IST5-002

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

IST5-002，一种有效的 Stat5a/b 抑制剂，选择性地抑制 Stat5a/b 的转录活性，IC50 值分别为 1.5 μM (Stat5a) 和 3.5 μM (Stat5b)。 IST5-002 诱导前列腺癌细胞和慢性粒细胞白血病 (CML) 细胞凋亡 (apoptotic) 和死亡。IST5-002 可用于前列腺癌和慢性粒细胞白血病 (CML) 的研究。

IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML).

IST5-002 (1.5-25 μM, 2 h) inhibits transcriptional activity of Stat5a and Stat5b in a dose-dependent manner.IST5-002 (0-40 μM, 3 h) inhibits Bcr-Abl-induced Stat5a/b phosphorylation in K562 cells.IST5-002 (5-100 μM, 2 h) inhibits Stat5a/b phosphorylation in T47D cells, and inhibits dimerization in PC-3 cells.IST5-002 (5-100 μM, 2 h) suppresses Stat5 nuclear translocation in PC-3 cells, and inhibits DNA binding of Stat5 target genes and COS-7 cells.IST5-002 (2-50 μM, 48 h) reduces expression of Stat5a/b target genes (Bcl-xL and cyclin D1) in CWR22Rv1 and LNCaP cells.IST5-002 (3.1-50 μM, 72 h) inhibits cell growth through induction of apoptosis in human prostate cancer cells.IST5-002 (25-100 μM, 7 days) induces epithelial cell death in patient-derived prostate cancers ex vivo in organ explant cultures.IST5-002 (5 μM, 24-72h) inhibits Stat5a/b phosphorylation and induces apoptosis of Imatinib (HY-15463)-sensitive and -resistant CML cells.Cell Viability Assay Cell Line:CWR22Rv1, LNCaP, and DU145 cells Concentration:3.1, 6.3, 12.5, 25, 50 μM Incubation Time:72 h Result:Decreased viable cells by 50% to 80% at 12.5 μM.Cell Cycle Analysis Cell Line:LNCaP and CWR22Rv1 cellsConcentration:6, 12, 25 μM Incubation Time:72 h Result:Increased the fraction of dead cells (sub-G1) and decreased the fraction of living cells (G2–M).Western Blot Analysis Cell Line:Bcr-Abl–positive K562 cells Concentration:0, 1, 5, 10, 20, 40 μM Incubation Time:3 h Result:Inhibited Bcr-Abl-induced Stat5a/b phosphorylation at 5 μM, without affecting Bcr-Abl tyrosine phosphorylation levels.Immunofluorescence Cell Line:PC-3 cells Concentration:5, 10, 15. 20, 40 μM Incubation Time:2 h Result:Inhibited Prl (Prolactin)-induced nuclear translocation of Stat5.

RORγt inverse agonist 29 (intraperitoneal injection, 25-100 mg/kg, daily for 10 days) inhibits tumor growth in prostate cancer xenograft model.Animal Model:Prostate cancer (CWR22Rv1) xenograft modelDosage:25, 50, and 100 mg/kg Administration:Intraperitoneal injection, daily for 10 days Result:Induced massive loss of viable tumor cells and dead rounded cells accumulation.Induced cell death through apoptosis (shown by fragmented DNA in tumor sections).Decreased nuclear Stat5a/b content by 60%, 78%, and 90% at 25, 50, and 100 mg/kg, respectively.

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13484-66-7

437.34

C17H20N5O7P

>98% (HPLC)

In Vitro:?H2O 中的溶解度 : 125 mg/mL (285.82 mM; 超声助溶) DMSO 中的溶解度 : 125 mg/mL (285.82 mM; 超声助溶 )

O[C@H]1[C@H](N2C=3C(N=C2)=C(NCC4=CC=CC=C4)N=CN3)O[C@H](COP(=O)(O)O)[C@H]1O

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(-20℃)

With Ice Pack

≥ 2 years