GDC-0980_1032754-93-0_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:AZD2932 is a new series of quinazoline ether inhibitor which potently inhibits VEGFR–2 and PDGFR with IC50s of 4 nM/8 nM/ 7 nM for PDGFRβ/VEGFR–2/Flt–3.IC50 value: 4/8/7 nM(PDGFRβ/VEGFR–2/Flt–3) [1]Target: PDGFRβ/VEGFR2The same C6 in vivo model was used to study tumor growth inhibition (TGI) with AZD2932. Twice daily oral dosing (b.i.d.) 10 h apart resulted in significant TGI of 64% for both 50 and 12.5 mg/kg doses on the day the control animals were terminated (day 22 on the graph). Most importantly, xenografts bearing non–PDGFR expressing tumor cells were also sensitive to AZD2932 treatment: growth of Calu–6 tumor was inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p <0.001) and LoVo tumors by 67% at 50 mg/kg b.i.d. (p <0.001)[1].PROTOCOL (Extracted from published papers and Only for reference)Animal administration [1]The female nude mice bearing C6 tumors from the above experiment are dosed iv with VEGF–A and PDGFBB 5 min prior to cull and 6h post last dose ofAZD2932 and the lungs excised immediately after. Lung lysates are analyzed by western blot for total and phosphorylated VEGFR–2 and PDGFRβ. AZD2932 at 3–50 mg/kg b.i.d. 10 h apart gave 60–80% inhibition of both p–VEGFR–2 and p–PDGFRβ in a 1:1 ratio.References:[1]. Plé PA, et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR–2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett.2012 Jan 1;22(1):262–6.Product Name:AZD2932Cat. No.:HY-18179CAS No.:883986-34-3Molecular Formula:C 24H 25N 5O 4Molecular Weight:447.49Target:PDGFR; VEGFR Pathway:Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK Solubility:DMSO: ≥ 41 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。

Product Name:Go 6983CAS No.:133053-19-7Cat. No.:HY-13689Product Data SheetMWt:442.51Formula:C26H26N4O3Purity :>98%Solubility:DMSO 58 mg/ml; Water <1 mg/mlMechanisms:Biological Activity:Go 6983is a pan PKC inhibitor against for PKC PKC PKC and PKC with IC50of 7nM 7nM Pathways:TGF-beta/Smad; Target:PKC Go 6983 is a pan-PKC inhibitor against for PKC α, PKC β, PKC γ and PKC δ with IC50 of 7 nM, 7 nM,6 nM and 10 nM, respectively; less potent to PKC ζ and inactive to PKC μ.IC50 value: 7/7/6/10/60 (PKC α/β/γ/δ/ζ) [1]Target: pan-PKC in vitro: Go 6983 (300 μM) suppresses PKC μ auto-phosphorylation by 20% reduction in NIH3T3transfected with PKC μ [1]. In hearts reperfused with PMNs and Go 6983 (100 nM), left ventricular developed pressure (LVDP) and the rate of LVDP recoveres to 89% and 74% of baseline values,respectively, significantly higher than PMNs alone. Go 6983 (100 nM) significantly reduces PMNsadherence to the endothelium and infiltration into the myocardium compared with Ischemia followedReferences:[1]. Gschwendt M, et al. Inhibition of protein kinase C mu by various inhibitors. Differentiation fromprotein kinase c isoenzymes. FEBS Lett, 1996, 392(2), 77-80.[2]. Peterman EE, et al. G0 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion.y p by reperfusion (I/R)+ PMN hearts, and significantly inhibits superoxide release from PMNs by 90%.Go 6983 attenuates post-I/R cardiac contractile dysfunction in the presence of PMNs...[],p y pJ Cardiovasc Pharmacol, 2004, 43(5), 645-656.[3]. Young LH, et al. G0 6983: a fast acting protein kinase C inhibitor that attenuates myocardialischemia/reperfusion injury. Cardiovasc Drug Rev, 2005, 23(3), 255-272.[4]. Kumar A, et al. PfPKB, a novel protein kinase B-like enzyme from Plasmodium falciparum: I.Identification, characterization, and possible role in parasite development. J Biol Chem, 2004,279(23), 24255-24264.Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。

