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881179-02-8

中文名稱 881179-02-8
英文名稱 Lith-O-Asp
CAS 881179-02-8
分子式 C28H45NO6
分子量 491.66
MOL 文件 881179-02-8.mol
881179-02-8 結(jié)構(gòu)式 881179-02-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11858
英文別名
Lith-O-Asp
Cholan-24-oic acid, 3-[(2S)-2-amino-3-carboxy-1-oxopropoxy]-, (3α,5β)-

物理化學性質(zhì)

熔點208-209 °C
沸點635.0±45.0 °C(Predicted)
密度1.19±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : ≥ 106 mg/mL (215.60 mM)
酸度系數(shù)(pKa)3.43±0.19(Predicted)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
Lith-O-Asp 是唾液酸轉(zhuǎn)移酶 (ST) 的抑制劑,其 IC50 值在 12-37 μM 之間。
靶點

IC50: 12-37 μM (ST).

體外研究

The results indicate that Lith-O-Asp shows no apparent growth inhibition effect toward different cancer cell lines at the tested doses of 10, 30, and 60 μM. By in vitro activity assay, it is revealed that the ability of Lith-O-Asp to inhibit the activities of ST3Gal I, ST3Gal III, and ST6GalI. The IC 50 values ranged from 12 to 37 μM. Flow cytometry shows a significant decrease in the expression of cell surface a-2,3- and a-2,6-sialylated antigens on The results indicates that Lith-O-Asp decreased the activity of both a-2,3- and a-2,6-sialyltransferases, and thus inhibit the transfer of sialic acids to the targeted glycoproteins.

體內(nèi)研究

A significant amount of secondary metastatic cancer cells are observed in lung tissues of DMSO control mice detected using IVIS in vivo imaging system after 26 days of fat pad inoculation. However, Lith-O-Asp–treated mice show fewer lung metastases. All DMSO-treated mice confirm secondary lung metastasis, but only 3 of 8 Lith-O-Asp-treated mice show lung metastasis. Average tumor nodules per mouse are 11±9 nodules in DMSO-treated group, and 2±4 nodules in Lith-O-Asp-treated group. Additionally, significantly stronger 4T1-Luc illumination signals are shown in control mice than in those injected with Lith-O-Asp-treated cancer cells on days 7 and 9.

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