NGI-189
Based on 1 Customer Validation
NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer.
For research use only. We do not sell to patients.
- Purity : 99.29%
- CAS No.: 2763063-26-7
- Formula: C22H30N4O4S2
- Molecular Weight:478.63
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Akt |
EGFRL858R/T790M |
EGFR |
Bim |
In Vitro
NGI-189 (0.09 μM) potently inhibits N-glycosylation in ER-LucT reporter cells with an IC50 of 0.09 μM[1].
NGI-189 (5 μM; 5 days) inhibits proliferation of parental PC9 EGFR mutant NSCLC cells by ~70%, with significant rescue observed in PC9-CD8-EGFR-CL cells that express N-glycosylation-independent EGFR[1].
NGI-189 (0-25 μM; 24 h) preferentially inhibits the OST-A complex in HEK293 wild-type, STT3A KO, and STT3B KO cells, reducing N-glycosylation of EGFR and Halo3N in a dose-dependent manner, with complete inhibition of OST-A-dependent glycosylation achievable only in STT3B KO cells[1].
NGI-189 (10 μM; 24 h) reduces N-glycosylation of bypass PTK7, MET and inhibits downstream STAT3 signaling in Osimertinib (HY-15772)-resistant H1975-OR and Gefitinib (HY-50895)-resistant HCC827-GR NSCLC cells[1].
NGI‑189 (5 μM) reduces clonogenic survival of parental PC9 EGFR‑mutant NSCLC cells and shows significant rescue in PC9‑CD8‑EGFR‑CL cells expressing N‑glycosylation‑independent EGFR; it also significantly decreases clonogenic survival of H3255, HCC‑4006, and HCC‑2935 EGFR‑mutant NSCLC cells[1].
NGI-189 (5 μM; 24 h) inhibits EGFR and downstream AKT/p70S6K/S6RP signaling, and induces pro-apoptotic Bim protein expression in H3255, HCC-4006, and HCC-2935 EGFR mutant NSCLC cells[1].
NGI-189 (5 μM; 24 h) induces G1 phase cell cycle arrest in PC9 EGFR-mutant NSCLC cells, and triggers G1 arrest accompanied by marked cell death (sub-G1 population) in H3255 and HCC-2935 EGFR-mutant NSCLC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK293 wild-type, STT3A knockout (KO), and STT3B KO cells expressing Halo3N glycoprotein
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Concentration:0 μM, 0.1 μM, 1 μM, 5 μM, 10 μM, 25 μM
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Incubation Time:24 h
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Result:Reduced the molecular weight of EGFR and Halo3N in wild-type HEK293 cells at all tested concentrations, indicating reduced N-glycosylation.
Showed weaker inhibition of N-glycosylation in STT3A KO cells, while showed potent inhibition in STT3B KO cells, demonstrating preferential activity against the OST-A (STT3A-containing) complex.
Achieved complete inhibition of OST-A dependent N-glycosylation in STT3B KO cells at doses >10 μM, but could not achieve complete N-glycosylation inhibition in wild-type cells due to OST catalytic subunit redundancy.
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Cell Line:Parental PC9 EGFR mutant non-small cell lung cancer (NSCLC) cells, PC9-CD8-EGFR-CL (N-glycosylation-independent EGFR) cells
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Concentration:5 μM
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Incubation Time:5 days
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Result:Reduced proliferation of parental PC9 cells by approximately 70%.
Showed significantly rescued proliferation of PC9-CD8-EGFR-CL cells relative to parental cells, confirming the anti-proliferative effect is mediated via inhibition of EGFR N-glycosylation.
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Cell Line:PC9 EGFR mutant NSCLC cells
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Concentration:1 μM, 5 μM
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Incubation Time:24 h
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Result:Caused dose-dependent inhibition of EGFR Y1068 phosphorylation, accompanied by reduced phosphorylation of AKT S473, p70 S6K T389, and S6RP S235-236.
Induced increased levels of the pro-apoptotic protein Bim at both tested concentrations.
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Cell Line:PC9 EGFR mutant NSCLC cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Induced a greater accumulation of PC9 cells in the G1 phase of the cell cycle compared to vehicle control, indicating G1 cell cycle arrest.
