Sitravatinib (MGCD516)

製品コードS8573 バッチS857303

印刷

化学情報

Synonyms

MG-516

Storage
(From the date of receipt)

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

化学式

C₃₃H₂₉F₂N₅O₄S

分子量

629.68

CAS No.

1123837-84-2

Solubility (25°C)*

体外

DMSO

100 mg/mL (158.81 mM)

Ethanol

5 mg/mL (7.94 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。	5.000mg/ml (7.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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。	0.830mg/ml (1.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 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	Sitravatinib (MGCD516, MG-516)は、c-Kit、PDGFRβ、PDGFRα、c-Met、Axlなど、肉腫細胞の増殖を促進する複数のRTKを標的とする新規低分子阻害剤です。
in vitro	Sitravatinib (MGCD516) is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL. Treatment with this compound resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.
in vivo	Sitravatinib (MGCD516) has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of its targets, including rearrangement of RET, NTRK, or CHR4q12 amplification. Treatment of tumor xenografts in vivo with this compound resulted in significant suppression of tumor growth.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	DDLS, LS141 and MPNST
	濃度	62.5, 125, 250, 500, 1000, 2000 nM/L
	反応時間	72 h
	実験の流れ	Sitravatinib (MGCD516) was used to treat 2,000-3,000 cells plated in 96-well plates in RPMI/DME media with 10% FBS the next day. After 72 hours, media was replaced with 100 μL of media with 10% serum and 10% CCK-8 solution. After 1 hour, the optical density was read at 450 nm to determine viability. Background values from negative control wells without cells were subtracted for final sample quantification. Data was plotted as % cell viability compared to DMSO control. IC50 was extrapolated from cell viability data using CompuSyn software according to the manufacturer's instructions.
動物実験	動物モデル	ICR/SCID mice
	投薬量	15 mg/kg
	投与方法	p.o.

参考

http://www.jto.org/article/S1556-0864(16)32735-6/pdf
https://pubmed.ncbi.nlm.nih.gov/26675259/

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：

Exploiting collateral sensitivity in the evolution of resistance to tyrosine kinase inhibitors in soft tissue sarcomas [ Commun Biol, 2025, 8(1):1185]	PubMed: 40781553
KinoViz: A User-Friendly Web Application for High-Throughput Kinome Profiling Analysis and Visualization in Cancer Research [ Res Sq, 2025, rs.3.rs-6431257]	PubMed: 40630533
An in vivo model of glioblastoma radiation resistance identifies long non-coding RNAs and targetable kinases [ JCI Insight, 2022, e148717]	PubMed: 35852875
SMARCA4 Depletion Induces Cisplatin Resistance by Activating YAP1-Mediated Epithelial-to-Mesenchymal Transition in Triple-Negative Breast Cancer [ Cancers (Basel), 2021, 13(21)5474]	PubMed: 34771636
Sitravatinib Sensitizes ABCB1- and ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs. [ Cancers (Basel), 2020, 12(1)]	PubMed: 31941029
Exploring the Roles of Long Non-Coding RNAs in Glioblastoma Tumor Recurrence and Therapy Resistance [ ProQuest, 2020, 28258447]	PubMed: None
Blockade of AXL activation overcomes acquired resistance to EGFR tyrosine kinase inhibition in non-small cell lung cancer [ Transl Cancer Res, 2019, 8(6):2425-2438]	PubMed: 35116995

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。