SKLB4771 (FLT3-IN-1)

製品コードS1099 バッチS109901

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₂₇N₇O₃S₂

分子量

537.66

CAS No.

1370256-78-2

Solubility (25°C)*

体外

DMSO

50 mg/mL (92.99 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.

* <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	SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10 nM.
in vitro	SKLB4771 (FLT3-IN-1) just weakly inhibits Aurora A, FMS, FLT4, and c-Kit (IC50s: 1.5 μM, 2.8 μM, 3.7 μM, and 6.8 μM, respectively). It displays almost no inhibitory activity against the other 13 selected protein kinases. This compound potently inhibits the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibits very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt’s lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively).^[1].
in vivo	In the MV4-11 xenograft model, treatment with SKLB4771 (FLT3-IN-1) at 100 mg/kg/d results in rapid and complete tumor regression in all mice of this group. At doses of 20 mg/kg/d and 40 mg/kg/d, it significantly slows down tumor growth, with inhibition rates of 66% and 84%, respectively. Throughout the experiment, no significant weight loss or other obvious signs of toxicity were observed in any of the treated mice. Tumor tissues from groups receiving this compound showed significantly fewer Ki67 (tumor mitotic index)-positive cells. TUNEL data indicated a time-dependent increase in the percentage of apoptotic cells.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MV4−11, K562, U937, Jurkat, Ramos, Karpas299, HCC827, A549, H2228, H820, PC-9, H292, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, SH-SY5Y
	濃度	increasing concentrations
	反応時間	72 h
	実験の流れ	SKLB4771 (FLT3-IN-1) is evaluated by seeding leukemia cells in a 96-well plate at 1–4 × 10⁴ cells per well, with an equal volume of medium containing increasing concentrations of this compound added to each well. At the end of the incubation period (72 h at 37 °C), 20 μL of 5 mg/mL MTT reagent is added per well for 2–4 h of incubation, and 50 μL of 20% acidified SDS per well is used to lyse the cells. The other cell lines are seeded in 96-well plates at a density of 2–5 × 10³ cells/well for 24 h followed by replacement of the medium with serial dilutions of the inhibitor in culture medium. Following a 72-h incubation, the MTT reagent is added for a 2–4-h incubation, and 100% DMSO is used to dissolve the cells.
動物実験	動物モデル	female NOD-SCID mouse (6−7 weeks old)
	投薬量	20 mg/kg, 40 mg/kg, 100 mg/kg
	投与方法	IV

参考

https://pubmed.ncbi.nlm.nih.gov/22452518/

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：

Atractylenolide-1 Targets FLT3 to Regulate PI3K/AKT/HIF1-α Pathway to Inhibit Osteogenic Differentiation of Human Valve Interstitial Cells [ Front Pharmacol, 2022, 13:899775]	PubMed: 35571096

Atractylenolide-1 Targets FLT3 to Regulate PI3K/AKT/HIF1-α Pathway to Inhibit Osteogenic Differentiation of Human Valve Interstitial Cells [ Front Pharmacol, 2022, 13:899775]

PubMed: 35571096

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。