rapamycin from streptomyces*hygroscopicus;23,27-EPOXY-3H-PYRIDO(2,1-C)(1,4)OXAAZACYCLOHENTRIACONTINE;AY 22989;NSC-226080;RAPA;RAPAMUNE;RAPAMYCIN;RAPAMYCIN, STREPTOMYCES HYGROSCOPICUS;RPM;SIROLIMUS;antibioticay22989;sila9268a;WYETH RAPAMYCIN, 1GM;RAPAMYCIN 1GM;RAPAMYCIN, STANDARD WITH MS, NMR RESULT;Rapamicin;Rapamicin(sirolimus );Rapamycin (AY 22989, Sirolimus, RAPA,NSC 226080, Rapamune®);Rapamycin (Sirolimus);Sirolimus solution;Siroliums; 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine,AY 22989,Sirolimus;Rapamycin from Streptomyces hygroscopicus;Resorcinol;23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine;(-)-Rapamycin;Rapammune;sirolimusum;Antibiotic AY 22989;SILA 9268A;W36ZG6FT64;C51H79NO13;DSSTox_CID_3582;DSSTox_RID_77091;DSSTox_GSID_23582;Cypher;Supralimus;Wy 090217;I 2190A;I2190A;SIIA 9268A
Cas No.
53123-88-9
分子式
C51H79NO13
分子量
914.17
包装储存
Powder; -20°C; 3 years; 4°C; 2 years;
生物活性
Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
性状
Solid
IC50 & Target[1][2]
mTOR0.1 nM (IC50, in HEK293 cells )Microbial Metabolite
体外研究(In Vitro)
Rapamycin (12.5-100 nM; 24 hours) treatment exerts modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines (A549, SPC-A-1, 95D and NCI-H446 cells) tested, achieving about 30-40% reduction in cell proliferation at 100 nM vs. ~10% reduction at 12.5 nM. Lung cancer cell line 95D cells are exposed to Rapamycin (10 nM, 20 nM) and RP-56976 (1 nM, 10 nM) alone or in combination (Rapamycin 20 nM+ RP-56976 10 nM). After 24 hours exposure to Rapamycin or RP-56976 alone does not significantly alter the level of expression or phosphorylation of ERK1/2, whereas cells treated with the combination of Rapamycin with RP-56976 exhibit a marked reduction in the phosphorylation levels of ERK1/2.Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
雷帕霉素(2.0 mg/kg;腹腔内注射;每隔一天;28天)单独使用有中等的抑制作用。然而,与对照组、雷帕霉素单药组相比,二甲双胍联合雷帕霉素对肿瘤生长的抑制作用明显增强。Medlife has not independently confirmed the accuracy of these methods. They are for reference only.Animal Model:24 male nu/nu mice aged 4-5 week o