BI1071
Based on 1 Customer Validation
BI1071 is an orally active Nur77-Bcl-2 apoptotic pathway modulator. BI1071 can bind to Nur77-LBD protein with a Kd of 0.17 μM. BI1071 can activate Nur77 signaling and induce apoptosis by translocating to mitochondria where it interacts with Bcl-2. BI1071 can inhibit tumor growth in SW620 xenograft mice model. BI1071 can be used for research of colon cancer.
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- Pureza : 98.93%
- Fòrmula: C25H19F3N2O3S
- Peso molecular:484.49
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Ver todos los productos específicos de isoformas Nuclear Hormone Receptor 4A/NR4A
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Nur77/NR4A1 |
Bcl-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-549 | IC50 |
0.17 μM
Compound: BI1071; 8n
|
Cytotoxicity against human BT-549 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Cytotoxicity against human BT-549 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
|
[PMID: 33279290] |
| HCT-116 | IC50 |
0.27 μM
Compound: BI1071; 8n
|
Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
|
[PMID: 33279290] |
| MCF-10A | IC50 |
4.29 μM
Compound: BI1071; 8n
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Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
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[PMID: 33279290] |
| MDA-MB-231 | IC50 |
0.22 μM
Compound: BI1071; 8n
|
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
|
[PMID: 33279290] |
| NCM460 | IC50 |
6.84 μM
Compound: BI1071; 8n
|
Cytotoxicity against human NCM460 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Cytotoxicity against human NCM460 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
|
[PMID: 33279290] |
| SW-620 | IC50 |
0.18 μM
Compound: BI1071; 8n
|
Cytotoxicity against human SW-620 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Cytotoxicity against human SW-620 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
|
[PMID: 33279290] |
Chemical Information
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Appearance Solid
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Peso molecular 484.49
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Fòrmula C25H19F3N2O3S
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Color Orange to red
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SMILES
FC(C1=CC=C([C+](C2=CNC3=C2C=CC=C3)C4=CNC5=C4C=CC=C5)C=C1)(F)F.CS(=O)([O-])=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (206.40 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
Protocolo
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Detection of 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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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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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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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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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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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.
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
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 (sealed storage, away from moisture and light). 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 | 2.0640 mL | 10.3201 mL | 20.6403 mL | 51.6007 mL |
| 5 mM | 0.4128 mL | 2.0640 mL | 4.1281 mL | 10.3201 mL | |
| 10 mM | 0.2064 mL | 1.0320 mL | 2.0640 mL | 5.1601 mL | |
| 15 mM | 0.1376 mL | 0.6880 mL | 1.3760 mL | 3.4400 mL | |
| 20 mM | 0.1032 mL | 0.5160 mL | 1.0320 mL | 2.5800 mL | |
| 25 mM | 0.0826 mL | 0.4128 mL | 0.8256 mL | 2.0640 mL | |
| 30 mM | 0.0688 mL | 0.3440 mL | 0.6880 mL | 1.7200 mL | |
| 40 mM | 0.0516 mL | 0.2580 mL | 0.5160 mL | 1.2900 mL | |
| 50 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 1.0320 mL | |
| 60 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8600 mL | |
| 80 mM | 0.0258 mL | 0.1290 mL | 0.2580 mL | 0.6450 mL | |
| 100 mM | 0.0206 mL | 0.1032 mL | 0.2064 mL | 0.5160 mL |