In Vitro Efficacy Testing Services for Multiple Myeloma

We provide robust and sensitive in vitro screening and characterization platforms for accelerating the discovery and screening of potential therapies for Multiple Myeloma. Our services enable comprehensive evaluation of candidate compounds targeting key proteins and signaling pathways implicated in myeloma, such as CD38, BCMA, and the proteasome pathway. We offer assays to assess cellular proliferation, apoptosis, cytokine production, and drug resistance mechanisms unique to the pathogenesis of Multiple Myeloma. These platforms support rapid assessment of therapeutic efficacy and mechanism of action in disease-relevant cellular models.

Our in vitro services utilize a diverse array of biochemical and cell-based assays, including luminescent, fluorescence, binding, and flow cytometry-based approaches. These methods are designed to characterize compound activity, target engagement, and molecular interactions relevant to Multiple Myeloma. Collectively, our assays provide reliable and quantitative data to guide preclinical drug development.

Arrestin protease recruitment assay: Measures the recruitment of arrestin proteins to activated receptors, providing insights into receptor signaling and potential drug efficacy.

Chemiluminescent assay: Detects biological events or molecular interactions through light emission, allowing sensitive quantification of analytes.

Competitive binding assay: Evaluates the ability of test compounds to compete with labeled ligands for binding to target proteins, important for assessing binding affinity and selectivity.

Displacement of 12G5 mAb: Assesses the ability of compounds to displace the 12G5 monoclonal antibody from its target, indicative of specific target engagement.

Displacement of 1D9 mAb: Measures the competitive displacement of the 1D9 monoclonal antibody, useful for evaluating compound-target interactions.

Displacement of 2B11 mAb: Detects the capability of compounds to inhibit binding of the 2B11 monoclonal antibody, reflecting their affinity and specificity.

Displacement of 44717 mAb: Determines the effectiveness of test agents in displacing the 44717 monoclonal antibody from its antigen, supporting epitope mapping and target validation.

ELISA assay: Utilizes enzyme-linked immunosorbent detection for quantifying proteins, antibodies, or cytokines in samples, supporting biomarker analysis and pharmacodynamic studies.

Flow cytometry assay: Enables multi-parameter analysis of cell surface markers, apoptosis, and cell cycle status in heterogeneous cell populations, essential for assessing therapeutic impact.

Fluorescence resonance energy transfer (FRET) assay: Monitors molecular interactions and conformational changes by measuring energy transfer between fluorescent probes.

Fluorescent assay: Employs fluorescent dyes or tags to detect cellular events or molecular binding, offering high sensitivity and throughput.

Fluorescent polarization assay: Measures changes in fluorescence polarization to quantify binding interactions, useful for studying small molecule-target engagement.

Homogeneous Time Resolved Fluorescence (HTRF) assay: Combines time-resolved fluorescence with homogeneous assay formats for sensitive detection of molecular interactions.

Luciferine/luciferase assay: Utilizes bioluminescent enzyme-substrate reactions to measure cellular viability, proliferation, or reporter gene activity.

RNA assay: Quantifies gene expression changes in response to treatment, supporting mechanistic and pathway analysis.

Succinyl-Leu-Leu-Val-Tyr-7-amino-4-methylcoumarin as substrate: Provides a fluorogenic substrate for protease activity assays, enabling measurement of proteasome or other protease functions relevant to Multiple Myeloma.

Our assays quantify key pharmacological parameters such as potency, efficacy, and target affinity, which are critical for ranking and optimizing lead compounds. These parameters, including EC-50, IC-50, Kd, Ki, MEC, and MIC, provide a comprehensive understanding of compound activity and selectivity. Accurate measurement of these metrics accelerates decision-making in the drug development process.

EC-50: The concentration of a compound that produces 50% of its maximal effect, indicating compound potency.

IC-50: The concentration of an inhibitor where the response (or binding) is reduced by half, widely used to assess inhibitory activity.

Kd: The equilibrium dissociation constant, reflecting the affinity between a ligand and its target protein; lower values indicate higher affinity.

Ki: The inhibition constant, representing the binding affinity of an inhibitor for its target, essential for comparing inhibitor strengths.

MEC: Minimum effective concentration, the lowest concentration at which a compound elicits a desired biological effect.

MIC: Minimum inhibitory concentration, the lowest concentration of a drug required to inhibit visible growth of a target organism or cell.

