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RSM-932A

CAS No. : 850807-63-5

MCE 国际站：RSM-932A

产品活性：RSM-932A (TCD-717) 是一种特异性 ChoKα 抑制剂，对人重组 ChoKα 和 ChoKβ 酶的 IC₅₀ 分别为 1 和 33 μM。RSM-932A 是针对 ChoKα 的“人类首创”化合物。RSM-932A 具有有效的体外抗肿瘤增殖和体内抗肿瘤活性，且显示低毒性。

研究领域：Others

作用靶点：Others

In Vitro: RSM-932A has a potent anti-proliferative activity against most tumor-derived cell lines tested, including those derived from breast, lung, colon, bladder, liver, ovary, bone, cervix, kidney, pancreas, melanoma, and brain tumors, with IC₅₀s of 1.3-7.1 μM for 72 hours.
?RSM-932A (TCD-717; 2-4 μM; for 24 hours) promotes cell death of colon cancer cells.
?RSM-932A (2-10 μM) exhibits a dosage-dependent decrease in the levels of thymidylate synthase (TS) and thymidine kinase (TK1) proteins proteins.
?RSM-932A inhibits Streptococcus pneumoniae choline kinase (sChoK) with IC₅₀ of 0.5 μM in LDH/PK and colorimetric enzymatic assays.
?The minimum inhibitory concentration (MIC) of RSM-932A for S. pneumoniae is 0.4 μM, and the minimum lethal concentration (MLC) is 1.6 μM.
?RSM-932A is a comparatively potent inhibitor with the IC₅₀ of 1.75 μM in a steady-state reaction in which the concentration of Choline is equivalent to its K_m.

In Vivo: RSM-932A exhibits a potent in vivo anticancer activity, and lack of toxicity at the effective doses.

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