TAS-116 (Pimitespib)

製品コードS7716 バッチS771601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₅H₂₆N₈O
	分子量	454.53	CAS No.	1260533-36-5
Solubility (25°C)*	体外	DMSO	91 mg/mL (200.2 mM)
		Ethanol	11 mg/mL (24.2 mM)
		Water	Insoluble
* <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	Pimitespib (TAS-116) は、新規の低分子HSP90阻害剤であり、HSP90α、HSP90β、GRP94、およびTRAP1に対してそれぞれ34.7 nmol/L、21.3 nmol/L、>50,000 nmol/L、および>50,000 nmol/LのKi値でゲルダナマイシン-FITCのHSP90タンパク質への結合を阻害します。さらに、TAS-116はHSP70などの他のATPaseを阻害しません（IC50 >200 μmol/L）。
in vitro	Pimitespib (TAS-116) is a selective inhibitor of cytosolic HSP90α and β that does not inhibit HSP90 paralogs such as endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μmol/L of this compound for 8 hours results in reduced levels of DDR1, which interacts with HSP90α and induction of HSP70, which is a surrogate marker of cytosolic HSP90 inhibition.
in vivo	Oral administration of Pimitespib (TAS-116) leads to tumor shrinkage in human tumor xenograft mouse models accompanied by depletion of multiple HSP90 clients. In a rat model, the antitumor activity of this compound is accompanied by a higher distribution in subcutaneously xenografted NCI-H1975 non-small cell lung carcinoma tumors than in retina. It shows activity against orthotopically transplanted NCI-H1975 lung tumors. Pharmacokinetic profiling in rodent and nonrodent species shows that TAS-116 is orally absorbed and had a bioavailability of almost 100% in mice, 69.0% in rats, and 73.9% in dogs without special formulation. In a HER2-expressing NCI-N87 human gastric cancer xenograft mouse model, chronic administration is tolerable, with the average weight loss in mice not exceeding 10% during the treatment period.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HCT116 cells
	濃度	0.3, 1 and 3 μM
	反応時間	8 hours
	実験の流れ	HCT116 cells are treated with Pimitespib (TAS-116) or 17-AAG for 8 hours. Western blotting is performed by using 10 μg of cell lysate.
動物実験	動物モデル	Six-week-old male BALB/c nude mice subcutaneously implanted with cancer cells
	投薬量	3.6 to 14.0 mg/kg/day
	投与方法	oral

参考

https://pubmed.ncbi.nlm.nih.gov/25416789/

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：

Strong Hsp90α/β Protein Expression in Advanced Primary CRC Indicates Short Survival and Predicts Response to the Hsp90α/β-Specific Inhibitor Pimitespib [ Cells, 2025, 14(11)836]	PubMed: 40498011
Heat shock protein 90 chaperone activity is required for hepatitis A virus replication [ J Virol, 2025, e0050225]	PubMed: 40470959
Heat shock protein 90 chaperone activity is required for hepatitis A virus replication [ J Virol, 2025, 99(7):e0050225]	PubMed: 40470959
Targeting HSP90 with Ganetespib to Induce CDK1 Degradation and Promote Cell Death in Hepatoblastoma [ Cancers (Basel), 2025, 17(8)1341]	PubMed: 40282517
Syringaresinol inhibits cardiorenal fibrosis through HSP90 in a cardiorenal syndrome type 2 [ Hum Exp Toxicol, 2023, 42:9603271231165678]	PubMed: 36960691
Single-cell dissection of the multiomic landscape of high-grade serous ovarian cancer [ Cancer Res, 2022, CAN-21-3819]	PubMed: 35969151

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。

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