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TAS1553

Chemical Structure : TAS1553

CAS No.: 2166023-31-8

TAS1553 (TAS-1553, TAS 1553)

货号: PC-38899Not For Human Use, Lab Use Only.

TAS1553 is a highly potent, selective small-molecule inhibitor of ribonucleotide reductase (RNR) with enzyme IC50 of 54.2 nM, binds to R1 subunit with Kd of 34.9 nM, disrupts PPI between R1 and R2 subunit.

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10 mg ¥1980 In stock
25 mg ¥3480 In stock
50 mg ¥5580 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

TAS1553 is a highly potent, selective small-molecule inhibitor of ribonucleotide reductase (RNR) with enzyme IC50 of 54.2 nM, binds to R1 subunit with Kd of 34.9 nM, disrupts PPI between R1 and R2 subunit.
TAS1553 displays clean selectivity profile againt at least 68 proteins, such as ion channels, transporters, nuclear receptors, and G protein-coupled receptors.
TAS1553 showed antiproliferative activity against both solid and hematological human cancer cell lines with GI50 values ranged from 0.228 to 4.15 uM.
TAS1553 rapidly and reversibly abrogated the protein-protein interaction between R1 and R2 in treated cells, reduces intracellular dATP pool and induces the replication stress and apoptosis in HCC38 and MV-4-11 cells.
SLFN11 is a factor to promote apoptosis induction by TAS1553.
TAS1553 demonstrates antitumor activity in both hematologic and solid tumor models.

物理化学性质&存储条件

分子量 482.911
分子式 C20H20ClFN4O5S
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

5-Chloro-2-[[[(1S,2R)-1-(4,5-dihydro-5-oxo-1,3,4-oxadiazol-2-yl)-2-(6-fluoro-2,3-dimethylphenyl)propyl]amino]sulfonyl]benzamide

参考文献

1. Hiroyuki Ueno, et al. Commun Biol. 2022 Jun 9;5(1):571.

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