Plixorafenib (PLX8394)

製品コードS7965 バッチS796501

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₂₁F₃N₆O₃S

分子量

542.53

CAS No.

1393466-87-9

Solubility (25°C)*

体外

DMSO

100 mg/mL (184.32 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Plixorafenib (PLX8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.
in vitro	PLX8394 is a next-generation, orally available small-molecule BRAFi that does not induce the RAF/MEK/ERK paradoxical activation and blocks signaling from both monomeric BRAF^V600 and dimeric BRAF^{non-V600 protein}^[1].
in vivo	PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with potential antineoplastic activity.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	colorectal cancer cell lines
	濃度	1 μM
	反応時間	6 h
	実験の流れ	Cells were treated with DMSO, PLX8394 at 1 μM for 6 h.
動物実験	動物モデル	Female NOD-SCID mice
	投薬量	150 mg/kg
	投与方法	p.o.

参考

http://mct.aacrjournals.org/content/17/1_Supplement/B176
https://pubmed.ncbi.nlm.nih.gov/26466569/
https://pubmed.ncbi.nlm.nih.gov/28659148/

https://pubmed.ncbi.nlm.nih.gov/34108213/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Bioluminescence-based assays for quantifying endogenous protein interactions in live cells [ J Biol Chem, 2025, 301(8):110454]	PubMed: 40617353
Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936]	PubMed: 38588697
ERK signaling promotes resistance to TRK kinase inhibition in NTRK fusion-driven glioma mouse models [ Cell Rep, 2024, 43(10):114829]	PubMed: 39365700
Mcl-1 mediates intrinsic resistance to RAF inhibitors in mutant BRAF papillary thyroid carcinoma [ Cell Death Discov, 2024, 10(1):175]	PubMed: 38622136
SB202190 Predicts BRAF-Activating Mutations in Primary Colorectal Cancer Organoids via Erk1-2 Modulation [ Cells, 2023, 12(4)664]	PubMed: 36831331
SB202190 Predicts BRAF-Activating Mutations in Primary Colorectal Cancer Organoids via Erk1-2 Modulation [ Cells, 2023, 12(4)664]	PubMed: 36831331
Design and Synthesis of Novel 2-Acetamido, 6-Carboxamide Substituted Benzothiazoles as Potential BRAFV600E Inhibitors - In vitro Evaluation of their Antiproliferative Activity [ ChemMedChem, 2023, e202300322.]	PubMed: 37792577
Classical RAS proteins are not essential for paradoxical ERK activation induced by RAF inhibitors [ Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119]	PubMed: 35091470
Increased IRF9-STAT2 signaling leads to adaptive resistance toward targeted therapy in melanoma by restraining GSDME-dependent pyroptosis [ J Invest Dermatol, 2022, S0022-202X(22)00096-3]	PubMed: 35148998
Preclinical Characterization of a Next-Generation Brain Permeable, Paradox Breaker BRAF Inhibitor [ Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2761]	PubMed: 34782366

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。