| Bioactivity | PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAFV600E. | ||||||||||||
| Invitro | PLX8394 在 PRT #3 和 PRT #4 细胞中以 >25 nM 以及在 10 nM 时有效抑制亲本细胞中的 ERK1/2 磷酸化。PLX8394 有效降低细胞周期蛋白 D3 和细胞周期蛋白 D1、视网膜母细胞瘤蛋白的磷酸化以及亲代细胞和 PRT #3 和 PRT #4 细胞中细胞周期蛋白 A2 的表达。PLX8394 抑制 ERK1/2 磷酸化和携带 BRAF V600K/L505H 双突变或转座子诱导的 N 末端截短形式的 BRAF PLX4032 抗性细胞的生长[1]。PLX8394 显著损害肿瘤细胞生长并抑制表达内源性 V600E 或非 V600 突变形式 BRAF[2]的 LA 细胞系中的 MAPK 信号传导。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Plixorafenib 相关抗体: | ||||||||||||
| In Vivo | PLX8394 (150 mg/kg/d) 显著抑制这些 H1755 异种移植肿瘤中的肿瘤生长、MAPK 通路信号和肿瘤细胞增殖，对小鼠没有明显毒性。PLX8394 与 CP-358774 结合产生 >1 μM 的CP-358774 血浆浓度[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
| CAS | 1393466-87-9 | ||||||||||||
| Formula | C25H21F3N6O3S | ||||||||||||
| Molar Mass | 542.53 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Basile KJ, et al. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors. Pigment Cell Melanoma Res. 2014 May;27(3):479-484. [2]. Okimoto RA, et al. Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer. Proc Natl Acad Sci U S A. 2016 Nov 22;113(47):13456-13461 |