NHL

PNU-159682, a metabolite of anthracycline nemorubicin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.

NHLP-002 (BP Lipid 218) is an ionizable liposome that can be used to make nanoparticles, often in the form of nanoparticles to deliver mRNA drugs.

Hydrotecan-NH-L-Ala-L-Val-L-Gln(CO-C5-succinimide)-D-glucitol (Example 9) is a conjugate comprising an ADC toxic molecule and a linker. The toxic molecule portion is Hydrotecan, while the linker portion consists of Mc-Glu(D-Glucamine)-val-ala.

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

ARV-393 is a PROTAC degrader targeting BCL6 with the advantage of being highly potent and orally available.ARV-393 recruits BCL6 and E3 ligase cerebellum to rapidly degrade BCL6 through the cell's natural ubiquitin proteasome system for the treatment of diffuse large b-cell lymphoma (DLBCL) and non-Hodgkin's lymphoma (NHL).

DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]

PRMT5-IN-48 (compound D3) is an orally active PRMT5 inhibitor with an IC50 of 20.7 nM, displaying antitumor activity. It effectively suppresses the growth of various cancer cells, induces apoptosis, and causes cell cycle arrest at the G0/G1 phase. PRMT5-IN-48 is applicable for research in non-Hodgkin's lymphoma (NHL).

PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active dual inhibitor of PI3Kδ and HDAC6, with IC50 values of 2.4 nM and 6.2 nM, respectively. It exhibits potent antiproliferative effects against non-Hodgkin's lymphoma (NHL) cells and demonstrates antitumor activity in vivo without significant toxicity. PI3Kδ/HDAC6-IN-1 induces cell cycle arrest at the G0/G1 phase and triggers apoptosis. Additionally, it inhibits the PI3K/AKT/mTOR signaling pathway and enhances the acetylation levels of α-tubulin and histone H3.

SB-743921, a kinesin spindle protein (KSP) inhibitor, is used potentially for the treatment of non-Hodgkin's lymphoma (NHL).

WNY1613 is a potent and selective PI3Kδ inhibitor with a piperazinone-containing purine scaffold, exhibiting anti-NHL effects both in vitro and in vivo by inhibiting phosphorylation of downstream components of PI3K in NHL cell lines and inducing apoptosis in cancer cells.

MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway.

LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor). LGB321 is unique relative to previously described PIM inhibitors, in that it is active in PIM2 dependent cell lines. , a kinase that has proven difficult to inhibit in the cellular context. Consistent with its activity on all three PIM kinases, LGB321 inhibits proliferation of a number of cell lines derived from diverse hematological malignancies, including MM, AML, CML and B-Cell NHL. In vivo, LGB-321 is orally available, demonstrates efficacy in tumor xenografts and is well-tolerated within the therapeutic exposure range in mice. (source: Clin Cancer Res. 2014 Apr 1;20(7):1834-45 )

Mosunetuzumab (BCT-4465A) is a humanized antibody based on immunoglobulin G1 that targets CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used to study relapsed or refractory (R/R) B-cell non-Hodgkin lymphoma (B-NHL) and refractory follicular lymphoma.

Veltuzumab (IMMU-106) is a humanized anti-CD20 monoclonal antibody that displays anti-proliferative, apoptotic, and antibody-dependent cytotoxic effects in vitro and inhibits tumor growth in mice harboring human lymphomas, and is indicated for use in non-Hodgkin's lymphoma (NHL).

Pinatuzumab is a humanised monoclonal antibody targeting CD22, commonly used to synthesise the ADC molecule Pinatuzumab vedotin, which is employed in the study of B-cell malignancies such as non-Hodgkin lymphoma (NHL) and chronic lymphocytic leukaemia (CLL).

Ulocuplumab (BMS-936564) is a fully human anti-CXCR4 IgG4 antibody.Ulocplumab exhibits antitumor activity in acute myeloid leukemia (AML), non-Hodgkin's lymphoma (NHL), and multiple myeloma transplantation models.Ulocplumab inhibits the migration of chronic lymphocytic leukemia (CLL) cells under CXCR4 activation, induces apoptosis, and inhibits the growth and migration of cancer cells. Ulocplumab inhibits CXCL12-mediated chronic lymphocytic leukemia (CLL) cell migration in response to CXCR4 activation and induces apoptosis.)

Galiximab (IDEC 114) is a primate-type anti-CD80 immunoglobulin G1 (IgG1)-like monoclonal antibody with antitumor activity that induces in vivo growth inhibition and prolongs survival of B-NHL tumor xenografts. Galiximab has been used in the study of hematologic malignancies.

Bectumomab (IMMU-LL 2), a humanized IgG2a monoclonal antibody (mAb) against human CD22 (antigen), serves as an anti-lymphoma agent. It is utilized in imaging procedures when combined with technetium 99 (Tc99m LL2 Fab), and employed in evaluating the staging of recurrent or newly diagnosed non-Hodgkin's lymphoma (NHL). Additionally, Bectumomab is used to examine targeting efficacy prior to radioimmunotherapy (RIT) [1].

Zuberitamab (HS-20090) is a humanized IgG1 monoclonal antibody targeting CD20. The compound specifically binds to CD20 on the surface of B cells, facilitating the depletion of malignant B cells through antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC), and the direct induction of apoptosis. In experimental studies, Zuberitamab serves as a potent tool for B-cell depletion to investigate hematological malignancies such as Non-Hodgkin Lymphoma (NHL).

Imvotamab (IGM-2323), a CD20xCD3 bispecific IGM antibody featuring a dual-action mechanism, promotes physiological T cell activation to avoid both over-stimulation and immune function down-regulation. This compound is under development for addressing B-cell malignant tumors, including multiple myeloma (MM) and non-Hodgkin's lymphoma (NHL) [1] [2] [3] [4].

Loncastuximab (RB4v1.2) is a monoclonal antibody inhibitor targeting CD19 with antitumor activity. It is used in research on non-Hodgkin lymphoma (NHL) and diffuse large B-cell lymphoma (DLBCL), and for synthesizing ADC molecules such as Loncastuximab tesirine.

Iladatuzumab (MCDS0593A) is a monoclonal antibody targeting CD79B and is a naked antibody to the ADC compound Iladatuzumab vedotin, which has potential anticancer activity for the study of B-cell non-Hodgkin's lymphoma (B-NHL).

Detumomab, a mouse monoclonal antibody, targets human B-cell lymphoma and is utilized in research on various cancers, including non-Hodgkin's lymphoma (NHL).

Anti-Siglec-2/CD22 Antibody (NCI m972) is a fully humanized monoclonal antibody targeting Siglec-2 (CD22). Identified via phage display technology, this product binds specifically to Ig-like domains 5 to 7 of CD22 with an apparent affinity of approximately 15 nM. As CD22 is a specific surface marker for B-cell malignancies (e.g., ALL, NHL), NCI m972 offers low immunogenicity and is widely used for researching the development of antibody-drug conjugates (ADCs), chimeric antigen receptor T-cells (CAR-T), and targeted imaging agents.