SKLB4771 (FLT3-IN-1)

製品コードS1099 バッチS109901

印刷

化学情報

Chemical Structure 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. It significantly slows down tumor growth at doses of 20 mg/kg/d and 40 mg/kg/d, with tumor inhibition rates of 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity are observed for all of the SKLB4771-treated mice. The tumor tissues from the SKLB4771-treated groups show significantly fewer Ki67(tumor mitotic index)-positive cells. The TUNEL data shows an obvious increase in the percentage of apoptotic cells in a time-dependent manner.[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 as follows: the leukemia cells are seeded in a 96-well plate at 1−4 × 104 cells per well, and an equal volume of medium containing increasing concentrations of this compound is 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 it 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

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。

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