|3-(2,3-二羟基苯并[b][1,4]二氧杂环己烷基-6-基)-5-吗啉-7H-噻吩[3,2-b]吡喃-7-酮|CsnPharm

CAS No.: 1174428-47-7

SF2523 Catalog No. CSN22559

Synonyms: Sf2523

SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The phosphatidylinositol 3-kinase (PI3K) pathway is a major focus for drug development in various cancer due to its function as a key regulator of cell growth and survival. The bromodomain and extraterminal domain (BET) family of epigenetic “reader” proteins, including BRDT, BRD2, BRD3, and BRD4, play important roles in histone acetylation-dependent transcriptional regulation. SF2523 is a highly selective and potent inhibitor of PI3K with IC₅₀s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively^[1]. In vitro, SF2523 decreased LPS- or IL4-induced MΘ polarization. At 500 nM, SF2523 significantly decreased mRNA expression of IL6 and iNos in LPS induced Bone marrow–derived macrophages (BMDMs) and gene expression of Arg, Tgfb, Vegf, Mmr, Ym1, and Fizz1 in IL4-induced BMDMs^[2]. In vivo, s.c. xenograft model of MYCN-amplified neuroblastoma in immunocompromised mice treated with SF2523 (50 mg/kg, three times a week) showed a significant reduction of tumor volume compared with vehicle-treated group, without gross toxicity^[1].
作用机制The structure of the BRD4 BD1–SF2523 complex reveals a characteristic four-helix bundle fold of BD1, with SF2523 occupying a deep hydrophobic pocket at one of the open ends of the bundle.
参考文献

[1] Andrews FH, Singh AR, Joshi S, Smith CA, Morales GA, Garlich JR, Durden DL, Kutateladze TG. Dual-activity PI3K-BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080. doi: 10.1073/pnas.1613091114. Epub 2017 Jan 30. PMID: 28137841; PMCID: PMC5320964.
[2] Joshi S, Singh AR, Liu KX, Pham TV, Zulcic M, Skola D, Chun HB, Glass CK, Morales GA, Garlich JR, Durden DL. SF2523: Dual PI3K/BRD4 Inhibitor Blocks Tumor Immunosuppression and Promotes Adaptive Immune Responses in Cancer. Mol Cancer Ther. 2019 Jun;18(6):1036-1044. doi: 10.1158/1535-7163.MCT-18-1206. Epub 2019 Apr 24. PMID: 31018997; PMCID: PMC6893301.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6925 mL
- 13.4623 mL
- 26.9246 mL
- 5 mM
- 0.5385 mL
- 2.6925 mL
- 5.3849 mL
- 10 mM
- 0.2692 mL
- 1.3462 mL
- 2.6925 mL

技术信息

CAS号

1174428-47-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H17NO5S

运输

蓝冰

分子量

371.41

别名

Sf2523

溶解度

DMSO	28.0 mg/mL (75.4 mM)
Water	Insoluble
Ethanol	7.0 mg/mL (18.8 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

SF2523 Catalog No. CSN22559

靶点选择性

请登录您的专属账户

确认信息