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Key Documents

S-015

Supelco

Sirolimus solution

1.0 mg/mL in acetonitrile, ampule of 1 mL, certified reference material, Cerilliant®

Synonym(s):

Rapamycin

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About This Item

Empirical Formula (Hill Notation):
C51H79NO13
CAS Number:
Molecular Weight:
914.17
EC Number:
MDL number:
UNSPSC Code:
41116107
PubChem Substance ID:
NACRES:
NA.24

grade

certified reference material

Quality Level

form

liquid

feature

Snap-N-Spike®/Snap-N-Shoot®

packaging

ampule of 1 mL

manufacturer/tradename

Cerilliant®

concentration

1.0 mg/mL in acetonitrile

technique(s)

gas chromatography (GC): suitable
liquid chromatography (LC): suitable

application(s)

clinical testing

format

single component solution

storage temp.

−70°C

SMILES string

CO[C@@H]1C[C@@H](CC[C@H]1O)C[C@H](C)[C@@H]2CC(=O)[C@H](C)C=C(C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)[C@H](C[C@@H]3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N4CCCC[C@H]4C(=O)O2)OC

InChI

1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1

InChI key

QFJCIRLUMZQUOT-HPLJOQBZSA-N

Gene Information

human ... FKBP1A(2280)

General description

This Certified Spiking Solution® is suitable for critical quantitative applications in clinical and diagnostic testing such as therapeutic drug monitoring assays to ensure patients remain within the drug’s narrow therapeutic range. The Snap-N-Spike® format allows laboratories to eliminate weighing operations of hazardous substances such as sirolimus, significantly reducing occupational exposure hazards related to the handling of acutely toxic powders, and provides the ability to spike into their matrix of choice just before use.

Sirolimus, also known as rapamycin, belongs to the group of natural hydrophobic macrolides and is used widely as an immunosuppressive drug. It also shows anti-fungal, anti-candidal, anti-tumor, and anti-proliferative, in addition to immunosuppressive activities. Sirolimus is produced by Streptomyces hygroscopicus bacterium and works as a mammalian Target of Rapamycin (mTOR)inhibitor. It acts by blocking the activation and proliferation of T-lymphocytes, in response to the cytokines and antigens.

Application

The certified reference solution (CRM) in solution can also be used as follows:
  • Multi-residue analysis of sirolimus, tacrolimus, everolimus, and cyclosporine A in whole blood samples by combining Bio-solid phase microextraction with mass spectrometry through a microfluidic open interface (Bio-SPME-MOI-MS/MS)
  • Development and validation of a high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) to determine immunosuppressive drugs― cyclosporine A, tacrolimus, sirolimus, and everolimus in whole blood samples
  • Determination of sirolimus in both pig whole blood and lung tissue samples by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and using a single protein precipitation step for sample preparation
  • Analysis of blood samples collected from former transplant patients for the quantification of sirolimus, cyclosporine A, tacrolimus, and everolimus by liquid chromatography and tandem mass spectrometryEstimation of sirolimus, cyclosporine A, and everolimus in the dried matrix on paper discs (DMPD) by liquid chromatography along with tandem mass spectrometry (LC-MS/MS)

Features and Benefits

  • Fully characterized under ISO/IEC 17025 and ISO 17034 accreditation
  • Accompanied with a comprehensive Certificate of Analysis (CoA) with data on stability, homogeneity, accuracy of concentration, uncertainty, and traceability
  • Rigorously tested through real-time stability studies to ensure accuracy and shelf life
  • Gravimetrically prepared using qualified precision balances to ensure minimal uncertainty
  • Flame sealed under argon into ampoules for long-term shelf life
  • Offered in a convenient, DEA-exempt format to improve laboratory efficiency

Legal Information

CERILLIANT is a registered trademark of Merck KGaA, Darmstadt, Germany
CERTIFIED SPIKING SOLUTION is a registered trademark of Cerilliant Corporation
Snap-N-Shoot is a registered trademark of Cerilliant Corporation
Snap-N-Spike is a registered trademark of Merck KGaA, Darmstadt, Germany

Pictograms

FlameExclamation mark

Signal Word

Danger

Hazard Classifications

Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Eye Irrit. 2 - Flam. Liq. 2

Storage Class Code

3 - Flammable liquids

WGK

WGK 2

Flash Point(F)

35.6 °F - closed cup

Flash Point(C)

2 °C - closed cup


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Certificates of Analysis (COA)

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M A Beigh et al.
Journal of biological regulators and homeostatic agents, 27(2), 399-408 (2013-07-09)
S6K1 regulation associates a central role with dynamics of sequential phosphorylations at the hydrophobic motif (T412) and activation loop (T252) of the enzyme, such that the hydrophobic motif phosphorylation supposedly brought about by mTOR- kinase, primes the enzyme for PDK1
Combination of rapamycin and imatinib in treating refractory chronic myeloid leukemia myeloid blast crisis:a case report(025B3;).
Jing Xie et al.
Chinese medical sciences journal = Chung-kuo i hsueh k'o hsueh tsa chih, 28(2), 127-128 (2013-06-29)
Elisabeth Brunner et al.
Advances in clinical and experimental medicine : official organ Wroclaw Medical University, 22(3), 355-359 (2013-07-06)
In lung transplantation, acute rejection episodes increase the risk of chronic rejection. Therefore treatment of acute rejection needs to be optimized for better long-term outcome of lung-transplantation and patient survival. The aim was to verify whether an inhibitor of the
Mario Campone et al.
European journal of cancer (Oxford, England : 1990), 49(12), 2621-2632 (2013-06-06)
Everolimus (EVE; an inhibitor of mammalian target of rapamycin [mTOR]) enhances treatment options for postmenopausal women with hormone-receptor-positive (HR(+)), human epidermal growth factor receptor-2-negative (HER2(-)) advanced breast cancer (ABC) who progress on a non-steroidal aromatase inhibitor (NSAI). This is especially
Tabetha Sundin et al.
Experimental cell research, 319(13), 2103-2112 (2013-06-12)
Translation is mediated partly by regulation of free eukaryotic initiation factor 4E (eIF4E) levels through PI3K-Akt-mTOR signaling. Cancer cells treated with the plant-derived perillyl alcohol (POH) or the mechanistic target of rapamycin (mTOR) inhibitor rapamycin dephosphorylate eIF4E-binding protein (4E-BP1) and

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