SKLB1002

製品コードS7258 バッチS725802

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	C₁₃H₁₂N₄O₂S₂
	分子量	320.39	CAS No.	1225451-84-2
Solubility (25°C)*	体外	DMSO	4 mg/mL (12.48 mM)
		Water	Insoluble
		Ethanol	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	SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
in vitro	SKLB1002 shows strikingly lower cytotoxicity on normal human cells L-02. SKLB1002 significantly inhibits HUVEC proliferation, migration, invasion, and tube formation, by inhibiting VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including ERK, FAK, and Src. ^[1]
in vivo	In the zebrafish embryos, SKLB1002 remarkably blocks the formation of embryonic and tumor-induced angiogenesis with no or least impact on normal cell proliferation. In athymic mice bearing SW620 or HepG2 xenografts, SKLB1002 (100 mg/kg daily, i.p.) causes significant inhibition of tumor growth, inhibits tumor angiogenesis and induces tumor apoptosis. ^[1] In 4T1 and CT26 tumor model, SKLB1002 and local hyperthermia produce a synergistic antiangiogenesis, anticancer and promotion of apoptosis efficacy. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase inhibition assays
キナーゼアッセイ	Kinase inhibition is measured by the use of radiometric assays conducted by Kinase Profiler service. Briefly, in the presence or absence of SKLB1002, VGFR2 (5–10 mU) is incubated in 25-μL reaction solution containing 8 mmol/L 3-(N-morpholino)propanesulfonic acid (MOPS), pH 7.0, 0.2 mmol/L EDTA, 0.33 mg/mL myelin basic protein, 10 mmol/L Mg acetate, and γ-[³³P]ATP. After incubation for 40 minutes at room temperature, the reaction is stopped and 10 μL of the reaction solution is then spotted onto a P30 filtermat and washed 3 times for 5 minutes in 75 mmol/L phosphoric acid and once in methanol prior to scintillation counting.
細胞アッセイ	細胞株	HUVECs, L-02, B16-F10, HepG2, and SW620 cells.
	濃度	~40 μM
	反応時間	24 hours
	実験の流れ	Cell proliferation is measured using MTT assay. Various cells including HUVECs, L-02, B16-F10, HepG2, and SW620 are treated with indicated concentrations of SKLB1002 for 24 hours. Vandetanib and sunitinib serve as positive controls. Each assay is replicated 3 times.
動物実験	動物モデル	Mice bearing SW620 or HepG2 tumors.
	投薬量	~100 mg/kg daily
	投与方法	i.p.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , BMC Cancer, 2017, 17(1):593]

: Data from [Data independently produced by , , BMC Cancer, 2017, 17: 593]

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：

The developing epicardium regulates cardiac chamber morphogenesis by promoting cardiomyocyte growth [ Dis Model Mech, 2023, 16(5)dmm049571]	PubMed: 36172839
Paracrine signaling by VEGF-C promotes non-small cell lung cancer cell metastasis via recruitment of tumor-associated macrophages. [ Exp Cell Res, 2018, 364(2):208-216]	PubMed: 29427623
VEGFR2 regulates endothelial differentiation of colon cancer cells. [Liu Z, et al. BMC Cancer, 2017, 17(1):593]	PubMed: 28854900

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。