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SC144 是一种口服活性 gp130 抑制剂。它结合 gp130,诱导 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,进一步抑制下游靶基因的表达。它对 gp130 配体触发的信号转导有明显的抑制作用,可诱导人卵巢癌细胞凋亡。
SC144 是一种口服活性 gp130 抑制剂。它结合 gp130,诱导 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,进一步抑制下游靶基因的表达。它对 gp130 配体触发的信号转导有明显的抑制作用,可诱导人卵巢癌细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 197 | 现货 | |
5 mg | ¥ 452 | 现货 | |
10 mg | ¥ 771 | 现货 | |
25 mg | ¥ 1,460 | 现货 | |
50 mg | ¥ 2,450 | 现货 | |
100 mg | ¥ 3,970 | 现货 | |
500 mg | ¥ 8,630 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 490 | 现货 |
产品描述 | SC144 is an orally active small-molecule gp130 inhibitor. |
靶点活性 | Gp130:< 1 μM (Cell assay) |
体外活性 | SC144 exhibits potent cytotoxicity against a panel of drug-sensitive and drug-resistant cancer cell lines. SC144 shows synergism with both 5-fluorouracil and oxaliplatin when co-treated in colorectal cancer HT29 cells. Pretreatment with SC144 in oxaliplatin-resistant HTOXAR3 cells is more effective than oxaliplatin pretreatment. In addition, the combination of SC144 and paclitaxel exhibited synergism in MDA-MB-435 cells with a schedule-dependent block in cell cycle. [1] SC144 treatment in vitro induces gp130 phosphorylation and deglycosylation, resulting in the downregulation of surface-bound gp130 and the abrogation of gp130-associated Stat3 activation. In addition, SC144 selectively inhibits the downstream signaling activation induced by gp130 substrates, including IL-6 and LIF. Protein expression regulated by the gp130/Stat3 axis in OVCAR-8 cells is also down-regulated after SC144 treatment, including Bcl-2, Bcl-XL, survivin, cyclin D1, MMP-7, gp130 and Ape1/Rel-1. [2] |
体内活性 | SC144 significantly inhibits tumor growth in a mouse xenograft model of human ovarian cancer via i.p. or p.o. administration. After SC144 treatment for two months, gp130, Bcl-2, Bcl-XL, MMP-7 and Ape1/Ref-1 protein levels are substantially decreased in the tumor site in the treatment group compared with the control group. [2] In an MDA-MB-435 mouse xenograft model, co-administration of SC144 and paclitaxel delays tumor growth in an SC144 dose-dependent manner. Evaluation of the pharmacokinetics of SC144 reveals that intraperitoneal administration of SC144 shows a two-compartmental pharmacokinetics elimination profile that is not observed in the oral dosing. [1] |
细胞实验 | MTT assay (Only for Reference) |
分子量 | 322.3 |
分子式 | C16H11FN6O |
CAS No. | 895158-95-9 |
Smiles | Cl.Fc1ccc2c(c1)nc(NNC(=O)c1cnccn1)c1cccn21 |
密度 | 1.53 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 15 mg/mL (46.54 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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