Wortmannin

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

一种有效的 PI3K 抑制剂，IC50 为 3 nM，不会抑制 PI4K 活性。

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity; inhibits both Fc epsilon RI-mediated histamine secretion and leukotriene release up to 80% with IC50 of 2.0 and 3.0 nM, respectively; Also inhibits DNA-PK and MLCK.(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. Wortmannin prevents nuclear entry of YAP.(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.

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.Wortmannin prevents nuclear entry of YAP. Cell Proliferation Assa 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.

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. Animal Model:Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft 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.

SL-2052 | KY-12420

PI3K/Akt/mTOR signaling

PI3K

PI3K,DNA-PK,ATM,MLCK,ATR

Cancer

——

19545-26-7

428.4319

C23H24O8

>98% (HPLC)

10 mM in DMSO

CC(O[C@@H](C1=C2C(C3=C4C(C(O[C@H](COC)[C@]14C)=O)=CO3)=O)C[C@]5(C)C(CC[C@]52[H])=O)=O

3H-Furo[4,3,2-de]indeno[4,5-h]-2-benzopyran-3,6,9-trione, 11-(acetyloxy)-1,6b,7,8,9a,10,11,11b-octahydro-1-(methoxymethyl)-9a,11b-dimethyl-, (1S,6bR,9aS,11R,11bR)-

(-20℃)

With Ice Pack

≥ 2 years