Home
Products
Rapamycin (Sirolimus)
| Product Name | Rapamycin (Sirolimus) |
| Price: | $34 / 20mg |
| Catalog No.: | CN00527 |
| CAS No.: | 53123-88-9 |
| Molecular Formula: | C51H79NO13 |
| Molecular Weight: | 914.18 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | CO[C@@H]1C[C@@H](CC[C@H]1O)C[C@H]([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H](CC[C@H]2C)C[C@H](OC)/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C1)C)/C)O)OC)C)C)/C)C |
| Contact us | |
|---|---|
| First Name: | |
| Last Name: | |
| E-mail: | |
| Question: | |
| Description | Rapamycin (Sirolimus) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM. |
| Target | mTOR:0.1 nM (IC50) Autophagy |
| In Vitro | Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of 0.1 nM, more potently than iRap and AP21967 with IC50 of 5 nM and 10 nM, respectively[1]. Rapamycin exerts its antitumor effect on malignant glioma cells by inducing autophagy and suggest that in malignant glioma cells a disruption of the PI3K/Akt signaling pathway could greatly enhance the effectiveness of mTOR inhibitors. Rapamycin inhibits cell viability in all three cell lines in a dose-dependent manner, but their sensitivities varied. The IC50 levels of T98G, U87-MG, and U373-MG cells are 2 nM, 1 μM, and >25 μM, respectively[3]. |
| In Vivo | Treatment with Rapamycin (i.p, 1.5 mg/kg) almost completely prevents the hypertrophic increases in plantaris muscle weight and fibre size at 7 and 14 days[4]. WT or LS/+ mice are treated daily Rapamycin (2 mg/kg body weight i.p.) for 4 weeks, follows by an additional 4 weeks of weekly injections of the same dose. There is significant reversal of the abnormal fetal gene expression profile of hearts from Rapamycin-treated LS/+ mice[5]. |
| Cell Assay | HL-60, NB4, U937, KG-1, and K562 cells are passaged routinely in RPMI-1640 supplemented with 10% heat- inactivated FBS, 2 mM L-glutamine, 50 U/mL penicillin and 50 μg/mL streptomycin in a 5% CO2 humidified atmosphere at 37°C. For the experiments, exponentially growing cells are harvested by centrifugation, and resuspended in fresh medium containing 10% FBS. The cells are seeded at an initial cell density of 2×105/mL in BD Falcon six-well plates in the presence of various concentrations of DMSO or 1 μM ATRA. Rapamycin (20 nM) is added 20 min prior to the differentiation agents. At day 2, 0.3 mL of fresh medium is added to each well. The viable cells are determined by trypan blue exclusion and quantified using a hemocytometer[2]. |
| Animal Admin | Rats[4] Female Sprague-Dawley rats (250-275 g), the adult female SD rats (225-250 g) are randomized to treatment or vehicle groups so that the mean starting body weights of each group are equal. Drug treatment began on the day of surgery or on the first day of reloading after the 14-day suspension. Rapamycin is delivered once daily by intraperitoneal injection at a dose of 1.5 mg/kg, dissolved in 2% carboxymethylcellulose. CsA is delivered once daily by subcutaneous injection at a dose of 15 mg/kg, dissolved in 10% methanol and olive oil. FK506 is delivered once daily via subcutaneous injection at a dose of 3 mg/kg, dissolved in 10% ethanol, 10% cremophor and saline. Mice[5] Rapamycin is dissolved in ethanol at a concentration of 20 mg/mL, filter sterilized, resuspended in vehicle (0.25% PEG, 0.25% Tween-80) at a concentration of 1 mg/mL, and injected i.p. (2 mg/kg body weight), either daily for 4 weeks or daily for 4 weeks followed by weekly injections for an additional 4 weeks. Injections began at either 8 weeks (prior to onset of hypertrophy) or 12 weeks (after established hypertrophy is indicated) of age, and mice are assessed after 4 weeks of treatment or after 8 weeks of treatment, as detailed in the Results and figure legends. As controls, WT and LS/+ mice are treated with vehicle alone. |
| Density | 1.2±0.1 g/cm3 |
| Boiling Point | 973.0±75.0 °C at 760 mmHg |
| Flash Point | 542.3±37.1 °C |
| Exact Mass | 913.555115 |
| PSA | 195.43000 |
| LogP | 3.54 |
| Vapour Pressure | 0.0±0.6 mmHg at 25°C |
| Storage condition | -20°C |