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AD80 是多激酶抑制剂,可抑制 RET、RAF、SRC 和 S6K,并大大降低 mTOR 活性。
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AD80 是多激酶抑制剂,可抑制 RET、RAF、SRC 和 S6K,并大大降低 mTOR 活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 385 | 现货 | |
5 mg | ¥ 949 | 现货 | |
10 mg | ¥ 1,520 | 现货 | |
25 mg | ¥ 2,970 | 现货 | |
50 mg | ¥ 4,280 | 现货 | |
100 mg | ¥ 6,130 | 现货 | |
500 mg | ¥ 12,200 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 991 | 现货 |
产品描述 | AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity. |
靶点活性 | RET (V804L):0.6 nM, RET (V804M):0.4 nM |
体外活性 | AD80和AD81抑制RET、RAF、SRC和S6K,相比于AD57和AD58,mTOR活性显著降低。AD80在抑制Ras-Erk信号通路方面表现最佳,具有针对Ret、Raf、Src、Tor和S6K的高效性和极低的毒性的最佳活性平衡。AD80能够抑制MZ-CRC-1和TT甲状腺癌细胞的增殖,这一作用可能通过诱导凋亡实现。AD80同时抑制S6K1和TAM家族酪氨酸激酶AXL,避免了S6K1的磷酸化和mTOR的共同关联,从而持久地抑制了S6K1引发的信号传导和蛋白质合成。 |
体内活性 | AD80在移植PTEN缺失白血病细胞的小鼠中拯救了50%的个体。口服AD80或AD81可使Drosophila ptc>dRetMEN2B模型中70-90%的动物成年,效果显著优于AD57。在小鼠异种移植模型中,AD80还能比vandetanib更有效地抑制肿瘤生长并减少体重调节。 |
细胞实验 | MZ-CRC-1 (MEN2B) and TT (MEN2A) cells are treated with AD80 (0.2 nM to 20 μM) for 7 days and cell viability is quantitated by MTT assay. |
动物实验 | Mice showing established growing tumors are separated into vehicle or drug treatment groups. A similar range of tumor sizes is selected for each experiment (vehicle vs AD57; vehicle vs AD80 vs Vandetanib). Vehicle, AD57 (20 mg/kg), AD80 (30 mg/kg), or Vandetanib (50 mg/kg) are administered by oral gavage (PO; per os or by mouth) once daily, five times a week. Tumor and body weight measurements are performed 3 times a week. |
分子量 | 473.43 |
分子式 | C22H19F4N7O |
CAS No. | 1384071-99-1 |
Smiles | CC(C)n1nc(-c2ccc(NC(=O)Nc3cc(ccc3F)C(F)(F)F)cc2)c2c(N)ncnc12 |
密度 | 1.49 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 | DMSO: 60 mg/mL (126.73 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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