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NSC 74859

CAS No. : 501919-59-1

MCE 站：NSC 74859

产品活性：NSC 74859 (S3I-201) 是选择性的 Stat3 抑制剂，IC₅₀ 为 86 μM。

研究领域：JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶点：STAT

In Vitro: NSC 74859 (S3I-201) preferentially inhibits Stat3 DNA-binding activity over that of Stat1 (IC₅₀ values, Stat3•Stat3, 86±33 μM; Stat1•Stat3, 160±43 μM; ａnd Stat1•Stat1, >300 μM) ａnd inhibits that of Stat5 with IC₅₀ of 166±17 μM). NSC 74859 significantly reduces viable cell numbers ａnd inhibits growth of transformed mouse fibroblasts NIH 3T3/v-Src ａnd breast carcinoma cell lines (MDA-MB-231, MDA-MB-435, ａnd MDA-MB-468). At 30-100 μM, NSC 74859 induces significant apoptosis in the representative human breast carcinoma cell line MDA-MB-435 ａnd NIH 3T3/v-Src, both of which harbor constitutively active Stat3. The breast carcinoma MDA-MB-435 cell line is more sensitive to 30 μM NSC 74859. By contrast, the human breast cancer MDA-MB-453 cells ａnd the normal mouse fibroblasts (NIH 3T3), which do not contain abnormal Stat3 activity, are less sensitive to NSC 74859 at 100 μM or less. At 300 μM or higher, NSC 74859 induced general, nonspecific cytotoxicity independent of Stat3 activation status. Huh-7 cells do not express β2SP or TBGFR2 ａnd are sensitive to STAT3 inhibition, with an IC₅₀ of 100 μM for NSC 74859, regardless of CD133⁺ status. The IC₅₀ of NSC 74859 is 150 μM for Huh-7 ａnd SNU-398 cells, 15 μM for SNU-475 cells ａnd 200 μM for SNU-182 cells. NSC 74859 inhibits breast carcinoma MDA-MB-435, MDA-MB-453 ａnd MDA-MB-231 cell lines with an IC₅₀ close to 100 μM.

In Vivo: Human breast (MDA-MB-231) tumor-bearing mice are given an i.v. injection of NSC 74859 (S3I-201) or vehicle every 2 or every 3 days for 2 weeks, ａnd tumor measurements are taken every 2-3 days. Compared with control (vehicle-treated) tumors, which continued to grow, human breast tumors in mice that received S3I-201 display strong growth inhibition. Continued evaluation of treated mice on termination of treatment shows no resumption of tumor growth, suggesting potentially a long-lasting effect of S3I-201 on tumor growth. Compared with vehicle-treated control tumors (n=15), which continued to grow, S3I-201 treatment of somatotroph tumor xenografts (n=15) significantly attenuated tumor growth for the duration of the experiment. Tumors derived from NSC 74859-treated rats are significantly smaller than those from the untreated group (220±16 mm³ vs. 287±16 mm³, P<0.01) as early as 5 days after NSC 74859 injection. Fifteen days after treatments, the average tumor volume of NSC 74859-treated rats is 64% of that of controls (449±40 mm³ vs. 708±83 mm³, P<0.01). Rats are sacrificed ａnd tumors are harvested 15 days after treatment initiation. The average tumor weight of NSC 74859-treated rats is 78±8 mg, while tumors derived from control rats weighed 114±13 mg (32% reduction; P<0.05).

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