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^{[ 3]}。

RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC 50 s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.

Solid

ChoKα

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

RSM-932A exhibits a potent in vivo anticancer activity, and lack of toxicity at the effective doses. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic nu/nu mice, CD1 nude mice,

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. Juan Carlos Lacal, et al. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol Cancer Ther. 2015 Jan;14(1):31-9.
[2]. Ana de la Cueva, et al. Combined 5-FU and ChoKα inhibitors as a new alternative therapy of colorectal cancer: evidence in human tumor-derived cell lines and mouse xenografts. PLoS One. 2013 Jun 10;8(6):e64961.

In Vitro: DMSO : 16.67 mg/mL (19.00 mM; ultrasonic and warming and heat to 60°C)配制储备液