| 中文名称: | PLX8394 | ||||
|---|---|---|---|---|---|
| 英文名称: | PLX8394 | ||||
| 别名: | FORE8394;PLX 8394 | ||||
| CAS No: | 1393466-87-9 | 分子式: | C25H21F3N6O3S | 分子量: | 542.53 |
| CAS No: | 1393466-87-9 | ||||
| 分子式: | C25H21F3N6O3S | ||||
| 分子量: | 542.53 | ||||
包装规格：
1mg 5mg 25mg 100mg in glass bottle
产品简介：
PLX8394 是一种口服活性的丝氨酸/苏氨酸蛋白激酶 B-Raf (BRaf) 蛋白抑制剂。 PLX8394 可以选择性地结合并抑制野生型和突变形式的 BRaf 的活性，然后抑制表达 BRaf 突变形式的肿瘤细胞的增殖。 PLX8394 似乎对表达多种激酶突变形式的肿瘤有效，并且可能是对其他对 BRaf V600E 突变体特异的 BRaf 抑制剂疗法耐药的肿瘤的有效治疗剂。
溶解性：
溶解性(25°C)体外DMSO: 100 mg/mL (184.32 mM);水:不溶性;乙醇:不溶性;
体外研究：
PLX8394 (>25 nM) effectively inhibits phosphorylation of ERK1/2 in PRT 3 and PRT 4 cells and in addition to parental cells at 10 nM. PLX8394 effectively reduces phosphorylation of retinoblastoma protein, cyclin D3/D1, and expression of cyclin A2 in parental cells and PRT 3/4 cells. PLX8394 inhibits ERK1/2 phosphorylation and the growth of vemurafenib-resistant cells harboring either a BRAF V600K/L505H double mutation or a transposon-induced, N-terminal truncated form of BRAF. PLX8394 significantly impairs tumor cell growth and suppresses MAPK signaling in LA cell lines expressing either endogenous V600E or non-V600 mutant forms of BRAF.
体内研究：
In mice H1755 xenograft tumors, PLX8394 (150 mg/kg/day) substantially suppresses tumor growth, tumor cell proliferation and MAPK pathway signaling without overt toxicity. PLX8394 combines with erlotinib yields plasma erlotinib concentrations of >1 μM.
细胞实验：
Dissolvent: DMSO. For MTT assays, 2×103.cells are seeded in triplicate in 96 wells in their regular culture medium (containing PLX4720 for PRT lines). Next day, cells are washed twice with PBS and then the medium is replenished containing the indicated RAF inhibitor. Medium is changed 48 hours later and after a further 48 hours, 10 μL of 5 mg/mL MTT reagent is added to wells and incubated for three hours. Formazan crystals are then solubilized overnight with a 1:10 dilution of 0.1 M glycine (pH 10.5) in DMSO. Wells are then analyzed at 450 nM in a Multiskan Spectrum spectrophotometer. Results depicted are normalized to DMSO conditions and are a composite of three independent experiments. Error bars shown are representative of the standard error of mean (SEM).
动物实验：
PLX8394 is dissolved in PEG 400 [20% (v/v)], TPGS [5% (v/v)], and water [75% (v/v)].H1755 tumor xenografts are generated by injection of 5×106 cells in a 50/50 mixture for matrigel and PBS into 6- to 8-wk-old female NOD/SCID mice. Mice are randomized to treatment groups once tumors reach an average size of 150 mm3. H1755 cells are s.c. implanted and allowed to grow to appr 200 mm3 (4 wk after implantation). Mice are then treated with vehicle, vemurafenib, or PLX8394 for 15 d. The vehicle for daily oral gavage is PEG 400 [20% (vol/vol)], tocopheryl polyethylene glycol succinate (TPGS) [5% (vol/vol)], water [75% (vol/vol)]. PLX8394 is dissolved in PEG 400 [20% (vol/vol)], TPGS [5% (vol/vol)], and water [75% (vol/vol)] and vortexed continuously throughout the dosing period. PLX8394 (p.o.) is given at a dose of 150 mg/kg/d.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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