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Home > Inhibitors & Agonists > Tyrosine Kinase > VEGFR

XL-999(Tyrosine kinase-IN-1)

  Cat. No.:  DC12371   Featured
Chemical Structure
705946-27-6
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More than 5000 active chemicals with high quality for research!
Field of application
XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the proliferation of some tumor cells.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 705946-27-6
Synonyms: XL999,XL 999
SMILES: O=C1NC2=C(C=C(NC3CCN(CC)CC3)C=C2)/C1=C(C4=CC=CC(F)=C4)/C5=NC=C(C)N5
Formula: C26H28FN5O
M.Wt: 445.22
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: XL-999(Tyrosine kinase-IN-1) is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
Target: Flt-1:4 nM (IC50) KDR:20 nM (IC50) PDGFRα:4 nM (IC50) FGFR1:2 nM (IC50)
In Vivo: Tyrosine kinase-IN-1 shows a reasonable PK profile (AUC(0–∞)=1.9, t1/2=4.6 h). It has a favorable oral bioavailability (F=63%) in rats[1].
In Vitro: Tyrosine kinase-IN-1 is from reference (compound 8K)[1].
Kinase Assay: Kinase Inhibition Assays Kinase activities of KDR and PDGFRα are measured as the percent of ATP consumed following the kinase reaction using luciferaseluciferin-coupled chemiluminescence. Kinase reactions are initiated by combining test compound (Tyrosine kinase-IN-1), ATP, kinases and substrates in a 20 mL volume using 384-well microtiter plates. For KDR, the final reaction mixture contained 3 mM ATP, 1.6 mM poly(Glu, Tyr) 4:1 and 1.5 nM KDR of residues D807-V1356 with an N-terminal GST tag. For PDGFRα, the final reaction mixture contained 2 mM ATP, 10 mM MBP and 14 nM PDGFRα of residues Q551-L1089 with an N-terminal GST tag. The reaction mixture is incubated at room temperature for 4 h (KDR) or 2 h PDGFRα before a 20 mL aliquot of Kinase Glo is added and luminescence signal is measured using a Victor2 plate reader. Total ATP consumption is limited below 50%[1].
References: [1]. Moon K, et al. The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 22 (2012) 4979–4985
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC12371 XL-999(Tyrosine kinase-IN-1) XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the proliferation of some tumor cells.
DC1082 ZM306416 ZM306416 is a vascular endothelial growth factor receptor (VEGFR) antagonist.
DC1097 XL-184 (Cabozantinib,BMS907351) XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
DC11268 VEGFR2 kinase inhibitor I(SU-5408) VEGFR2 kinase inhibitor I(SU-5408)is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase (IC50 = 70 nM).
DC3134 Vandetanib (ZD6474) Vandetanib (Zactima, ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
DC9586 Telatinib Telatinib(Bay 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
DC12256 TAS-115 mesylate (TAS-115 methanesulfonate) TAS-115 mesylate is a potent VEGFR and c-Met/HGFR kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
DC3146 Sunitinib malate Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
DC9781 SU4312(NSC86429) SU4312(NSC86429) is a selective, cell-permeable inhibitor of VEGFR2 and PDGFR tyrosine kinases (IC50s = 0.8 and 19.4 μM, respectively).
DC7509 SU1498 SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1with an IC50 of value of 700 nM.
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