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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-E7449
E7449

Chemical Structure : E7449

CAS No.: 1140964-99-3

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E7449 (Stenoparib, E-7449, 2X-121)

货号: PC-43025Not For Human Use, Lab Use Only.

E7449 (2X-121) is a potent, orally bioavailable, brain penetrable dual inhibitor of PARP1/2 and TNKS1/2 with IC50 of 2.0/1.0 nM (PARP1/2), 50-100 nM (TNKS1/2).

规格 价格 库存 数量
5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

E7449 (Stenoparib, 2X-121) is a potent, orally bioavailable, brain penetrable dual inhibitor of PARP1/2 and TNKS1/2 with IC50 of 2.0/1.0 nM (PARP1/2), 50-100 nM (TNKS1/2).
E7449 (Stenoparib, 2X-121) displays no significant inhibitory activity for PARP3 or PARPs6-16.
E7449 (Stenoparib, 2X-121) shows sensitivity to cells deficient in DNA repair pathways beyond homologous recombination, inhibits Wnt/β-catenin signaling in colon cancer cell lines, stabilizes axin and TNKS proteins resulting in β-catenin de-stabilization and significantly alters expression of Wnt target genes.
E7449 (Stenoparib, 2X-121) potentiates antitumor activity of chemotherapies temozolomide and carboplatin both in vitro and in vivo.

物理化学性质&存储条件

分子量 317.3446
分子式 C18H15N5O
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

DMSO: < 6.96 mg/mL
Chemical Name/SMILES

3H-Pyridazino[3,4,5-de]quinazolin-3-one, 8-[(1,3-dihydro-2H-isoindol-2-yl)methyl]-1,2-dihydro-

参考文献

1. McGonigle S, et al. Oncotarget. 2015 Dec 1;6(38):41307-23.
2. Sharon McGonigle, et al. Abstract 4688: E7449: A novel PARP inhibitor enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors . Cancer Research: April 15, 2012; Volume 72, Issue 8, Su

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