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Wortmannin (SL-2052) 是一種有效的,不可逆的,選擇性PI3K 抑制劑,IC50 值為 3 nM。Wortmannin (SL-2052) 阻斷自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3,IC50 值分別為 5.8 和 48 nM。
生物活性
Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively[1][2][3].
體外研究(In Vitro)
Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively[4]. Wortmannin prevents nuclear entry of YAP[6].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[4]
Cell Line: | K562 cells |
Concentration: | 0, 6.25, 12.5, 25, 50 and 100 nM |
Incubation Time: | 0, 24, 48 and 72 hours |
Result: | Inhibited the K562 cells proliferation. The IC50 value at 24 hour, 48 hour, and 72 hour was 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM. |
體內研究(In Vivo)
Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation[5].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft[5] |
Dosage: | 1 mg/kg and 1.5 mg/kg |
Administration: | Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 days then 1.0 mg/kg for 9 days. |
Result: | The growth rate of the treated tumors was significantly slower during drug administration than that of nontreated tumors. |
分子量:428.43
Formula:C23H24O8
CAS 號:19545-26-7
中文名稱:渥曼青霉素;沃氏籃酶素;奧特曼寧
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : ≥ 50 mg/mL (116.71 mM)
* "≥" means soluble, but saturation unknown.
濃度溶劑體積質量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.3341 mL | 11.6705 mL | 23.3410 mL |
5 mM | 0.4668 mL | 2.3341 mL | 4.6682 mL |
10 mM | 0.2334 mL | 1.1671 mL | 2.3341 mL |
請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內使用,-20°C 儲存時,請在 1 個月內使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻
Wortmannin (SL-2052) 是一種有效的,不可逆的,選擇性PI3K 抑制劑,IC50 值為 3 nM。Wortmannin (SL-2052) 阻斷自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3,IC50 值分別為 5.8 和 48 nM。
生物活性
Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively[1][2][3].
體外研究(In Vitro)
Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively[4]. Wortmannin prevents nuclear entry of YAP[6].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[4]
Cell Line: | K562 cells |
Concentration: | 0, 6.25, 12.5, 25, 50 and 100 nM |
Incubation Time: | 0, 24, 48 and 72 hours |
Result: | Inhibited the K562 cells proliferation. The IC50 value at 24 hour, 48 hour, and 72 hour was 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM. |
體內研究(In Vivo)
Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation[5].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft[5] |
Dosage: | 1 mg/kg and 1.5 mg/kg |
Administration: | Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 days then 1.0 mg/kg for 9 days. |
Result: | The growth rate of the treated tumors was significantly slower during drug administration than that of nontreated tumors. |
分子量:428.43
Formula:C23H24O8
CAS 號:19545-26-7
中文名稱:渥曼青霉素;沃氏籃酶素;奧特曼寧
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : ≥ 50 mg/mL (116.71 mM)
* "≥" means soluble, but saturation unknown.
濃度溶劑體積質量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.3341 mL | 11.6705 mL | 23.3410 mL |
5 mM | 0.4668 mL | 2.3341 mL | 4.6682 mL |
10 mM | 0.2334 mL | 1.1671 mL | 2.3341 mL |
請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內使用,-20°C 儲存時,請在 1 個月內使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