CBR-5884

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CBR-5884 是一种选择性、活性磷酸甘油酸脱氢酶 (PHGDH) 抑制剂，IC50 为 33 μM。 CBR-5884 抑制癌细胞中的丝氨酸从头合成，并对具有高丝氨酸生物合成活性的癌细胞系具有选择性毒性。

CBR-5884 is an ?selective, active of phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 33 μM.?CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity.?CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.?Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDHCBR-5884 (15 or 30 μM; 3-5 days) selectively inhibits breast cancer lines that have a high propensity for serine synthesis. CBR-5884 (15 or 30 μM; 3-5 days) also selectively inhibits the proliferation of melanoma.

CBR-5884 (15 or 30 μM; 3-5 days) selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Cell Proliferation Assay Cell Line:Breast and melanoma cell lines Concentration:15 or 30 μM Incubation Time:3-5 days Result:Inhibited the proliferation of melanoma and breast cancer lines.

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Metabolic Enzyme/Protease

Dehydrogenase

PHGDH|serine synthesis

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681159-27-3

336.39

C14H12N2O4S2

>98% (HPLC)

DMSO:47 mg/mL (139.72 mM; Need ultrasonic);H2O:< 0.1 mg/mL (insoluble)

CCOC(=O)c1sc(NC(=O)c2ccco2)c(SC#N)c1C

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(-20℃)

With Ice Pack

≥ 2 years