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首页-小分子抑制剂&激动剂-Others-Other Targets-Dencatistat
Dencatistat

Chemical Structure : Dencatistat

CAS No.: 2377000-84-3

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Dencatistat (STP938, STP-938)

货号: PC-24123Not For Human Use, Lab Use Only.

Dencatistat (STP938) is a potent, orally bioavailable, selective inhibitor of cytidine triphosphate synthase 1 (CTPS1) with IC50 of <100 nM, specifically blocks cell proliferation of the hematological cancers.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Dencatistat (STP938) is a potent, orally bioavailable, selective inhibitor of cytidine triphosphate synthase 1 (CTPS1) with IC50 of <100 nM, > 1,300-fold selectivity over CTPS2, specifically blocks cell proliferation of the hematological cancers.
STP938 has an IC50 <100 nM against 43 (77%) of the hematological cell lines, whereas only 15% of the solid tumor derived cell lines are affected.
T-cell derived cell lines are extremely sensitive to STP938 with many IC50 <10 nM.
STP938 demonstrated the selective depletion of CTP but not ATP or GTP in activated human T-cells.|
STP938 enables cell specific inhibition of de novo pyrimidine nucleotide synthesis with a particular sensitivity displayed by cell lines derived from hematological malignancies.
STP938 selectively induces apoptosis in lymphocyte cells but not in other cell types that are able to rely upon CTPS2 for their CTP synthesis.

物理化学性质&存储条件

分子量 525.58
分子式 C24H27N7O5S
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

4-(2-(cyclopropanesulfonamido)pyrimidin-4-yl)-N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)tetrahydro-2H-pyran-4-carboxamide

参考文献

1. Andy Parker, et al. Blood (2020) 136 (Supplement 1): 31.

2. Philip Beer, et al. Blood (2022) 140 (Supplement 1): 12027–12028.

3. Patent WO2019179652 A1.

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