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STAT3-IN-10
STAT3-IN-10 (A11) 是一个 IC50 值为5.18 µM 的 STAT3 抑制剂。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)
STAT3-IN-10 Chemical Structure
CAS No. : 2499491-04-0
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
STAT3-IN-10 (A11) is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, inhibits tumor cell growth and induces apoptosis in cancer cells[1].
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| IC50 & Target |
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体外研究
(In Vitro) |
STAT3-IN-10 (A11) (48 h) shows IC50 values 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].
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: |
Breast cancer cell lines: MDA-MB-231 and MDA-MB-468; human liver carcinoma cell line: HepG2. |
| Concentration: |
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| Incubation Time: |
48 h, re-incubated for 4 h (MDA-MB-468, MDA-MB-231) and 1h (HepG2). |
| Result: |
Showed IC50 values 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 |
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体内研究
(In Vivo) |
STAT3-IN-10 (A11) (5 and 10 mg/kg; IP; once a day, 21 days) inhibits the growth of human xenograft tumor in vivo[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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