Taladegib (LY2940680)

製品コードS2157 バッチS215702

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₂₄F₄N₆O

分子量

512.5

CAS No.

1258861-20-9

Solubility (25°C)*

体外

DMSO (warmed with 60ºC water bath)

75 mg/mL (146.34 mM)

Ethanol

27 mg/mL (52.68 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。	3.75mg/ml (7.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 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。	0.54mg/ml (1.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.8 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	Taladegib (LY2940680) は Smoothened (Smo) 受容体に結合し、Hedgehog (Hh) シグナル伝達を強力に阻害します。第1/2相。
in vitro	Taladegib (LY2940680) inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patients with cancer who developed resistance to vismodegib.
in vivo	Taladegib (LY2940680) has excellent pharmacokinetic properties in rodent and non-rodent species. When administered orally to Ptch^+/- p53^-/- transgenic mice which spontaneously develop medulloblastoma, it produces remarkable efficacy and significantly improves their survival. This compound reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. It inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity.

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/22007748/
http://cancerres.aacrjournals.org/cgi/content/meeting_abstract/71/8_MeetingAbstracts/2819?si

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：

Sensitivity of Human Intrahepatic Cholangiocarcinoma Subtypes to Chemotherapeutics and Molecular Targeted Agents: A Study on Primary Cell Cultures [ PLOS One, November 16, 2015, e0142124]	PubMed: nan
New Ameloblastoma Cell Lines Enable Preclinical Study of Targeted Therapies [ Journal of Dental Research, 2022, 1517-1525]	PubMed: 35689405
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7]	PubMed: 34997030
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004]	PubMed: 31740922
L-4, a Well-Tolerated and Orally Active Inhibitor of Hedgehog Pathway, Exhibited Potent Anti-tumor Effects Against Medulloblastoma in vitro and in vivo. [ Front Pharmacol, 2019, 10:89]	PubMed: 30846937
DRUGPATH - a novel bioinformatic approach identifies DNA-damage pathway as a regulator of size maintenance in human ESCs and iPSCs [ Sci Rep, 2019, 9(1):1897]	PubMed: 30760778
MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. [Hoch L, et al. FASEB J, 2015, 29(5):1817-29]	PubMed: 25636740

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。