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Cell Line:H3255 (EGFR L858R), HCC-4006 (EGFR del747-749, A750P), and HCC-2935 (EGFR del746-751, S752I) EGFR mutant NSCLC cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Inhibited EGFR Y1068 phosphorylation, reduced phosphorylation of AKT S473, p70 S6K T389, and S6RP S235-236, and induced increased levels of Bim in all three EGFR mutant NSCLC cell lines.
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Cell Line:H3255 and HCC-2935 EGFR mutant NSCLC cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Induced a modest increase in G1 cell cycle arrest and a significant increase in the sub-G1 populationl, indicating induction of cell death.
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Cell Line:H1975-OR (osimertinib-resistant, EGFR L858R/T790M) and HCC827-GR (gefitinib-resistant, EGFR del19/MET-amplified) NSCLC cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Reduced PTK7 N-glycosylation and inhibited STAT3 Y705 phosphorylation in H1975-OR cells.
Reduced PTK7 and MET N-glycosylation and inhibited STAT3 Y705 phosphorylation in HCC827-GR cells.
In Vivo
NGI-189 (10 mg/kg; i.p.; every other day) induces significant tumor regression in osimertinib-resistant H1975-OR NSCLC xenografts[1].
NGI-189 (10 mg/kg; i.p.; every other day; 3 total doses) is well tolerated in mice, with no significant toxicity detected in blood work or organ histopathology[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female, 6-8 weeks old, immunodeficient)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; 8 total doses
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Result:Kept tumor volume at 193 mm3 by Day 8, while vehicle-treated tumors grew to 450 mm3.
Doubled the time for tumors to reach 500 mm3.
Reduced EGFR protein levels in tumors.
Showed weight changes similar to vehicle-treated mice.\nKept tumor volume at 167 mm3 by Day 12, while vehicle-treated tumors grew to 414 mm3.
Doubled the time for tumors to reach 500 mm3.
Showed significantly higher body weight at the end of treatment compared to vehicle controls.
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Animal Model:athymic Swiss nu/nu mice (female, 6-8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day
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Result:Induced significant tumor regression.
Achieved 60% of treated mice remaining progression-free at Day 90, compared to 0% of vehicle-treated mice.
Showed weight changes similar to vehicle-treated mice.
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Animal Model:athymic Swiss nu/nu mice (female, 6-8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; 8 total doses
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Result:Limited tumor volume to 400 mm3 by Day 20.
Prolonged the time for tumors to reach 500 mm3.
Showed weight changes similar to vehicle-treated mice.
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Animal Model:athymic Swiss nu/nu mice (female, 6-8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; 3 total doses
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Result:Showed no significant differences from vehicle-treated mice in blood counts, serum chemistries, or organ cytopathology.
Had only minor age-related abnormalities, same as vehicle group.
Chemical Information
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CAS No. 2763063-26-7
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Appearance Solid
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Molecular Weight 478.63
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Formula C22H30N4O4S2
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Color White to off-white
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SMILES
O=C(C1=CC(S(=O)(N2CCOCC2)=O)=CC=C1N(C3CCCC3)C)NC4=NC=C(CC)S4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (208.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
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Data Sheet (290 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0893 mL | 10.4465 mL | 20.8930 mL | 52.2324 mL |
| 5 mM | 0.4179 mL | 2.0893 mL | 4.1786 mL | 10.4465 mL | |
| 10 mM | 0.2089 mL | 1.0446 mL | 2.0893 mL | 5.2232 mL | |
| 15 mM | 0.1393 mL | 0.6964 mL | 1.3929 mL | 3.4822 mL | |
| 20 mM | 0.1045 mL | 0.5223 mL | 1.0446 mL | 2.6116 mL | |
| 25 mM | 0.0836 mL | 0.4179 mL | 0.8357 mL | 2.0893 mL | |
| 30 mM | 0.0696 mL | 0.3482 mL | 0.6964 mL | 1.7411 mL | |
| 40 mM | 0.0522 mL | 0.2612 mL | 0.5223 mL | 1.3058 mL | |
| 50 mM | 0.0418 mL | 0.2089 mL | 0.4179 mL | 1.0446 mL | |
| 60 mM | 0.0348 mL | 0.1741 mL | 0.3482 mL | 0.8705 mL | |
| 80 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6529 mL | |
| 100 mM | 0.0209 mL | 0.1045 mL | 0.2089 mL | 0.5223 mL |