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Axitinib

  Cat. No.:  DCAPI1524   Featured
Chemical Structure
319460-85-0
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More than 5000 active chemicals with high quality for research!
Field of application
Axitinib is a non-selective receptor kinase inhibitor of Flt and Flk proteins. This compound also inhibits VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively. Axitinib is studied as an ant
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 319460-85-0
Chemical Name: Axitinib
Synonyms: Axitinib;Axitinib (usan);D03218;Axitinib(AG 013736);Axtinib;N-Methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzaMide;Inlyta;Axitinib (TINIBS);(E)-N-Methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)benzamide;[14C]-Axitinib;Afatinib;AG-010376;Axitinib (AG-013736, Inlyta®); AG013736;AG-013736 N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide;AVERMECTINB;AG-013736;N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide
SMILES: CNC(C1C=CC=CC=1SC1=CC=C2C(=NNC2=C1)C=CC1C=CC=CN=1)=O
Formula: C22H18N4Os
M.Wt: 386.469522953033
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
In Vivo: A single oral dose of Axitinib (100 mg/kg) markedly suppresses murine VEGFR-2 phosphorylation for up to 7 h compared with control tumors. Axitinib rapidly inhibits VEGF-induced vascular permeability in the skin of mice; the inhibition is dose-dependent and directly correlated with drug concentration in mice. Pharmacokinetic/pharmacodynamic analysis indicate an unbound EC50 of 0.46 nM. Similar inhibitory effects are also shown in the skin of MV522 tumor-bearing mice without exogenous VEGF-A stimulation. Axitinib inhibits the growth of human xenograft tumors in mice. Axitinib produces dose-dependent growth delay regardless of initial tumor size, model type, or implant site[2].
In Vitro: Axitinib (AG-013736) is a potent and selective inhibitor of VEGFR 1 to 3. In transfected or endogenous RTK-expressing cells, Axitinib potently blocks growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 with average IC50 values of 0.2 and 0.1 to 0.3 nM, respectively. Cellular activity against VEGFR-1 is 1.2 nM (measured in the presence of 2.3% bovine serum albumin), equivalent to an absolute IC50 of ~0.1 nM, based on protein binding of Axitinib. The potency against murine VEGFR-2 (Flk-1) in Flk-1-transfected NIH-3T3 cells is 0.18 nM, similar to that of its human homologue. Axitinib shows ~8- to 25-fold higher IC50 against the closely related type III and V family RTKs, including PDGFR-β (1.6 nM), KIT (1.7 nM), and PDGFR-α (5 nM); nanomolar concentrations of Axitinib blocks PDGF BB-mediated human glioma U87MG cell (PDGFR-β-positive) migration but not proliferation[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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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