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    AMG 925 (FLX925; AMG925)
    AMG 925 (FLX925; AMG925)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0587
    CAS #: 1401033-86-0 Purity ≥98%

    Description: AMG 925 (also called FLX-925; AMG-925) is a novel, potent, selective and orally bioavailable FLT3/CDK4 dual inhibitor with potential antitumor activity. It inhibits FLT3/CDK4 with an IC50 of 1 nM and 3 nM, respectively. AMG 925 exhibits excellent anti-proliferative activity in vitro and inhibits cell growth with IC50 values of 19nM and 18nM, respectively, through inhibiting P-FLT3 and P-STAT5 and inducing apoptosis. It also has high in vivo antitumor efficacy in AML tumor–bearing mice, administration of AMG 925 shows inhibition of P-STAT5 and P-RB as well as cell growth both in subcutaneous MOLM13 xenograft tumor model and systemic MOLM13-Luc xenograft tumor model.

    References: Mol Cancer Ther. 2014 Apr;13(4):880-9.

    Related CAS: 1401034-19-2 (HCl Salt)

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    Molecular Weight (MW)471.55
    FormulaC26H29N7O2
    CAS No.1401033-86-0(free); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mM
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)2% hydroxypropyl methylcellulose+1% Tween 80: 30mg/mL
    SynonymsFLX 925; AMG925; FLX925; FLX-925; AMG-925; AMG 925; 

    Chemical Name: 2-hydroxy-1-(2-((9-((1r,4r)-4-methylcyclohexyl)-9H-pyrido[4',3':4,5]pyrrolo[2,3-d]pyrimidin-2-yl)amino)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl)ethanone

    InChi Key: BBUVDDPUURMFOX-SAABIXHNSA-N

    InChi Code: InChI=1S/C26H29N7O2/c1-16-2-5-18(6-3-16)33-22-13-27-10-8-19(22)20-12-28-26(31-25(20)33)30-23-7-4-17-14-32(24(35)15-34)11-9-21(17)29-23/h4,7-8,10,12-13,16,18,34H,2-3,5-6,9,11,14-15H2,1H3,(H,28,29,30,31)/t16-,18-

    SMILES Code: C[[email protected]]1CC[[email protected]](N2C3=CN=CC=C3C4=CN=C(NC5=NC6=C(CN(C(CO)=O)CC6)C=C5)N=C42)CC1


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    In Vitro

    In vitro activity: AMG 925 inhibits cell growth (IC50 values of 19nM and 18nM, respectively) through inhibiting P-FLT3 and P-STAT5 and inducing apoptosis. FLT3 mutants cause resistance to the current FLT3 inhibitors. AMG 925 is reported to inhibit cell growth in AML cells with FLT3 mutants FLT3-D835Y and FLT3-D835V. 


    Kinase Assay: AMG 925 also inhibits CDK6, CDK2, and CDK1 in kinase assays with IC50s of 8±2 nM, 375±150 nM, 1.90±0.51 μM, respectively. A fair overall kinase selectivity of AMG 925 is as determined by KinomScan against a panel of 442 various kinases. 


    Cell Assay: MOLM13 and Mv4-11 are used. MOLM13-Luc cells are constructed by transduction of MOLM13 cells with the pLV218G luciferin/lentivector, which expresses luciferase under the murine EF1α promoter. Sorafenib-resistant MOLM13 (MOLM13sr) and Mv4-11 (Mv4-11sr) are isolated by passaging the cells in growth medium containing increasing concentrations of Sorafenib (1-1 nM). Cell growth is measured by a DNA synthesis assay. Cells are seeded in a 96-well Cytostar T plate at a density of 5×103 cells/well in a total volume of 160 μL. Test compounds (e.g., AMG 925; 0.03 and 0.3μM) are serially diluted into the plate (20 μL/well) and 20 μL/0.1 μCi of [14C]-Thymidine added to each well. Isotope incorporation is determined using a β plate counter after further 72-hour incubation. Apoptosis is assayed by using the Vybrant Apoptosis Assay Kit. Briefly, cells are seeded into a 6-well plate at 5×105 cells per well and treated with compounds (e.g., AMG 925; 0.003, 0.01, 0.03, 0.1, 0.3, and 1 μM) for 24 hours. The cells are then stained with reagents provided in the kit and analyzed by flow cytometry. The Sytox Green fluorescence versus allophycocyanin fluorescence dot plot shows resolution of live, apoptotic, and dead cells, which are quantified using the Flowjo software. The cell-cycle analysis is done by treating the cells with AMG 925 for 24 hours followed by using the CycleTest Kit. Ten thousand events are acquired and the proportions of cells in each cycle phase are calculated using the ModFit software

    In VivoIn AML tumor –bearing mice, administration of AMG 925 shows inhibition of P-STAT5 and P-RB as well as cell growth both in subcutaneous MOLM13 xenograft tumor model and systemic MOLM13-Luc xenograft tumor model. AMG 925 is also reported to have antitumor activity in a dose-dependent manner in theRB-positive Colo205 colon adenocarcinoma xenograft model.
    Animal modelMOLM13 tumor-bearing mice
    Formulation & Dosage12.5, 25, or 37.5 mg/kg; oral
    ReferencesMol Cancer Ther. 2014 Apr;13(4):880-9


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    AMG 925

    Activity of AMG 925 in subcutaneous MOLM13 xenograft tumor model.Mol Cancer Ther. 2014 Apr;13(4):880-9.

    AMG 925

    Activity of AMG 925 in systemic MOLM13-Luc xenograft tumor model. Mol Cancer Ther. 2014 Apr;13(4):880-9.

    AMG 925

    Activity of AMG 925 in Colo205 xenograft tumor model. Mol Cancer Ther. 2014 Apr;13(4):880-9.


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