SF2523

製品コードS8589 バッチS858901

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

C₁₉H₁₇NO₅S

分子量

371.41

CAS No.

1174428-47-7

Solubility (25°C)*

体外

DMSO

29 mg/mL (78.08 mM)

Ethanol

7 mg/mL (18.84 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.

* <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	SF2523は、PI3Kα、PI3Kγ、DNA-PK、BRD4、mTORに対してそれぞれ34 nM、158 nM、9 nM、241 nM、280 nMのIC50値を持つ、PI3Kの非常に選択的かつ強力な阻害剤です。
in vitro	SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2. It blocks M1-M2 transition and decreases levels of p-AKT, N-MYC in several neuroblastoma cell lines. This compound treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473. It interacts robustly with the full-length BRD4 (Kd = 140 nM) and exhibits comparable affinity to the BRD4 first BD (BD1) (Kd =150 nM), however it binds more weakly to the second BD (BD2) of BRD4 (Kd = 710 nM). Comparison of binding affinities of this chemical for BDs of other proteins reveals that it binds equally well to BDs of BRD4, BRD2, and BRD3; shows moderate binding to BDs of CECR2 and BRDT; but associates much weaker with other BDs.
in vivo	SF2523 blocks spontaneous metastasis and tumor growth. This compound has demonstrated animal efficacy results without toxicity in the following 4 animal models: orthotopic pancreatic model, multiple myeloma model, renal cell carcinoma model, neuroblastoma xenograft model. It targets PI3K-driven and BRD4-driven oncogenic pathways in vivo. It is less toxic to the host organism in vivo than a combination of an equipotent PI3K inhibitor and BRD4 inhibitor.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	neuroblastoma SKNBE2 cell line
	濃度	5 μM
	反応時間	24 h
	実験の流れ	SKNBE2 cells are serum-starved for 4 h, stimulated with 50 ng/mL IGF, and treated with 1 μM JQ1, 5 μM SF2523, 10 μM this compound, 1 μM BKM120, 1 μM BEZ235, or 200 nM CAL101 for 24 h. Then, cells are harvested and total RNA is extracted; Perform RT-PCR.
動物実験	動物モデル	Nude mice (8-wk old, female, NSG) with xenografted tumor
	投薬量	50 mg/kg
	投与方法	i.p.

参考

http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b00438
http://cancerres.aacrjournals.org/content/76/14_Supplement/LB-211.short
https://pubmed.ncbi.nlm.nih.gov/28137841/

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：

MDM2 antagonists promote CRISPR/Cas9-mediated precise genome editing in sheep primary cells [ Mol Ther Nucleic Acids, 2023, 31:309-323]	PubMed: 36726409
Kynurenine produced by tryptophan 2,3-dioxygenase metabolism promotes glioma progression through an aryl hydrocarbon receptor-dependent signaling pathway [ Cell Biol Int, 2022, 10.1002/cbin.11833]	PubMed: 35702760
Dual inhibition of BRD4 and PI3K-AKT by SF2523 suppresses human renal cell carcinoma cell growth. [ Oncotarget, 2017, 8(58):98471-98481]	PubMed: 29228703

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。