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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-SRX3262
SRX3262

Chemical Structure : SRX3262

CAS No.: 2409965-28-0

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SRX3262 (SRX 3262, SRX-3262 )

货号: PC-73384Not For Human Use, Lab Use Only.

SRX3262 (SRX 3262, SRX 3262) is a potent, triple action BTK, PI3K and BRD4 inhibitor with potency against BTK (IC50=35 nM), PI3Kδ (IC50=16 nM), PI3Kα (IC50=64 nM), and both bromodomains of BRD4 (IC50 BD1=228 nM, IC50 BD2=348 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SRX3262 (SRX 3262) is a potent, triple action BTK, PI3K and BRD4 inhibitor with potency against BTK (IC50=35 nM), PI3Kδ (IC50=16 nM), PI3Kα (IC50=64 nM), and both bromodomains of BRD4 (IC50 BD1=228 nM, IC50 BD2=348 nM).
SRX3262 shows dose-dependent antiproliferative activity in MCL cell lines with IC50 of 0.62 μM, 0.13 μM, and 1.2 μM for JeKo-1, Mino, and Ibrutinib-resistant Granta cells, respectively.
SRX3262 simultaneously blocks three interrelated MCL driver pathways: BTK, PI3K-AKT-mTOR and MYC.
SRX3262 concomitantly binds to BTK, PI3K, and BRD4, exhibits potent in vitro and in vivo activity against MCL, and overcomes the Ibrutinib resistance resulting from the BTK-C481S mutation.
SRX3262 inhibits IgM-induced BTK and AKT phosphorylation and abrogates binding of BRD4 to MYC loci.
SRX3262 promotes c-MYC destabilization, induces cell cycle arrest and apoptosis, and shows antitumor activity in in vivo xenograft models.

物理化学性质&存储条件

分子量 424.47
分子式 C22H20N2O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(4-acryloyl-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-5-morpholino-7H-thieno[3,2-b]pyran-7-one

参考文献

1. Dhananjaya Pal, et al. iScience. 2021 Jul 30;24(9):102931.

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