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Chemical Structure : DS55980254
CAS No.: 2488609-41-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $358 | In stock | |
| 5 mg | $498 | In stock | |
| 10 mg | $728 | In stock | |
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| 50 mg | Get quote | ||
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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.
| M.Wt | 638.46 | |
| Formula | C29H18F8N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Yohei Yoshihama, et al. Cancer Res. 2022 Nov 2;82(21):4031-4043.
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