Sapanisertib (MLN0128, INK-128)

製品コードS2811 バッチS281101

化学情報

	Synonyms	INK 128,TAK-228	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₅H₁₅N₇O
	分子量	309.33	CAS No.	1224844-38-5
Solubility (25°C)*	体外	DMSO	62 mg/mL (200.43 mM)
		Ethanol	2 mg/mL (6.46 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	Sapanisertib (MLN0128, INK 128, TAK-228)は、細胞フリーアッセイにおいて1 nMのIC50を示す強力かつ選択的なmTOR阻害剤であり、クラスI PI3Kアイソフォームに対しては200倍以上効力が低く、mTORC1/2の阻害に優れ、プロ浸潤遺伝子に感受性を示します（Rapamycinと比較して）。現在フェーズ1です。
in vitro	INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors.
in vivo	In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models.

製品説明

Sapanisertib (MLN0128, INK 128, TAK-228)は、細胞フリーアッセイにおいて1 nMのIC50を示す強力かつ選択的なmTOR阻害剤であり、クラスI PI3Kアイソフォームに対しては200倍以上効力が低く、mTORC1/2の阻害に優れ、プロ浸潤遺伝子に感受性を示します（Rapamycinと比較して）。現在フェーズ1です。

in vitro

INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases.

As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors.

in vivo

In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day.

Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	1.4 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Nude mice
	投薬量	0.3 and 1 mg/kg
	投与方法	o.g.

参考

https://pubmed.ncbi.nlm.nih.gov/20622997/
http://mct.aacrjournals.org/cgi/content/meeting_abstract/8/12_MeetingAbstracts/B148
https://pubmed.ncbi.nlm.nih.gov/22367541/

カスタマーフィードバック

: Data from [Data independently produced by Biochem Biophys Res Commun, 2013, 440(4), 701-6]

: , , Antonino Maria Spart from University of Bologn

: ,

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：

Enhancing immunotherapy through PD-L1 upregulation: the promising combination of anti-PD-L1 plus mTOR inhibitors [ Mol Oncol, 2025, 19(1):151-172]	PubMed: 39258533
Uncoupling of Akt and mTOR signaling drives resistance to Akt inhibition in PTEN loss prostate cancers [ Sci Adv, 2025, 11(6):eadq3802]	PubMed: 39919177
A TFEB-TGFβ axis systemically regulates diapause, stem cell resilience and protects against a senescence-like state [ Nat Aging, 2025, 5(7):1340-1357]	PubMed: 40588651
PI3K/mTOR inhibition induces tumour microenvironment remodelling and sensitises pS6high uterine leiomyosarcoma to PD-1 blockade [ Clin Transl Med, 2024, 14(5):e1655]	PubMed: 38711203
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728]	PubMed: 39264808
NFκB and JNK pathways mediate metabolic adaptation upon ESCRT-I deficiency [ Cell Mol Life Sci, 2024, 81(1):458]	PubMed: 39560723
Different Impacts of DNA-PK and mTOR Kinase Inhibitors in Combination with Ionizing Radiation on HNSCC and Normal Tissue Cells [ Cells, 2024, 13(4)304]	PubMed: 38391917
PI3K-dependent reprogramming of hexokinase isoforms controls glucose metabolism and functional responses of B lymphocytes [ iScience, 2024, 27(10):110939]	PubMed: 39635128
Epstein-Barr Virus Latent Membrane Protein 2A (LMP2A) Enhances ATP Production in B Cell Tumors through mTOR and HIF-1α [ Int J Mol Sci, 2024, 25(7)3944]	PubMed: 38612754
The highly selective and oral phosphoinositide 3-kinase delta (PI3K-δ) inhibitor roginolisib induces apoptosis in mesothelioma cells and increases immune effector cell composition [ Transl Oncol, 2024, 43:101857]	PubMed: 38412661

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。