Recommended In Vitro Efficacy Tests

C-X-C Motif Chemokine Receptor 4

C-X-C Motif Chemokine Receptor 4 (CXCR4) drives multiple myeloma progression and drug resistance by mediating tumor cell migration and microenvironment interactions. Our CXCR4 testing service aids drug development by evaluating compound efficacy and receptor engagement using assays including flow cytometry, competitive binding, FRET, fluorescent assays, and mAb displacement (44717, 1D9, 2B11, 12G5), as well as arrestin recruitment and HTRF. Key parameters measured include IC50, Ki, and MIC.

Caspase 3

Our Caspase 3 testing service supports Multiple Myeloma drug development by quantifying apoptosis via a sensitive chemiluminescent assay. Caspase 3 is a crucial executioner enzyme in apoptosis, and its activation indicates therapeutic efficacy in Multiple Myeloma cells. This assay measures Caspase 3 activity and determines the Minimum Inhibitory Concentration (MIC) of candidate compounds, providing essential data for evaluating anti-myeloma drug potency and optimizing candidate selection.

Cereblon

Cereblon plays a key role in the mechanism of action of immunomodulatory drugs in Multiple Myeloma. Testing Cereblon binding is crucial for drug development and efficacy prediction. Our service offers high-sensitivity assays—fluorescent polarization, HTRF, and FRET—to assess compound-Cereblon interactions. Main parameters measured include IC-50, indicating inhibitory potency, and Kd, reflecting binding affinity, enabling robust evaluation of potential therapeutics.

Exportin 1

Exportin 1 (XPO1) mediates nuclear export of tumor suppressors and is often overexpressed in Multiple Myeloma, promoting malignancy. Exportin 1 testing is crucial for identifying and optimizing XPO1-targeted therapies. Our service employs chemiluminescent and RNA assays to quantitatively assess XPO1 activity and drug efficacy. The primary parameter measured is the Minimum Effective Concentration (MEC), enabling precise evaluation of candidate compounds for drug development.

G Protein-Coupled Receptor Class C Group 5 Member D

G Protein-Coupled Receptor Class C Group 5 Member D (GPRC5D) is a promising therapeutic target in Multiple Myeloma due to its selective expression on malignant plasma cells. Our testing service utilizes flow cytometry assays to evaluate drug candidates targeting GPRC5D, measuring key parameters such as IC-50 (half-maximal inhibitory concentration) and Kd (binding affinity). This enables precise assessment of drug efficacy and binding, supporting informed decision-making in Multiple Myeloma drug development.

Ikaros Family Zinc Finger 3

The Ikaros Family Zinc Finger 3 (IKZF3) plays a critical role in regulating gene expression in Multiple Myeloma. Testing IKZF3 activity is essential for evaluating the efficacy of novel therapeutics targeting this pathway. Utilizing luciferin/luciferase and chemiluminescent assays, this service quantifies IKZF3 activity and determines drug potency by calculating EC-50 values, providing key data for drug development and candidate optimization in Multiple Myeloma research.

Nuclear Receptor Subfamily 3 Group C Member 1

Nuclear Receptor Subfamily 3 Group C Member 1 (NR3C1), encoding the glucocorticoid receptor, modulates cell survival in Multiple Myeloma. Testing NR3C1 expression via RNA assays is crucial for evaluating drug efficacy and resistance mechanisms. Key parameters measured include EC-50 (half-maximal effective concentration) and MEC (minimum effective concentration), guiding dose optimization and therapeutic strategy development in Multiple Myeloma drug discovery.

Proteasome 20S Subunit Beta 5

Proteasome 20S Subunit Beta 5 is crucial in protein degradation and is a primary target in Multiple Myeloma therapy. Testing its activity helps evaluate drug efficacy and resistance. Using Succinyl-Leu-Leu-Val-Tyr-7-amino-4-methylcoumarin as a substrate, this assay quantifies proteasome inhibition, with IC50 as the main parameter to determine compound potency, supporting effective Multiple Myeloma drug development.

Tumor Necrosis Factor

Tumor Necrosis Factor (TNF) is a key mediator in Multiple Myeloma progression and drug response. Our TNF testing service employs ELISA and RNA assays to quantify TNF protein and gene expression, aiding in efficacy evaluation. Critical parameters measured include IC-50 (drug concentration for 50% inhibition) and MIC (minimum inhibitory concentration), providing essential data for optimizing drug candidates targeting TNF in Multiple Myeloma therapy development.