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Pladienolide B 是一种有效的剪接体抑制剂,是从钝顶链霉菌 Mer-12 中分离出的大环内酯类化合物,其作用靶向剪接体的 SF3B1 亚单位。Pladienolide B 通过抑制前 mRNA 剪接发挥抗肿瘤作用,诱导调亡。Pladienolide B 具有抗肿瘤活性,可用于研究白血病和淋巴肿瘤。
Pladienolide B 是一种有效的剪接体抑制剂,是从钝顶链霉菌 Mer-12 中分离出的大环内酯类化合物,其作用靶向剪接体的 SF3B1 亚单位。Pladienolide B 通过抑制前 mRNA 剪接发挥抗肿瘤作用,诱导调亡。Pladienolide B 具有抗肿瘤活性,可用于研究白血病和淋巴肿瘤。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 μg | ¥ 3,480 | 现货 |
产品描述 | Pladienolide B is a potent spliceosome inhibitor, a macrolide isolated from Streptomyces obtusususus Mer-12, which targets the SF3B1 subunit of the spliceosome.Pladienolide B exerts its antitumor effects by inhibiting pre-mRNA splicing and inducing necrosis.Pladienolide B possesses antitumor activity and can be used to study leukemia and lymphoid tumors. Pladienolide B has antitumor activity and can be used to study leukemia and lymphoid tumors. |
体外活性 | Pladienolide B (0.1-2 nM; 24-48 h; HeLa cells) decreases SF3b1 expression in human cervical carcinoma cells. Pladienolide B causes (0.1-2 nM; 24 h; HeLa cells) cell cycle arrest and apoptosis. Pladienolide B (0.1-2 nM; 24-72 h; HeLa cells) suppresses human cervical carcinoma cells viability. Pladienolide B Significantly decreased cell viability, and the decrease was concentration- and time-dependent.[3] |
体内活性 | Pladienolide B (2.5-10 mg/kg; i.v.; daily for 5 days; BALB/c nu/nu mice; PC-3, OVCAR-3, DU-145, WiDr, and HCT-116, BSY-1 xenografts) showed strong growth inhibitory or regressive activities against these xenografts. Having intense antitumor activities.[4] |
别名 | 普拉地内酯B |
分子量 | 536.7 |
分子式 | C30H48O8 |
CAS No. | 445493-23-2 |
Smiles | C([C@@H](/C=C/C=C(\C)/[C@@H]1[C@@H](C)/C=C/[C@H](OC(C)=O)[C@](C)(O)CC[C@@H](O)CC(=O)O1)C)[C@@H]2[C@@]([C@@H]([C@H](CC)O)C)(O2)[H] |
密度 | 1.13 g/cm3 (Predicted) |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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