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STAT3-IN-10
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
STAT3-IN-10图片
CAS NO:2499491-04-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
STAT3-IN-10 是一种STAT3抑制剂,IC50为 5.18 μM。STAT3-IN-10 与STAT3 SH2结构域直接结合,抑制肿瘤细胞生长和诱导肿瘤细胞的凋亡 (apoptosis)。
生物活性

STAT3-IN-10 is aSTAT3inhibitor with anIC50value of 5.18 μM. STAT3-IN-10 directly binds toSTAT3SH2domain, inducescancercellsapoptosis[1].

IC50& Target

STAT3

5.18 μM (IC50)

体外研究
(In Vitro)

STAT3-IN-10 (A11) (48 h) shows IC50values of 0.67, 0.77, 1.24 μM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively[1].
STAT3-IN-10 (A11) directly binds to the STAT3 SH2 domain[1].
STAT3-IN-10 (A11) (0-3 μM, 24 h) inhibits the phosphorylation of STAT3 and its downstream target proteins and has a good selectivity against the tumor suppressor STAT1[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) induces apoptosis in cancer cells[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) dose-dependently causes a significant S phase arrest in MDA-MB-231 cells[1].

Cell Viability Assay[1]

Cell Line:Breast cancer cell lines: MDA-MB-231 and MDA-MB-468; human liver carcinoma cell line: HepG2.
Concentration:
Incubation Time:48 h, re-incubated for 4 h (MDA-MB-468, MDA-MB-231) and 1h (HepG2).
Result:Showed IC50values of 0.67, 0.77, 1.24 μM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively.

Western Blot Analysis[1]

Cell Line:MDA-MB-231.
Concentration:0, 0.75, 1.5 and 3.0 μM.
Incubation Time:24 h.
Result:Decreased the STAT3-Y705 phosphorylation without affecting the total amount of STAT3 protein and decreased the expression of STAT3 target genes, including C-Myc and Cyclin D1 in a dose-dependent manner. Had little impact on the level of STAT1 and its phosphorylation on Tyr701.

Apoptosis Analysis[1]

Cell Line:MDA-MB-231.
Concentration:0, 1, 2, and 4 μM.
Incubation Time:24 h.
Result:Induced the apoptosis in MDA-MB-231 cells in a concentration-dependent manner

Cell Cycle Analysis[1]

Cell Line:MDA-MB-231.
Concentration:0, 1, 2, and 4 μM.
Incubation Time:24 h.
Result:Could dose-dependently cause a significant S phase arrest in MDA-MB-231 cells
体内研究
(In Vivo)

STAT3-IN-10 (A11) (i.p.; 5, 10 mg/kg; once a day, 21 days) inhibits the growth of human xenograft tumor in vivo[1].

Animal Model:Five weeks old female BALB/c nude mice (16–18g) bearing inoculation of human breast cancer cells MDA-MB-231[1].
Dosage:5 and 10 mg/kg
Administration:IP, once a day, 21 days
Result:Inhibited the growth of human xenograft tumor in vivo without apparent body-weight loss for treated mice and inhibited the levels of p-STAT3 in tumor tissues.
分子量

311.29

Formula

C17H13NO5

CAS 号

2499491-04-0

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.