STAT3-IN-10

Modify Date: 2024-01-16 01:48:30

STAT3-IN-10 structure	Common Name	STAT3-IN-10
	CAS Number	2499491-04-0	Molecular Weight	311.29
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₇H₁₃NO₅	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of STAT3-IN-10

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].

Name	STAT3-IN-10

Description	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].
Related Catalog	Signaling Pathways >> Stem Cell/Wnt >> STAT Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> STAT
Target	STAT3:5.18 μM (IC50)
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]. 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 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
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]. 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.
References	[1]. Kai-Rui Feng, et al. Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy. Eur J Med Chem. 2020 Sep 1;201:112428.

Molecular Formula	C₁₇H₁₃NO₅
Molecular Weight	311.29