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CAS No. : 197723-00-5
MCE 国际站:BOLD-100
产品活性:BOLD-100 (NKP-1339; IT-139) 是针对实体癌开发的一流钌抗癌试剂,副作用小。BOLD-100 通过线粒体途径诱导 G2/M 细胞周期停滞,DNA 合成阻断 (DNA synthesis) 和诱导细胞凋亡 (apoptosis)。BOLD-100 具有很高的肿瘤靶向潜力,与血清蛋白 (serum proteins) 如白蛋白和转铁蛋白强烈结合,并在还原性肿瘤环境中激活。
研究领域:Cell Cycle/DNA Damage | Apoptosis
作用靶点:DNA/RNA Synthesis | Apoptosis
In Vitro: BOLD-100 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC50 values of 45-200?μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC50 value of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC50 values of 178 μM, 111 μM, and 143 μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL-8, SW480 and HCT116 cells, respectively.BOLD-100 (0-150 μM; 24 hours) induces cell apoptosis alone. When it combines with sorafenib, it increases the numbers of the apopotic cells. Additionally, the p-PARP and caspase 7 cleavage is promoted either.BOLD-100 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment.
In Vivo: BOLD-100 (intravenous injection; 30 mg/kg; once a week; 42sdays) combines with the multi-kinase inhibitor sorafenib and exhibits a further anticancer activity when compares to the BOLD-100 treatment alone in Hep3B xenografts grown in Balb/c SCID mice .
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Lung Cancer Compound Library | SY-5609 | BRD4 Inhibitor-18 | 8α-Tigloyloxyhirsutinolide 13-O-acetate | AAPK-25 | Dutasteride-13C6 | IBU-DC Phosphoramidite | Oleic acid-13C | Anticancer agent 120 | Abacavir sulfate | Meloxicam-d3-1 | 2,4-D sodium salt | Thailanstatin D | SB-218078 | Toyocamycin | Sorafenib-d4 | Busulfan | PTC-028 | Carboplatin-d4 | Dinaciclib | Caracemide | CR-1-31-B | 142I5 | Farudodstat | Ecteinascidin 770 | AT9283 | Staurosporine | SNS-032 | AZA1 | Antitumor agent-96 | Bleomycin A5
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