in vitro and in vivo cytotoxic activity against various B-cell malignancies. GBR-401 induces cell death by antibody dependent cellular cytotoxicity (ADCC) and direct killing effect. GBR-401 demonstrates potent activity of depleting malignant B cells and prolongs mice survival in multiple xenograft severe combined immunodeficiency (SCID) mice models .
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(5)
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- HY-P991562
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Transmembrane Glycoprotein
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Cancer
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MDX-1411 is a fully human monoclonal antibody targeting CD70. MDX-1411 is capable of inducing antibody-dependent cellular cytotoxicity (ADCC). MDX-1411 can be used in the research of B-cell malignancies .
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(5)
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- HY-P99911
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MEDI-6383
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Orexin Receptor (OX Receptor)
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Inflammation/Immunology
Cancer
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Efizonerimod alfa (MEDI-6383) is a recombinant human OX40L IgG4P Fc fusion protein that assembles into a hexameric structure and exerts potent agonist activity upon binding to OX40. The activity of Efizonerimod alfa is enhanced by Fcγ receptor-mediated aggregation. Efizonerimod alfa binds to OX40 on the surface of activated T cells, induces NF-κB promoter activity in OX40-expressing T cells, and triggers the production of Th1-type cytokines, T cell proliferation, and resistance to regulatory T cell (Treg)-mediated suppression. Efizonerimod alfa enhances the cytolytic activity of tumor-reactive T cells and slows tumor growth in immunodeficient mice. Efizonerimod alfa induces the proliferation of CD4, CD8, and B cells in the peripheral blood of healthy non-human primates. Efizonerimod alfa can be used in the research of advanced solid malignancies and melanoma .
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(5)
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- HY-P991935
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Apoptosis
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Cancer
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ANT1034 is humanized anti-CD52 antibody. ANT1034 directs antibody dependent and complement dependent cell cytotoxicity, induces Apoptosis when cross-linked or in the presence of a cross-linking antibody. ANT1034 leads to increased survival in a SCID CD52 tumour xenograft model. ANT1034 can be used for the research of B cell malignancies .
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(5)
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- HY-P991912
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(5)
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- HY-P991924
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(5)
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-15582S
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Auristatin E-d8 is the deuterium labeled Auristatin E (HY-15582). Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
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