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Rapamycin Europäischer Partner

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mg
ArtNr HY-10219-10mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Alternative Names
Sirolimus; AY-22989
CAS
53123-88-9
MWt
914.17
Formula
C51H79NO13
Solubility
H2O : < 0.1 mg/mL (insoluble); DMSO : 125 mg/mL (136.74 mM; Need ultrasonic); Ethanol : 50 mg/mL (54.69 mM; Need ultrasonic)
Clinical Information
Launched
Research Area
Cancer
Pathway
Anti-infection, PI3K/Akt/mTOR, Autophagy, Metabolic Enzyme/Protease, Immunology/Inflammation, Apoptosis, Autophagy, Anti-infection
Target
Fungal, mTOR, Autophagy, Endogenous Metabolite, FKBP, FKBP, FKBP, Antibiotic
SMILES
O=C([C]1(O)[CH](CC[CH](C[CH](/C(C)=C/C=C/C=C/[CH](C[CH](C)C([CH]([CH](/C(C)=C/[CH]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[CH]3C(O[CH](CC2=O)[CH](C[CH]4C[CH]([CH](O)CC4)OC)C)=O)=O
Biological Activity
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[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
IC50 & Target: IC50: 0.1 nM (mTOR)[1]
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. ca.10% reduction at 12.5 nM[3].

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[3].
In Vivo: Rapamycin (2.0 mg/kg; intraperitoneal injection; every other day; 28 days) alone has a moderate inhibitory effect. However, the combination of Metformin and Rapamycin exerts a significantly increased inhibition of tumor growth compared with the control group, the Rapamycin monotherapy group and the Metformin monotherapy group[4].

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Menge: 10mg
Lieferbar: In stock
lieferbar

Lieferung vsl. bis 13.04.2023 

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