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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-DBK-1154
DBK-1154

Chemical Structure : DBK-1154

CAS No.: 1809068-70-9

DBK-1154 (SMAP-2, DT-1154, DBK1154)

货号: PC-62749Not For Human Use, Lab Use Only.

SMAP-2 (DT-1154, DBK1154) is an orally bioavailable small molecule activator of PP2A, binds to PP2A Aα scaffold subunit and inhibits KRAS-driven tumor growth both in vitro and in vivo.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SMAP-2 (DT-1154, DBK1154) is an orally bioavailable small molecule activator of PP2A, binds to PP2A Aα scaffold subunit and inhibits KRAS-driven tumor growth both in vitro and in vivo.
SMAP-2 (DT-1154, DBK1154) decreases cellular viability and clonogenicity and induces apoptosis in castrate-resistant prostate cancer (CRPC) cells.
SMAP-2 (DT-1154, DBK1154) significantly changes the phosphoproteome, including dephosphorylation of full-length and truncated isoforms of the AR and downregulation of its regulatory kinases.
SMAP-2 (DT-1154, DBK1154) exhibits efficacy comparable to enzalutamide in vivo.

物理化学性质&存储条件

分子量 532.578
分子式 C27H27F3N2O4S
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

N-((1S,2S,3R)-3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-2-hydroxycyclohexyl)-4-(trifluoromethoxy)benzenesulfonamide

参考文献

1. Sangodkar J, et al. J Clin Invest. 2017 Jun 1;127(6):2081-2090.

2. McClinch K, et al. Cancer Res. 2018 Jan 22. pii: canres.0123.2017.

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