HS-1793

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

白藜芦醇类似物 HS-1793 在裸鼠异种移植模型中下调缺氧诱导的 HIF-1 和 VEGF 的表达并抑制人乳腺癌细胞的肿瘤生长。

HS-1793, a resveratrol analogue, downregulates the expression of hypoxia-induced HIF-1 and VEGF and inhibits tumor growth of human breast cancer cells in a nude mouse xenograft model.

HS-1793 (0-100 μM; 24 h) suppresses proliferation of MCF-7, MDA-MB-231 and HCT116 cells.HS-1793 (0-50 μM; 4 h) inhibits hypoxia-induced HIF-1α protein in MCF-7 and MDA-MB-231 cells unrelated to cell death, downregulates hypoxia-induced VEGF expression, and suppresses hypoxia-induced mRNA expression of VEGF at the transcriptional level.HS-1793 (0-100 μM; 24 h) induces apoptosis, promotes G2/M cell cycle arrest, and inhibits Akt and ERK phosphorylation in HCT116 cells. Cell Proliferation Assay Cell Line:MCF-7, MDA-MB-231 and MCF-10A Concentration:0-100 μM Incubation Time:24 h Result:Showed antiproliferation activity with IC50 values of 26.3±3.2, 48.2±4.2 and >100 μM against MCF-7, MDA-MB-231 and MCF-10A, respectively.Western Blot Analysis Cell Line:MCF-7, MDA-MB-231 Concentration:12.5, 25 and 50 μM Incubation Time:4 h Result:Downregulated HIF-1α expression in a concentration-dependent manner in both cell lines.RT-PCR Cell Line:MCF-7, MDA-MB-231 Concentration:12.5, 25 and 50 μMIncubation Time:4 h Result:Downregulated the expression of VEGF mRNA, with the more marked results observed in MDA-MB-231 cells.Cell Proliferation Assay Cell Line:HCT116 Concentration:12.5, 25, 50 and 100 μMIncubation Time:1, 2 and 4 daysResult:Significantly reduced the cell viability concentration- and time-dependently. Significantly suppressed proliferation of colon cancer cell line HCT116.Apoptosis Analysis Cell Line:HCT116 Concentration:12.5, 25, 50 and 100 μM Incubation Time:24 h Result:Induced cell apoptosis in a dose-dependent manner. Caused chromatin condensation and fragmentation.Western Blot Analysis Cell Line:HCT116 Concentration:12.5, 25, 50 and 100 μM Incubation Time:24 h Result:Effectively induced the reduction of pro-caspase-8 and pro-caspase-3 at 100 μM. Activated caspase-8 and caspase-3. Caused the PARP cleavage. Slightly downregulated the level of antiapoptotic protein Bcl-2 at 100 μM. Promoted an increase in the release of cytochrome c from the mitochondria into the cytosol. Decreased the expression of G2/M cell cycle regulatory protein cyclin B1, Cdc2 and Cdc25C. Decreased the level of CDK4 and CDK6. Decreased Akt phosphorylation and reduced total Akt at high-concentration.

HS-1793 (5 and 10 mg/kg; i.p.; twice a week, 4 weeks) significantly inhibits MDA-MB-231 xenograft tumor growth and in a dose-dependent manner and relatively hampers angiogenesis with non-toxicity. Animal Model:Five-week-old female BALB/c nude mice injected with MDA-MB-231 cells Dosage:5 mg/kg and 10 mg/kg (dissolved in PBS containing 0.1% v/v dimethyl sulfoxide (DMSO)) Administration:Intraperitoneal injection, twice a week, 4 weeks Result:Significantly inhibited MDA-MB-231 xenograft tumor growth in a dose-dependent manner with non-toxicity. Significantly lowered Ki-67 (a proliferation marker) and CD31 expression. Successfully suppressed the expression of HIF-1α and VEGF in tumor tissues.

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927885-00-5

252.27

C16H12O3

>98% (HPLC)

DMSO:10 mM

C1=CC2=C(C=CC(=C2)O)C=C1C3=C(C=C(C=C3)O)O

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(-20℃)

With Ice Pack

≥ 2 years