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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-RK-287107
RK-287107

Chemical Structure : RK-287107

CAS No.: 2171386-10-8

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RK-287107 (RK287107;RK 287107)

货号: PC-35703Not For Human Use, Lab Use Only.

RK-287107 (RK287107) is a novel potent, tankyrase-specific inhibitor with IC50 of 14.3 and 10.6 nM for tankyrase-1 (TNKS1) and tankyrase-2 (TNKS2) respectively, shows no activity against PARP-1.

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5 mg ￥1580 In stock
10 mg ￥2580 In stock
25 mg ￥4280 In stock
50 mg ￥7280 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

RK-287107 (RK287107) is a novel potent, tankyrase-specific inhibitor with IC50 of 14.3 and 10.6 nM for tankyrase-1 (TNKS1) and tankyrase-2 (TNKS2) respectively, shows no activity against PARP-1.
RK-287107 shows 4-8-fold more potency than G007-LK; causes Axin2 accumulation and downregulates β-catenin, T-cell factor/lymphoid enhancer factor reporter activity and the target gene expression in colorectal cancer cells harboring the shortly truncated APC mutations.
RK-287107 inhibits the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells but not the APC-wild (β-catenin-independent) colorectal cancer RKO cells.
RK-287107 suppresses COLO-320DM tumor growth in NOD-SCID mice (intraperitoneal or oral administration).

物理化学性质&存储条件

分子量 416.473
分子式 C22H26F2N4O2
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

2-(4,6-difluoro-1-(2-hydroxyethyl)spiro[indoline-3,4'-piperidin]-1'-yl)-5,6,7,8-tetrahydroquinazolin-4(3H)-one

参考文献

1. Mizutani A, et al. Cancer Sci. 2018 Sep 20. doi: 10.1111/cas.13805.

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