产品说明书
Silmitasertib sodium salt
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同义名 : | CX-4945 sodium salt;CX-4945 Sodium |
| CAS号 : | 1309357-15-0 | |
| 货号 : | A188483 | |
| 分子式 : | C19H11ClN3NaO2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 371.752 | |
| MDL号 : | MFCD28385881 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 5 mg/mL(13.45 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 15 mg/mL(40.35 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | Protein kinase CK2 is a tetrameric enzyme with two catalytic subunits and two regulatory subunits that constitutively actives serine/threonine protein kinase as a prototypical non-oncogene. CX-4945 Sodium is a selective inhibitor of CK2 catalytic subunits with an IC50 value of 1 nmol/L. Four-hour exposure to 5 and 10 μmol/L CX-4945 in BT-474 cells and BxPC-3 cells caused rapid dephosphorylation of CK2 phophorylation site, Akt (S129), and both canonical regulatory sites, Akt (T308) and Akt (S473). Treatment of BT-474 cells with 1-10 μmol/L CX-4945 for 24 hours induced a G2/M cell-cycle arrest, while the treatment of BxPC-3 cells led to G1/M arrest. Incubating HUVEC cells with 0.1-10 μmol/L CX-4945 led to rapid dephosphorylation of Akt (S129), Akt (T308) and Akt (S473) at 4 hours. Also in HUVEC cells, reduced phosphorylation at the CK2-phosphorylation sites on PTEN (S370/S380) was also observed after 24-hour exposure to 0.1-10 μmol/L CX-4945. CX-4945 inhibited HUVEC cell proliferation, migration, and tube formation with IC50 values of 5.5, 2, and 4 μmol/L at 72 hours, 24 hours and 18 hours, respectively. Treatment of BT-474 and BxPC-3 cells under hypoxic conditions with 5 μmol/L CX-4945 for 48 hours prevented the downregulation of p53 and pVHL. The activation of HIF-1α transcription in Hela cells under hypoxic versus normoxic conditions was also suppressed by 12.5 and 25 μmol/L CX-4945 48 hours after the treatment. In BT-474 xenograft mice, oral administration of 25 and 75 mg/kg CX-4945 twice a day for 31 days inhibited 88% and 97% tumor growth, respectively. In BxPC-3 mouse model, 75 mg/kg bid oral gavage of CX-4945 for 35 days resulted in 93% tumor growth inhibition[1]. | ||
| 作用机制 | CX-4945 Sodium acts as an ATP-competitive inhibitor of both isoforms of CK2 catalytic subunits, CK2α and CK2α’, directly blocking the phosphorylation of Akt at Serine 129 in PI3K/Akt signaling pathway[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.69mL 0.54mL 0.27mL |
13.45mL 2.69mL 1.34mL |
26.90mL 5.38mL 2.69mL |
| 参考文献 |
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