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首页-小分子抑制剂&激动剂-Others-Other Targets-DS55980254
DS55980254

Chemical Structure : DS55980254

CAS No.: 2488609-41-0

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DS55980254 (DS 55980254)

货号: PC-49548Not For Human Use, Lab Use Only.

DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.

规格 价格 库存 数量
2 mg ￥1980 In stock
5 mg ￥3580 In stock
10 mg ￥5580 In stock
25 mg ￥8980 In stock
50 mg Get quote
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

DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.
DS55980254 strongly suppressed the de novo PS synthesis in PTDSS2-KO HCT116 clone, whereas they weakly suppressed it in parental HCT116.
DS55980254 selectively suppressed the growth of PTDSS2-KO HCT116 in vitro.(
DS55980254 (10-30 mg/kg, daily, p.o.) induced tumor regression in PTDSS2-KO HCT116 and PTDSS2-KO A375 subcutaneous xenograft models, without body weight loss and severe toxicity.
DS55980254 induced selective cell death in PTDSS2-deleted cancer cells, induced ER stress downstream of PS depletion in PTDSS2-deleted tumor cells.
DS55980254 suppressed the growth of tumor containing both PTDSS2 wild-type and knockout cells in immunocompetent mice, showing potency for overcoming tumor heterogeneity by modulating the tumor immune microenvironment.

物理化学性质&存储条件

分子量 638.46
分子式 C29H18F8N4O4
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

7-(4-(4-(3,5-bis(trifluoromethyl)phenoxy)phenyl)-5-(2,2-difluoropropyl)-6-oxo-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzo[d]oxazol-2(3H)-one

参考文献

1. Yohei Yoshihama, et al. Cancer Res. 2022 Nov 2;82(21):4031-4043.

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