Sulofenur
Sulofenur (LY186641) is an orally active anti-tumor agent. Sulofenur induces gene expression through calcium ion-dependent pathways and some protein kinase-independent pathways, and its effect is particularly enhanced in H-ras mutant cells. Sulofenur exhibits significant activity in mouse solid tumor models and human tumor xenograft models.
For research use only. We do not sell to patients.
- CAS No.: 110311-27-8
- Formula: C16H15ClN2O3S
- Molecular Weight:350.82
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Calcium Channel Isoforms
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>20 μM
Compound: Sulofenur
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Anticancer activity against human A549 cells by MTT assay
Anticancer activity against human A549 cells by MTT assay
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[PMID: 21570750] |
| A549 | IC50 |
11.34 μM
Compound: LY-186641
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In vitro cytotoxic activity against human lung carcinoma A549 cell line
In vitro cytotoxic activity against human lung carcinoma A549 cell line
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10.1016/0960-894X(96)00463-5 |
| A549 | IC50 |
36.43 μM
Compound: 2
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Cytotoxicity against human lung carcinoma A549 cell line using MTT assay
Cytotoxicity against human lung carcinoma A549 cell line using MTT assay
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[PMID: 9873387] |
| CCRF-CEM | IC50 |
11.2 μg/mL
Compound: 104 (LY-186641)
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Concentration required to inhibit growth of CCRF-CEM cells in culture for 72 hr to 50% of control growth
Concentration required to inhibit growth of CCRF-CEM cells in culture for 72 hr to 50% of control growth
|
[PMID: 2391684] |
| CCRF-CEM | IC50 |
11.2 μg/mL
Compound: Sulofenur
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In vitro cytotoxicity against CCRF-CEM cells
In vitro cytotoxicity against CCRF-CEM cells
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[PMID: 9083492] |
| CCRF-CEM | IC50 |
32 μM
Compound: Sulofenur
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Cytotoxicity against CCRF-CEM lymphocytic leukemia cell line
Cytotoxicity against CCRF-CEM lymphocytic leukemia cell line
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[PMID: 10476861] |
| COLO 205 | IC50 |
23.06 μM
Compound: Sulofenur
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Anticancer activity against human COLO205 cells by MTT assay
Anticancer activity against human COLO205 cells by MTT assay
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[PMID: 21570750] |
| K562 | IC50 |
19.2 μM
Compound: Sulofenur
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Anticancer activity against human K562 cells by MTT assay
Anticancer activity against human K562 cells by MTT assay
|
[PMID: 21570750] |
| K562 | IC50 |
50.08 μM
Compound: 2
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Cytotoxicity against human chronic myelogenous leukemia (K562) cell line using MTT assay
Cytotoxicity against human chronic myelogenous leukemia (K562) cell line using MTT assay
|
[PMID: 9873387] |
| P388D1 | IC50 |
>100 μM
Compound: Sulofenur
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Anticancer activity against mouse P388D1 cells by MTT assay
Anticancer activity against mouse P388D1 cells by MTT assay
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[PMID: 21570750] |
| SK-MEL-2 | IC50 |
12.91 μM
Compound: LY-186641
|
In vitro cytotoxic activity against human melanoma SK-MEL-2 cell line
In vitro cytotoxic activity against human melanoma SK-MEL-2 cell line
|
10.1016/0960-894X(96)00463-5 |
| SK-OV-3 | IC50 |
222.9 μM
Compound: 2
|
Cytotoxicity against human ovarian adenocarcinoma (SK-OV-3) cell line using MTT assay
Cytotoxicity against human ovarian adenocarcinoma (SK-OV-3) cell line using MTT assay
|
[PMID: 9873387] |
| SK-OV-3 | IC50 |
78.2 μM
Compound: Sulofenur
|
Anticancer activity against human SKOV3 cells by MTT assay
Anticancer activity against human SKOV3 cells by MTT assay
|
[PMID: 21570750] |
Chemical Information
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CAS No. 110311-27-8
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Molecular Weight 350.82
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Formula C16H15ClN2O3S
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SMILES
O=S(C1=CC2=C(CCC2)C=C1)(NC(NC3=CC=C(Cl)C=C3)=O)=O
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Synonyms
Diarylsulfonylurea; LY186641
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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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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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
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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
References
[1]. Gu H, et al. H-ras transfection of the rat kidney cell line NRK-52E results in increased induction of c-fos, c-jun and hsp70 following sulofenur treatment. Cancer Lett. 1996 Sep 10;106(2):199-205. [Content Brief]
[2]. Brown TD, et al. Phase I trial of sulofenur (LY186641) given orally on a daily x 21 schedule. Anticancer Drugs. 1994 Apr;5(2):151-9. [Content Brief]
[3]. Ehlhardt WJ, et al. Pharmacokinetics of the anticancer agent sulofenur in mice, rats, monkeys, and dogs. J Pharm Sci. 1993 Jul;82(7):683-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)