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SIJ1777是一种嘧啶并嘧啶酮类II型泛BRAF抑制剂,作为GNF-7的优化衍生物,其通过同时抑制MAPK通路(MEK/ERK)与PI3K/AKT通路的磷酸化活化来发挥抗肿瘤效应。SIJ1777核心优势在于对现有临床药物(如vemurafenib、PLX8394)不敏感的二/三类BRAF突变(非V600突变)及NRAS突变黑色素瘤细胞仍能维持双位数纳摩尔级别的GI50值,并能有效诱导凋亡并阻断肿瘤细胞的迁移与锚定非依赖性生长。
SIJ1777是一种嘧啶并嘧啶酮类II型泛BRAF抑制剂,作为GNF-7的优化衍生物,其通过同时抑制MAPK通路(MEK/ERK)与PI3K/AKT通路的磷酸化活化来发挥抗肿瘤效应。SIJ1777核心优势在于对现有临床药物(如vemurafenib、PLX8394)不敏感的二/三类BRAF突变(非V600突变)及NRAS突变黑色素瘤细胞仍能维持双位数纳摩尔级别的GI50值,并能有效诱导凋亡并阻断肿瘤细胞的迁移与锚定非依赖性生长。

| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 2,330 | 现货 | |
| 5 mg | ¥ 5,630 | 现货 | |
| 10 mg | ¥ 7,880 | 现货 | |
| 25 mg | ¥ 11,700 | 现货 | |
| 50 mg | ¥ 15,300 | 现货 | |
| 100 mg | ¥ 19,500 | 现货 |
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| 产品描述 | SIJ1777 is a pyrimidopyrimidinone class type II pan-BRAF inhibitor, optimized as a derivative of GNF-7. It exerts anti-tumor effects by simultaneously inhibiting the phosphorylation and activation of the MAPK pathway (MEK/ERK) and the PI3K/AKT pathway. The core advantage of SIJ1777 is its ability to maintain double-digit nanomolar GI50 values against class II/III BRAF mutants (non-V600 mutants) and NRAS-mutant melanoma cells that are insensitive to current clinical drugs (such as vemurafenib, PLX8394), effectively inducing apoptosis and blocking tumor cell migration and anchorage-independent growth. |
| 体外活性 | SIJ1777显著增强了对多种黑色素瘤细胞 (SK-MEL-2、SK-MEL-28、A375、WM3670、WM3629)的抗增殖活性,其效果是GNF-7的2至14倍。 |
| 分子量 | 536.51 |
| 分子式 | C26H23F3N8O2 |
| CAS No. | 839707-55-0 |
| Smiles | O=C(NC1=CC=C(C(=C1)N2C(=O)N(C3=NC(=NC=C3C2)NC4=NN(C=C4)C)C)C)C5=CC=CC(=C5)C(F)(F)F |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 |
对于不同动物的给药剂量换算,您也可以参考 更多