CAS No. : 1025720-94-8

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For research use only. Not Intended for Therapeutic Use!
Cat No:I000168
Molecular Formula:C₂₅H₁₉ClF₂N₄O₄
Molecular Weight:512.89
IC50:3.9/1.1/1.8/4.3 nM (c-Met/Axl/Ron/Tyro3) [1]
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Appearance:white solid powder
Purity: > 98%
Cat No:I000168
Cas No:1025720-94-8

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
IC50 value: 3.9/1.1/1.8/4.3 nM (c-Met/Axl/Ron/Tyro3) [1]
Target: c-Met/Axl/Ron/Tyro3
in vitro: BMS-777607 is a selective ATP-competitive Met kinase inhibitor which potently blocks the autophosphorylation of c-Met with IC50 of 20 nM in GTL-16 cell lysates, and demonstrates selective inhibition of proliferation in Met-driven tumor cell lines, such as GTL-16 cell line, H1993 and U87 [1]. BMS-777607 inhibits hepatocyte growth factor (HGF)-triggered c-Met autophosphorylation with IC50 of <1 nM in PC-3 and DU145 prostate cancer cells. BMS 777607 has little effect on tumor cell growth, but exhibits inhibitory effect on HGF-induced cell scattering in PC-3 and DU145 cells, with almost complete inhibition at 0.5 μM. BMS 777607 also suppresses stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 0.1 μM) in both cell lines [2]. Application of BMS 777607 (~10 μM) to the highly metastatic murine KHT cells for 2 hours potently eliminates basal levels of autophosphorylated c-Met with IC50 of 10 nM without affecting the total c-Met, leading to dose-dependent inhibition of phosphorylation of downstream signaling molecules including ERK, Akt, p70S6K and S6. Treatment with BMS-777607 (~1 μM) for 24 hours potently inhibits the KHT cell scatter, motility and invasion at doses in the nanomolar range which consists with MET gene knockdown, and modestly affects cell proliferation and colony formation [3].
in vivo: Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity [1]. Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control [3].

1:Inhibiting receptor tyrosine kinase AXL with small molecule inhibitor BMS-777607 reduces glioblastoma growth, migration, and invasion in vitro and in vivo. Onken J, Torka R, Korsing S, Radke J, Krementeskaia I, Nieminen M, Bai X, Ullrich A, Heppner F, Vajkoczy P.Oncotarget. 2016 Mar 1;7(9):9876-89. doi: 10.18632/oncotarget.7130. PMID: 26848524 Free PMC Article
2:BMS-777607 promotes megakaryocytic differentiation and induces polyploidization in the CHRF-288-11 cells. Nurhayati RW, Ojima Y, Taya M.Hum Cell. 2015 Apr;28(2):65-72. doi: 10.1007/s13577-014-0102-2. Epub 2014 Oct 11. PMID: 25304900
3:Discovery of novel type II c-Met inhibitors based on BMS-777607. Zhang W, Ai J, Shi D, Peng X, Ji Y, Liu J, Geng M, Li Y.Eur J Med Chem. 2014 Jun 10;80:254-66. doi: 10.1016/j.ejmech.2014.04.056. Epub 2014 Apr 21. PMID: 24792774
4:Prevention of BMS-777607-induced polyploidy/senescence by mTOR inhibitor AZD8055 sensitizes breast cancer cells to cytotoxic chemotherapeutics. Sharma S, Yao HP, Zhou YQ, Zhou J, Zhang R, Wang MH.Mol Oncol. 2014 May;8(3):469-82. doi: 10.1016/j.molonc.2013.12.014. Epub 2014 Jan 2. PMID: 24444656 Free Article
5:Synergistic activities of MET/RON inhibitor BMS-777607 and mTOR inhibitor AZD8055 to polyploid cells derived from pancreatic cancer and cancer stem cells. Zeng JY, Sharma S, Zhou YQ, Yao HP, Hu X, Zhang R, Wang MH.Mol Cancer Ther. 2014 Jan;13(1):37-48. doi: 10.1158/1535-7163.MCT-13-0242. Epub 2013 Nov 14. PMID: 24233399 Free Article
6:Small-molecule inhibitor BMS-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents. Sharma S, Zeng JY, Zhuang CM, Zhou YQ, Yao HP, Hu X, Zhang R, Wang MH.Mol Cancer Ther. 2013 May;12(5):725-36. doi: 10.1158/1535-7163.MCT-12-1079. Epub 2013 Mar 6. PMID: 23468529 Free Article
7:Constitutively active c-Met kinase in PC-3 cells is autocrine-independent and can be blocked by the Met kinase inhibitor BMS-777607. Dai Y, Siemann DW.BMC Cancer. 2012 May 28;12:198. doi: 10.1186/1471-2407-12-198. PMID: 22639908 Free PMC Article
8:Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation. Dai Y, Bae K, Pampo C, Siemann DW.Clin Exp Metastasis. 2012 Mar;29(3):253-61. doi: 10.1007/s10585-011-9447-z. PMID: 22286523
9:BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Dai Y, Siemann DW.Mol Cancer Ther. 2010 Jun;9(6):1554-61. doi: 10.1158/1535-7163.MCT-10-0359. Epub 2010 Jun 1. PMID: 20515943 Free Article
10:Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. Schroeder GM, An Y, Cai ZW, Chen XT, Clark C, Cornelius LA, Dai J, Gullo-Brown J, Gupta A, Henley B, Hunt JT, Jeyaseelan R, Kamath A, Kim K, Lippy J, Lombardo LJ, Manne V, Oppenheimer S, Sack JS, Schmidt RJ, Shen G, Stefanski K, Tokarski JS, Trainor GL, Wautlet BS, Wei D, Williams DK, Zhang Y, Zhang Y, Fargnoli J, Borzilleri RM.J Med Chem. 2009 Mar 12;52(5):1251-4. doi: 10.1021/jm801586s. PMID: 19260711
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