NS-0011
NS-0011 is a CDK5 inhibitor with a Kd value of 16 μM. NS-0011 binds to the nuclear export signal domain of CDK5, disrupts its interaction with CRM-1 and increases the accumulation of CDK5 in the nucleus. NS-0011 inhibits the proliferation of gastric cancer cells. NS-0011 suppresses the occurrence of gastric cancer xenograft tumors. NS-0011 is applicable to gastric cancer-related research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1076234-33-7
- 分子式: C12H9ClF3N3O2
- 分子量:319.67
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
CDK5 16 μM (Kd) |
体外実験
NS-0011 binds directly to purified recombinant CDK5 protein with a binding constant of 16 μmol/L[1].
NS-0011 (1-2 μmol/L; 24-80 h) accumulates CDK5 in the nucleus and completely inhibits proliferation of MGC-803 human gastric cancer cells at 2 μmol/L, an effect dependent on CDK5 expression[1].
NS-0011 (2 μmol/L; 48 h) specifically upregulates p16 expression in MGC-803 and SGC-7901 human gastric cancer cells at 2 μmol/L for 48 hours[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:human gastric cancer MGC-803 cells
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Concentration:1-2 μmol/L (immunofluorescence; proliferation; proliferation with CDK5 siRNA)
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Incubation Time:24 h (immunofluorescence); up to 80 h (proliferation); up to 72 h (proliferation with CDK5 siRNA)
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Result:Caused clear accumulation of CDK5 in the nucleus of MGC-803 cells at 2 μmol/L for 24 h.
Inhibited MGC-803 cell proliferation in a dose-dependent manner: completely inhibited cell growth at 2 μmol/L over 80 h, while caused partial inhibition at 1 μmol/L.
Saw its antiproliferative effect largely reversed when CDK5 was depleted by siRNA.
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Cell Line:human gastric cancer MGC-803 and SGC-7901 cells
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Concentration:2 μmol/L
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Incubation Time:48 h
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Result:Significantly increased p16 protein levels in both MGC-803 and SGC-7901 cells.
Had no effect on the levels of p21, p27, or p57.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (6-week-old male, immunocompromised, subcutaneous xenograft model via MGC-803 gastric cancer cell injection)[1]
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Dosage:2 μmol/L (pretreatment of cells); 4 μmol/L (in cell suspension for injection)
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Administration:in vitro pretreatment (48 hours); in-cell suspension injection
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Result:Significantly suppressed xenograft tumorigenesis, resulting in reduced maximum tumor diameter and reduced tumor weight compared to DMSO controls.
化学情報
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CAS 番号 1076234-33-7
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分子量 319.67
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分子式 C12H9ClF3N3O2
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SMILES
O=C1C(C)=C(C)C(N1NC2=NC(Cl)=C(C(F)(F)F)C=C2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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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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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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)