1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea

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1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea 

STAT3-IN-7 是一种 Sorafenib 的衍生物，可有效抑制 STAT3 的磷酸化。STAT3-IN-7 通过依赖 SHP-1 的 STAT3 失活诱导细胞凋亡 (apoptosis)，不抑制激酶活性，并具有抗癌作用。

1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea

1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea Chemical Structure

CAS No. : 1313019-65-6

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生物活性

STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects[1].

IC50 & Target[1]

p-STAT3

 

体外研究
(In Vitro)

STAT3-IN-7 (SC-1; 1-10 μM; 48 hours; breast cancer cells) treatment demonstrates dose-dependent suppression of cell viability in all tested breast cancer cells[1].
STAT3-IN-7 (SC-1; 1-10 μM; 36 hours; breast cancer cells) treatment induces potent apoptotic activity[1].
STAT3-IN-7 (SC-1; 1-10 μM; 36 hours; breast cancer cells) treatment shows downregulation of p-STAT3 and its downstream proteins cyclin D1 and survivin in a dose-dependent manner in breast cancer cell lines[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HCC-1937, MDA-MB-231, MDA-MB-468, MDA-MB-453, SK-BR3 and MCF-7 cells
Concentration: 1 μM, 2 μM, 5 μM, 7.5 μM, 10 μM
Incubation Time: 48 hours
Result: Demonstrated dose-dependent suppression of cell viability in all tested breast cancer cells.

Apoptosis Analysis[1]

Cell Line: HCC-1937, MDA-MB-231, MDA-MB-468, MDA-MB-453, SK-BR3 and MCF-7 cells
Concentration: 1 μM, 2 μM, 5 μM, 7.5 μM, 10 μM
Incubation Time: 36 hours
Result: Induced potent apoptotic activity.

Western Blot Analysis[1]

Cell Line: HCC-1937, MDA-MB-231, MDA-MB-468, MDA-MB-453, SK-BR3 and MCF-7 cells
Concentration: 1 μM, 2 μM, 5 μM, 7.5 μM, 10 μM
Incubation Time: 36 hours
Result: Showed downregulation of p-STAT3 and its downstream proteins cyclin D1 and survivin in a dose-dependent manner in breast cancer cell lines.

体内研究
(In Vivo)

STAT3-IN-7 (10 mg/kg; oral gavage; daily; for 28 days; female NCr athymic nude mice) treatment shows efficacious antitumor activity and p-STAT3 downregulation in MDA-MB-468 xenograft tumors[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NCr athymic nude mice (4-6 weeks of age) injected with breast cancer cells [1]
Dosage: 10 mg/kg
Administration: Oral gavage; daily; for 28 days
Result: Showed efficacious antitumor activity and p-STAT3 downregulation in MDA-MB-468 xenograft tumors.

分子量

431.80

Formula

C21H13ClF3N3O2
CAS 号

1313019-65-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chun-Yu Liu, et al. Novel sorafenib analogues induce apoptosis through SHP-1 dependent STAT3 inactivation in human breast cancer cells. Breast Cancer Res. 2013;15(4):R63.

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