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Larotrectinib sulfate (LOXO-101 sulfate) 是一种 ATP 竞争性的,口服选择性抑制剂,对原肌凝蛋白相关激酶家族受体的三个亚型具有纳摩尔级别的 50% 抑制浓度。
Larotrectinib sulfate (LOXO-101 sulfate) 是一种 ATP 竞争性的,口服选择性抑制剂,对原肌凝蛋白相关激酶家族受体的三个亚型具有纳摩尔级别的 50% 抑制浓度。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 278 | 现货 | |
2 mg | ¥ 393 | 现货 | |
5 mg | ¥ 655 | 现货 | |
10 mg | ¥ 987 | 现货 | |
25 mg | ¥ 1,980 | 现货 | |
50 mg | ¥ 3,280 | 现货 | |
100 mg | ¥ 5,390 | 现货 | |
500 mg | ¥ 10,800 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 759 | 现货 |
产品描述 | Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
体外活性 | Larotrectinib是一种特定的激酶抑制剂,具有针对TRKA/TRKB/TRKC的纳摩级活性,但对其他激酶没有显著的抑制作用(1 μM)。Larotrectinib不抑制表达其他致癌基因靶点(EGFR, ROS1或ALK)的Ba/F3细胞的增殖,也不抑制不含NTRK1融合基因的肺和结直肠细胞系的增殖。它能够引起KM12细胞G1期的细胞周期停滞和凋亡。 |
体内活性 | 早期/持续而非晚期/急性给予ARRY-470(LOXO-101)明显减轻了骨癌痛,并阻断了感觉神经纤维的异位生长和肿瘤负重骨中神经瘤样结构的形成,但对肿瘤生长或骨重塑没有显著抑制作用。其穿过血脑屏障的能力非常有限。 |
细胞实验 | Concentrations: 10,100,1000 nM. Method: Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G,gefitinib 1,000 nM) or DMSO control.The cell lysate is used for western blot analysis. |
动物实验 | Animal Models: Adult male C3H/HeJ mice. Formulation: Labrafac; polygly-colyzed glyceride. Dosages: 10-100 mg/kg. Administration: p.o. |
别名 | LOXO-101 sulfate, LOXO-101 (sulfate), ARRY-470 (sulfate) |
分子量 | 526.51 |
分子式 | C21H22F2N6O2·H2O4S |
CAS No. | 1223405-08-0 |
Smiles | OS(O)(=O)=O.O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F |
密度 | no data available |
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: 50 mg/mL (94.96 mM) Ethanol: 10 mg/mL (19 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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