Product Name:Loteprednol Etabonate CAS No.:82034-46-6Cat. No.:HY-17358Product Data SheetMWt:466.95Formula:C24H31ClO7Purity :>98%Solubility:DMSO 90 mg/mL; Water <1 mg/mL y Mechanisms:Biological Activity:Loteprednol Etabonate is an anti inflammatory corticosteroid used in optometry and ophthalmologyPathways:GPCR/G protein; Target:Glucocorticoid Receptor g gLoteprednol Etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology.IC50 Value:Target: Glucocorticoid Receptorin vitro:in vivo: Intravenous administration of loteprednol etabonate (5 mg/kg) to dogs revealed a terminal half-life of 2.8 h, a volume of distribution of 3.7 L/kg, and a total body clearance of 0.9 L/h/kg. Intact loteprednol etabonate was not detectable in the urine. After oral administration of the drug (5 mg/kg)to dogs, only metabolites, but no intact drug, were found in the plasma, an indication for a high first-pass effect. A pronounced binding of the drug to plasma protein (> 90%) and a high erythrocyte-References:[1]. Noble S, Goa KL. Loteprednol etabonate: clinical potential in the management of ocularinflammation. BioDrugs. 1998 Oct;10(4):329-39.[2]. Szelenyi I, Hochhaus G, Heer S et al. Loteprednol etabonate: a soft steroid for the treatment of p p g g p p ()g y ybuffer partition coefficient of 7.8 were determined in vitro....allergic diseases of the airways. Drugs Today (Barc). 2000 May;36(5):313-20.[3]. Howes JF. Loteprednol etabonate: a review of ophthalmic clinical studies. Pharmazie. 2000Mar;55(3):178-83.[4]. Pavesio CE, Decory HH. Treatment of ocular inflammatory conditions with loteprednoletabonate. Br J Ophthalmol. 2008 Apr;92(4):455-9.[5]. Comstock TL, Decory HH. Advances in corticosteroid therapy for ocular inflammation:loteprednol etabonate. Int J Inflam. 2012;2012:789623.[6]. Loteprednol Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。

P d t D t Sh tProduct Name:TAK-733CAS No.:1035555-63-5Cat. No.:HY-13449Product Data Sheet MWt:504.23Formula:C17H15F2IN4O4Purity :>98%Solubility:DMSO 101 mg/mL Water <1mg/mL Ethanol <1mg/mL Mechanisms:Biological Activity:TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM,Pathways:MAPK; Target:MEK mg/mL Ethanol <1 mg/mLinactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.IC50 Value: 3.2 nM [1]Target: MEK1in vitro: Sensitivity of cutaneous and uveal melanoma cell lines to TAK733 was investigated. five cutaneous melanoma cell lines wild type for mutations in NRAS, BRAF, GNAQand GNA11 and only one was highly sensitive to TAK733 with IC50s below 1 nM, while two were considered sensitive with IC50 less than 10 nM. All five uveal melanoma cell lines were sensitive to TAK733 with IC50values below 10 nM, with three of them being highly sensitive. All these cell lines carried GNAQ or GNA11driver mutations Inhibition of oncogenic MAPK signaling through MEK1and MEK2by References:[1]. Erika von Euw, Mohammad Atefi, Narsis Attar, Antitumor effects of the investigational selectiveMEK inhibitor TAK733 against cutaneous and uveal melanoma cell lines. Mol Cancer. 2012; 11: 22.[2]Robyn Fabrey Shawn O'Connell Andrew Stanton TAK 733an investigational selective GNA11 driver mutations. Inhibition of oncogenic MAPK signaling through MEK1 and MEK2 by TAK733 results in antitumor activity in vitro against a large subset of melanoma cell lines[1].in vivo: The in vivo antitum...[2]. Robyn Fabrey, Shawn O'Connell, Andrew Stanton, TAK-733, an investigational, selective MEK1/2 inhibitor, in combination with alisertib (MLN8237), an investigational, selective Aurora A kinase inhibitor is tolerated and results in additive to synergistic antitumor activity: Results from InVivo Studies. Cancer Res 2012; 72(8 Supplement): 3739.[3]. Akintunde Akinleye, Muhammad Furqan, Nikhil Mukhi, MEK and the inhibitors: from bench tobedside. J Hematol Oncol. 2013; 6: 27.Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。