SAR131675

製品コードS2842 バッチS284209

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

C₁₈H₂₂N₄O₄

分子量

358.39

CAS No.

1433953-83-3

Solubility (25°C)*

体外

DMSO

72 mg/mL (200.89 mM)

Water

Insoluble

Ethanol

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。	10.000mg/ml (27.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 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.

* <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	SAR131675 is a VEGFR3 inhibitor with IC50/K_i of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.
in vitro	SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20 nM. This compound dose dependently inhibits rh-VEGFR-3–TK activity with an IC50 of 23 nM. It inhibits VEGR-3–TK activity with a K_i of about 12 nM. It inhibits VEGFR-1–TK activity with an IC50 of > 3 μM and VEGFR-2–TK activity with an IC50 of 235 nM. It inhibits VEGFR-1 autophosphorylation with an IC50 of about 1 μM and VEGFR-2 with an IC50 of about 280 nM. It moderately inhibits VEGFR-2 and has very little effect on VEGFR-1, showing a good selectivity for VEGFR-3. It inhibits VEGFA-induced VEGFR-2 phosphorylation in a dose-dependent manner, with an IC50 of 239 nM. It potently inhibits lymphatic cell survival induced by VEGFC and VEGFD with IC50 of 14 nM and 17 nM, respectively. It inhibits VEGFA-induced survival with an IC50 of 664 nM. It significantly and dose dependently inhibits VEGFC-induced Erk phosphorylation, with an IC50 of about 30 nM. ^[1]
in vivo	In embryonic angiogenesis using the zebrafish model, SAR131675 efficiently impaires embryonic vasculogenesis. This compound at 100 mg/kg/d has significantly reduced the levels of VEGFR-3 and hemoglobin content by about 50%. It efficiently abrogates lymphangiogenesis and angiogenesis induced in vivo by FGF2. This chemical at a dose of 300 mg/kg is able to inhibit both VEGFR-2 and VEGFR-3 signaling. In the prevention study, 5 weeks treatment with this compound is well tolerated and the number of angiogenic islets in the pancreas of SAR131675-treated mice is significantly decreased by 42%, compared with the vehicle-treated group. In the intervention study, daily oral administration of this chemical from week 10 to week 12.5 causes a significant decrease in tumor burden by 62%. Treatment with it significantly reduces the tumor volume 24% and 50% at 30 mg/kg/d and 100 mg/kg/d, respectively. ^[1]
特徴	A potent and selective VEGFR-3–tyrosine kinase inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ	Tyrosine kinase assay
キナーゼアッセイ	Multiwell plates are precoated with a synthetic polymer substrate poly-Glu-Tyr (polyGT 4:1). The reaction is carried out in the presence of kinase buffer (10 ×: 50 mM HEPES buffer, pH 7.4, 20 mM MgCl₂, 0.1 mM MnCl₂, and 0.2 mM Na₃VO₄) supplemented with ATP and dimethyl sulfoxide (DMSO) for the positive control (C⁺) or SAR131675 (ranging from 3 nM–1,000 nM). ATP is used at 30 μM for VEGFR-1 and VEGFR-3 and at 15 μM for VEGFR-2. The phosphorylated poly-GT is probed with a phosphotyrosine specific monoclonal antibody (mAb) conjugated to horseradish peroxidase (HRP; 1/30,000) and developed in the dark with the HRP chromogenic substrate (OPD). The reaction is then stopped by the addition of 100 μL 1.25 M H₂SO₄, and absorbance is determined using an Envision spectrophotometer at 492 nm.
細胞アッセイ	細胞株	HEK cells
	濃度	20 nM
	反応時間	30 minutes
	実験の流れ	Cells were treated with various concentrations of SAR131675.
動物実験	動物モデル	BALB/c mice with 4T1 cells
	投薬量	30 mg/kg/d, 100 mg/kg/d, and 300 mg/kg/d
	投与方法	Oral

参考

https://pubmed.ncbi.nlm.nih.gov/22584122/

カスタマーフィードバック

: , , Neuroscience, 2015, 290C:90-102.

: Data from [Data independently produced by , , Clin Exp Metastasis, 2015, 32(8):789-98]

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 472(1):182-8.]

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：

Inhibition of VEGFR-3 by SAR131675 decreases renal inflammation and lymphangiogenesis in the murine lupus nephritis model [ Cell Death Discov, 2025, 11(1):320]	PubMed: 40651955
Vegfr3 activation of Pkd2l1+ CSF-cNs triggers the neural stem cell response in spinal cord injury [ Cell Signal, 2025, 130:111675]	PubMed: 39986360
Compensatory lymphangiogenesis is required for edema resolution in zebrafish [ Sci Rep, 2025, 15(1):8177]	PubMed: 40065081
Piezo1 regulates meningeal lymphatic vessel drainage and alleviates excessive CSF accumulation [ Nat Neurosci, 2024, 10.1038/s41593-024-01604-8]	PubMed: 38528202
Fibroblasts facilitate lymphatic vessel formation in transplanted heart [ Theranostics, 2024, 14(5):1886-1908]	PubMed: 38505621
VEGFD signaling balances stability and activity-dependent structural plasticity of dendrites [ Cell Mol Life Sci, 2024, 81(1):354]	PubMed: 39158743
Lack of RAMP1 Signaling Suppresses Liver Regeneration and Angiogenesis Following Partial Hepatectomy in Mice [ In Vivo, 2024, 38(5):2261-2270]	PubMed: 39187322
VEGFR-3 signaling restrains the neuron-macrophage crosstalk during neurotropic viral infection [ Cell Rep, 2023, 42(5):112489]	PubMed: 37167063
Rotator cuff healing is regulated by the lymphatic vasculature [ J Orthop Translat, 2023, 38:65-75]	PubMed: 36313978
SAR131675 exhibits anticancer activity on human ovarian cancer cells through inhibition of VEGFR-3/ERK1/2/AKT signaling pathway [ Cell Signal, 2023, 111:110856]	PubMed: 37598918

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。