Selpercatinib (LOXO-292)

製品コードS8781 バッチS878102

印刷

化学情報

Synonyms

ARRY-192

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₉H₃₁N₇O₃

分子量

525.60

CAS No.

2152628-33-4

Solubility (25°C)*

体外

DMSO

40 mg/mL (76.1 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	Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively.
in vitro	Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NB1 cells
	濃度	1 μM
	反応時間	2 h
	実験の流れ	Cells were pre-treated with LOXO292 (1 µM) for 2 h before stimulation with ALKAL2 or GDNF.
動物実験	動物モデル	Female nu/nu BALB/c mice
	投薬量	3 mg/kg
	投与方法	o.g.

参考

https://www.loxooncology.com/docs/presentations/2016_EORTC_LOXO-292_POSTER.pdf
https://pubmed.ncbi.nlm.nih.gov/33921066/
https://pubmed.ncbi.nlm.nih.gov/31988000/

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：

AP1-mediated reprogramming of EGFR expression triggers resistance to BLU-667 and LOXO-292 in RET-rearranged tumors [ J Exp Clin Cancer Res, 2025, 44(1):154]	PubMed: 40405293
Potent and highly selective inhibition of selpercatinib towards UDP-glucuronosyltransferase 1A4 (UGT1A4) isoform [ Toxicol Appl Pharmacol, 2025, 500:117393]	PubMed: 40354983
LC-MS/MS method development and validation for novel targeted anticancer therapies adagrasib, capmatinib, ensartinib, entrectinib, larotrectinib, lorlatinib, pralsetinib, selpercatinib and sotorasib [ J Pharm Biomed Anal, 2025, 266:117078]	PubMed: 40743983
Activation of the AKT-mTOR pathway confers selpercatinib resistance in thyroid cancer cells harboring the CCDC6-RET fusion gene [ Biochem Biophys Rep, 2025, 43:102136]	PubMed: 40688508
Loss of tumor suppressor TMEM127 drives RET-mediated transformation through disrupted membrane dynamics [ Elife, 2024, 12RP89100]	PubMed: 38687678
Novel therapeutic strategies targeting bypass pathways and mitochondrial dysfunction to combat resistance to RET inhibitors in NSCLC [ Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249]	PubMed: 38768929
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Loss of Tumour Suppressor TMEM127 Drives RET-mediated Transformation Through Disrupted Membrane Dynamics [ bioRxiv, 2023, 2023.06.28.546955]	PubMed: 37425958
Novel Calcium-Binding Ablating Mutations Induce Constitutive RET Activity and Drive Tumorigenesis [ Cancer Res, 2022, 82(20):3751-3762]	PubMed: 36166639
CIC-mediated modulation of MAPK signaling opposes receptor tyrosine kinase inhibitor response in kinase-addicted sarcoma [ Cancer Res, 2022, canres.1397.2021]	PubMed: 35074756

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。