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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-CCT361814
CCT361814

Chemical Structure : CCT361814

CAS No.: 1693734-80-3

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CCT361814 (NXP800, CCT 361814, NXP 800)

货号: PC-73319Not For Human Use, Lab Use Only.

CCT361814 (NXP800) is a potent, selective and orally bioavailable inhibitor of HSF1 pathway with IC50 of 94 nM (SK-OV-3, HSP72 cell-based ELISA).

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5 mg ￥1980 In stock
10 mg ￥2980 In stock
25 mg ￥4980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CCT361814 (NXP800) is a potent, selective and orally bioavailable inhibitor of HSF1 pathway with IC50 of 94 nM (SK-OV-3, HSP72 cell-based ELISA).
CCT361814/NXP800 exhibits excellent antiproliferative activity against human ovarian cancer cells with IC50 of 8.5 nM.
CCT361814/NXP800 displays clean selectivity in the Cerep in vitro safety screen of 87 potentially high-risk off-target proteins, with one exception adenosine A2A receptor (IC50=2 uM).
CCT361814/NXP800 displayed good mouse oral bioavailability (42%) from moderate total blood clearance (CLtb = 10 mL/min/kg, extraction ratio = 11%, Fmax = 89%).
CCT361814/NXP800 increased expression of CHAC1 mRNA and reduced expression of HSPA1A mRNA, which represent useful PD markers both in vivo tumor samples and in vitro. 
CCT361814/NXP800 (35 mg/kg po qd) exhibits tumor growth inhibition (TGI) of 120% in SK-OV-3 human ovarian cancer solid tumor xenografts.

物理化学性质&存储条件

分子量 569.637
分子式 C32H32FN5O4
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-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-fluorophenyl)-2-((4-ethylpiperazin-1-yl)methyl)quinoline-6-carboxamide

参考文献

1. A Elisa Pasqua, et al. J Med Chem. 2023 Apr 5.

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