DT-061 (SMAP)

製品コードS8774 バッチS877401

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₂₃F₃N₂O₅S

分子量

520.52

CAS No.

1809427-19-7

Solubility (25°C)*

体外

DMSO

100 mg/mL (192.11 mM)

Ethanol

50 mg/mL (96.05 mM)

Water

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.250mg/ml (2.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.800mg/ml (1.54mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	DT-061 (SMAP) is a bioavailable PP2A activator. It decreases cell viability in HCC827 and HCC3255 cell lines, with IC50 values of 14.3 μM and 12.4 μM respectively.
in vivo	PP2A reactivation using single agent SMAP DT-061 is a well-tolerated and orally bioavailable therapeutic strategy that is as efficacious as a combination of kinase inhibitors in antagonizing EGFR-driven TKI-resistant LUAD models.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HCC827 and H3255 cell lines
	濃度	2.5, 5, 7.5, 10, 12.5, 15, 17.5, or 20 μM
	反応時間	48 h
	実験の流れ	Cells are treated with DMSO control or 2.5, 5, 7.5, 10, 12.5, 15, 17.5, or 20 μM SMAP DT-061 for 48 hours.
動物実験	動物モデル	A TKI-resistant EGFR(L858R) patient-derived xenograft (PDX) model (NSG female mice)
	投薬量	5 mg/kg
	投与方法	by oral gavage

参考

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6478418/

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：

AKR1B10 dictates c-Myc stability to suppress colorectal cancer metastasis via PP2A nitration [ Sci Adv, 2025, 11(34):eadv6937]	PubMed: 40845116
14-3-3 binding motif phosphorylation disrupts Hdac4-organized condensates to stimulate cardiac reprogramming [ Cell Rep, 2024, 43(4):114054]	PubMed: 38578832
LincR-PPP2R5C Promotes Th2 Cell Differentiation Through PPP2R5C/PP2A by Forming an RNA-DNA Triplex in Allergic Asthma [ Allergy Asthma Immunol Res, 2024, 16(1):71-90]	PubMed: 38262392
LincR-PPP2R5C Deficiency Alleviates Airway Remodeling by Inhibiting Epithelial-Mesenchymal Transition Through the PP2A/TGF-β1 Signaling Pathway in Chronic Experimental Allergic Asthma [ Allergy Asthma Immunol Res, 2024, 16(4):422-433]	PubMed: 39155740
Protocol for in vitro observation of HDAC4 condensation during induced cardiac reprogramming [ STAR Protoc, 2024, 6(1):103523]	PubMed: 39705143
A transcriptional network governing ceramide homeostasis establishes a cytokine-dependent developmental process [ Nat Commun, 2023, 10.1038/s41467-023-42978-w]	PubMed: 37945603
Carboxypeptidase A4 negatively regulates HGS-ETR1/2-induced pyroptosis by forming a positive feedback loop with the AKT signalling pathway [ Cell Death Dis, 2023, 14(12):793]	PubMed: 38049405
A Wnt-induced lncRNA-DGCR5 splicing switch drives tumor-promoting inflammation in esophageal squamous cell carcinoma [ Cell Rep, 2023, 42(6):112542]	PubMed: 37210725
LCK-Mediated RIPK3 Activation Controls Double-Positive Thymocyte Proliferation and Restrains Thymic Lymphoma by Regulating the PP2A-ERK Axis [ Adv Sci (Weinh), 2022, e2204522]	PubMed: 36161785
GSK3β is a critical, druggable component of the network regulating the active NOTCH1 protein and cell viability in CLL [ Cell Death Dis, 2022, 13-9:755]	PubMed: 36050315

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。