Selumetinib (AZD6244, ARRY-142886)是一种有效，高选择性的MEK抑制剂，对MEK1的IC50为14 nM，对MEK2的Kd值为530 nM。它也抑制ERK1/2磷酸化，IC50为10 nM，对p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等没有抑制作用。Selumetinib可抑制细胞增殖、迁移并诱导凋亡。Phase 3。
| CAS No. | 606143-52-6 |
| 生物活性 | Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. |
| 分子式 | C17H15BrClFN4O3 |
| 分子量 | 457.68 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 10 mg/mL (21.85 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
| 体内研究 | Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts. Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model. |
| 体外研究 | Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells. Selumetinib (AZD6244) (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells. Selumetinib (AZD6244) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line. |
| 纯度及产品资料 | 98% |
邮箱：info@TianyaBio.com
电话：020-3107 8154
地址：广州市番禺区兴业大道东路1078号2-50
微信公众号
微信客服
