Retaspimycin_Hydrochloride_COA_06085_MedChemExpress

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Retapamulin(SB–275833) is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM.IC50 Value: 3 nM(Kd, E.coli)Target: AntibacterialRetapamulin is a topical antibiotic developed by GlaxoSmithKline. Retapamulin(SB–275833) is the first drug in the new class ofpleuromutilin antibiotics to be approved for human use.Retapamulin(SB–275833) is marketed as an ointment under the brand names Altabax and Altargo. Retapamulin(SB–275833) is useful for Antibiotics.References:[1]. Kircik LH. Efficacy and tolerability of retapamulin 1% ointment for the treatment of infected atopic dermatitis: a pilot study. J Drugs Dermatol. 2012 Jul 1;11(7):858–60.[2]. Candel FJ, Morales G, Picazo JJ. In vitro activity of retapamulin against linezolid and methicillin–resistant Staphylococcus aureus isolates. Rev Esp Quimioter. 2011 Sep;24(3):127–30.[3]. Pérez–Trallero E, Tamayo E, Montes M, García–Arenzana JM, Iriarte V. In vitro activities of retapamulin and 16 other antimicrobial agents against recently obtained Streptococcus pyogenes isolates. Antimicrob Agents Chemother. 2011 May;55(5):2406–8.[4]. Weinberg JM, Tyring SK. Retapamulin: an antibacterial with a novel mode of action in an age of emerging resistance to Staphylococcus aureus. J Drugs Dermatol. 2010 Oct;9(10):1198–204.[5]. Retapamulin: focus on its use in the treatment of uncomplicated superficial skin infections and impetigo By Jacobs, Michael R.From Expert Review of Dermatology (2010), 5(5), 505–517.Product Name:Retapamulin Cat. No.:HY-17010CAS No.:224452-66-8Molecular Formula:C 30H 47NO 4S Molecular Weight:517.76Target:Bacterial Pathway:Anti–infection Solubility:DMSO: ≥ 52 mg/mLCaution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Certificate of Analysis

PHYSICAL AND CHEMICAL PROPERTIES 

Molecular Formula:C26H35N7O6SMolecular Weight:573.66Storage:Powder-20°C3 years4°C2 yearsIn solvent-80°C6 months-20°C1 monthChemical Structure:

ANALYTICAL DATA 

Appearance:Light yellow to yellow (Solid)1 H NMR Spectrum:Consistent with structureLCMS:Consistent with structureHPLC:Consistent with structurePurity (HPLC):99.98%Conclusion:The product has been tested and complies with the given specifications.

Product Name:Palbociclib (isethionate)Cat. No.:HY-A0065CAS No.:827022-33-3Batch No.:14499Chemical Name:Ethanesulfonic acid, 2-hydroxy-, compd. with 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one (1:1)

Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@MedChemExpress.comAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Data Sheet

BIOLOGICAL ACTIVITY: 

Regorafenib (BAY 73–4506) is a multi–target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf–1 with IC50 of 13nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.IC50 value:Target: VEGFR; Raf; PDGFRβin vitro: Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH–3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs,regorafenib suppress PDGFR–β autophosphorylation after stimulation with PDGF–BB, with an IC50 of 90 nM. Regorafenib also inhibitsFGFR signaling in MCF–7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptorsKITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation ofVEGF165–stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2–stimulated HUVECsand of PDGF–BB–stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively [1]. Regorafenib targets both tumor cellproliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) andserine/threonine kinases (Raf and p38MAPK) [2]. Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in aconcentration– and time–dependent manner [3].in vivo: Regorafenib reveals potent dose–dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkagesin breast MDA–MB–231 and renal 786–O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung [1].

Product Name:Formula:C10H8F2N4OMolWeight:238.19CAS No.: 106308-44-5Cat. No.:HY-A0042Batch No: 09172Test Date:Retest Date:2013-7-15

2015-7-14

RufinamideCertificate of Analysis

ItemsSpecifications ResultsAppearanceWhite to off-white SolidConforms

Purity by LCMSNLT 98.0%99.37%ConclusionThe product tested complies with the specifications.

Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com

Store in a tightly closed container, in a cool and dry place. ConformsIdentificationThe retention time of the major peak in the chromatogram ofsample corresponds to that in the chromatogram of standardpreparation

ConformsMass spectrum of sample corresponds to that of standardpreparationConforms

1H NMR spectrum of sample corresponds to that of standardpreparation

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