Rapamycin-d3
Based on 1 publication(s) in Google Scholar
Rapamycin-d3 (Sirolimus-d3; AY-22989-d3; NSC 226080-d3) is the deuterated-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
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- Reinheit : 95.92%
- CAS. Nr.: 392711-19-2
- Formel: C51H76D3NO13
- Molecular Weight:917.19
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-16046
RimiducidDimerization Inducer -
HY-10219
RapamycinmTOR Inhibitor -
HY-10218
EverolimusmTORC Inhibitor -
HY-13003
Torin 1mTOR Inhibitor -
HY-10422
AZD-8055mTOR Inhibitor -
HY-10219G
Rapamycin (GMP)mTOR Inhibitor -
HY-10219R
Rapamycin (Standard)Reference Standard -
HY-50908
RidaforolimusmTOR Inhibitor -
HY-10423
OSI-027mTOR Inhibitor -
HY-10297
OmipalisibPI3K/mTOR Inhibitor -
HY-10218R
Everolimus (Standard)mTORC Inhibitor -
HY-12034
WYE-354mTOR inhibitor
Publications Citing Use of MedChemExpress (MCE) Rapamycin-d3
MoreAlle Endogenous Metabolite Isoform-spezifische Produkte anzeigen
MoreAlle Antibiotic Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
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mTOR 0.1 nM (IC50, in HEK293 cells ) |
Microbial Metabolite |
FKBP12 |
Autophagy |
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
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Concentration:12.5 nM, 25 nM, 50 nM, 100 nM
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Incubation Time:24 hours
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Result:Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.
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Cell Line:95D cells
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Concentration:10 nM and 20 nM
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Incubation Time:24 hours
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Result:Combination treatment with RP-56976 decreased phosphorylation of ERK.
In Vivo
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Animal Model:24 male nu/nu mice aged 4-5 week old (15-20 g)[4]
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Dosage:2.0 mg/kg
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Administration:Intraperitoneal injection; every other day; 28 days
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Result:Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.
Anwendung
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS. Nr. 392711-19-2
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Unlabeled CAS 53123-88-9
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Appearance Solid
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Molecular Weight 917.19
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Formel C51H76D3NO13
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Color White to off-white
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SMILES
O=C([C@@]1(O[C@@H](CC[C@H]1C)C[C@@H](/C(C)=C/C=C/C=C/[C@H](C2)C)OC([2H])([2H])[2H])O)C(N3[C@@H](CCCC3)C(O[C@@H](CC([C@@H](/C=C([C@H]([C@H](C([C@@H]2C)=O)OC)O)\C)C)=O)[C@@H](C[C@@H]4CC[C@H]([C@@H](C4)OC)O)C)=O)=O
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Synonyms
Sirolimus-d3; AY-22989-d3; NSC 226080-d3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Ecotoxicol Environ Saf
ATF4-mediated different mode of interaction between autophagy and mTOR determines cell fate dependent on the level of ER stress induced by Cr(VI). [Abstract]2024 Aug:281:116639. PMID: 38964069
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (109.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (762 KB)
- English - EN (762 KB)
- Français - FR (762 KB)
- Deutsch - DE (762 KB)
- Norwegian - NO (762 KB)
- Español - ES (762 KB)
- Swedish - SV (762 KB)
- Italian - IT (762 KB)
- Korean - KR (762 KB)
- Portuguese - PT (762 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem, 2007, 282(18), 13395-13401. [Content Brief]
[2]. Rangaraju S, et al. Rapamycin activates autophagy and improves myelination in explant cultures from neuropathicmice. J Neurosci. 2010 Aug 25;30(34):11388-97. [Content Brief]
[3]. Niu H, et al. Rapamycin potentiates cytotoxicity by RP-56976 possibly through downregulation of Survivin in lung cancer cells. J Exp Clin Cancer Res. 2011 Mar 10;30:28. [Content Brief]
[4]. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816. [Content Brief]
[5]. Svensson JE, et al. Evaluating the effect of rapamycin treatment in Alzheimer's disease and aging using in vivo imaging: the ERAP phase IIa clinical study protocol. BMC Neurol. 2024 Apr 4;24(1):111. [Content Brief]
[6]. Soini L, et al. Molecular glues to stabilise protein-protein interactions. Curr Opin Chem Biol. 2022 Aug;69:102169. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.0903 mL | 5.4514 mL | 10.9029 mL | 27.2572 mL |
| 5 mM | 0.2181 mL | 1.0903 mL | 2.1806 mL | 5.4514 mL | |
| 10 mM | 0.1090 mL | 0.5451 mL | 1.0903 mL | 2.7257 mL | |
| 15 mM | 0.0727 mL | 0.3634 mL | 0.7269 mL | 1.8171 mL | |
| 20 mM | 0.0545 mL | 0.2726 mL | 0.5451 mL | 1.3629 mL | |
| 25 mM | 0.0436 mL | 0.2181 mL | 0.4361 mL | 1.0903 mL | |
| 30 mM | 0.0363 mL | 0.1817 mL | 0.3634 mL | 0.9086 mL | |
| 40 mM | 0.0273 mL | 0.1363 mL | 0.2726 mL | 0.6814 mL | |
| 50 mM | 0.0218 mL | 0.1090 mL | 0.2181 mL | 0.5451 mL | |
| 60 mM | 0.0182 mL | 0.0909 mL | 0.1817 mL | 0.4543 mL | |
| 80 mM | 0.0136 mL | 0.0681 mL | 0.1363 mL | 0.3407 mL | |
| 100 mM | 0.0109 mL | 0.0545 mL | 0.1090 mL | 0.2726 mL |
Rapamycin-d3 Related Classifications
HY-10219S Related Classifications
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