Axitinib

Modify Date: 2024-01-06 18:58:57

Axitinib structure	Common Name	Axitinib
	CAS Number	319460-85-0	Molecular Weight	386.470
	Density	1.4±0.1 g/cm3	Boiling Point	668.9±55.0 °C at 760 mmHg
	Molecular Formula	C₂₂H₁₈N₄OS	Melting Point	213-215ºC
	MSDS	Chinese USA	Flash Point	358.3±31.5 °C
	Symbol	GHS07, GHS09	Signal Word	Warning

Use of Axitinib

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.

Name	axitinib
Synonym	More Synonyms

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.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR Research Areas >> Cancer
Target	VEGFR1:0.1 nM (IC50) VEGFR2:0.2 nM (IC50) VEGFR3:0.1 nM (IC50) PDGFRβ:1.6 nM (IC50)
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].
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].
Cell Assay	Endothelial or tumor cells are starved for 18 h in the presence of either 1% FBS (HUVEC) or 0.1% FBS (tumor cells). Axitinib is added and cells are incubated for 45 min at 37°C in the presence of 1 mM Na3VO4. The appropriate growth factor is added to the cells, and after 5 min, cells are rinsed with cold PBS and lysed in the lysis buffer and a protease inhibitor cocktail. The lysates are incubated with immunoprecipitation antibodies for the intended proteins overnight at 4°C. Antibody complexes are conjugated to protein A beads and supernatants are separated by SDS-PAGE[2].
Animal Admin	Mice and Rats[2] Mice with M24met xenograft tumors (400-600 mm3) are administered with a single dose of Axitinib or the control (0.5% carboxymethylcellulose/H2O). Blood and tumor tissue samples are collected for pharmacokinetic and VEGFR-2 measurements. Total protein concentrations in tumor tissues are determined using the Bradford colorimetric assay. Six-day-old Sprague-Dawley rats are given two i.p. injections of Axitinib (30 mg/kg ). Animals are sacrificed, retinas are collected and lysed, and immunoprecipitation/immunoblotting experiments are done. ECL-Plus is used for detection and densitometry analysis is done using the Alpha Imager 8800.
References	[1]. Fenton BM, et al. The addition of AG-013736 to rractionated radiation improves tumor response without functionally normalizing the tumor vasculature. Cancer Res. 2007 Oct 15;67(20):9921-8. [2]. Hu-Lowe DD, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83 [3]. Allen E, et al. Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. Cell Rep. 2016 May 10;15(6):1144-60.

Density	1.4±0.1 g/cm3
Boiling Point	668.9±55.0 °C at 760 mmHg
Melting Point	213-215ºC
Molecular Formula	C₂₂H₁₈N₄OS
Molecular Weight	386.470
Flash Point	358.3±31.5 °C
Exact Mass	386.120117
PSA	95.97000
LogP	4.15
Vapour Pressure	0.0±2.0 mmHg at 25°C
Index of Refraction	1.728
Storage condition	-20°C Freezer

Axitinib MSDS(Chinese)

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H302-H400
Precautionary Statements	P273
Hazard Codes	Xn,N
Risk Phrases	22-50/53
Safety Phrases	60-61
RIDADR	UN 3077 9 / PGIII
HS Code	2933990090

Precursor 2
CAS#:100-69-6 2-Vinylpyridine CAS#:885126-34-1 2-((3-IODO-1H-I...
DownStream 0

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Heparan sulfate D-glucosaminyl 3-O-sulfotransferase-3B1 (HS3ST3B1) promotes angiogenesis and proliferation by induction of VEGF in acute myeloid leukemia cells.

J. Cell. Biochem. 116(6) , 1101-12, (2015)

Heparan sulfate (HS) are complex polysaccharides that reside on the plasma membrane of almost all mammalian cells, and play an important role in physiological and pathological conditions. Heparan sulf...

Involvement of corneal lymphangiogenesis in a mouse model of allergic eye disease.

Invest. Ophthalmol. Vis. Sci. 56 , 3140-8, (2015)

The contribution of lymphangiogenesis (LA) to allergy has received considerable attention and therapeutic inhibition of this process via targeting VEGF has been considered. Likewise, certain inflammat...

Chronic inflammation, lymphangiogenesis, and effect of an anti-VEGFR therapy in a mouse model and in human patients with aspiration pneumonia.

J. Pathol. 235(4) , 632-45, (2015)

Chronic inflammation induces lymphangiogenesis and blood vessel remodelling. Since aged pneumonia patients often have repeated episodes of aspiration pneumonia, the pathogenesis may involve chronic in...

N-Methyl-2-({3-[(E)-2-(2-pyridinyl)vinyl]-1H-indazol-6-yl}sulfanyl)benzamide

Benzamide, N-methyl-2-[[3-[(E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-

UNII-C9LVQ0YUXG

Inlyta

Benzamide, N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-

10mg

Axitinib (usan)

N-Methyl-2-({3-[(E)-2-(pyridin-2-yl)vinyl]-1H-indazol-6-yl}sulfanyl)benzamide

AG-013736 N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide

Axtinib

AVERMECTINB

Axitinib

N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide

[14C]-Axitinib

DC Chemicals Limited
China
Product Name: Axitinib
Price: $150.0/100mg $300.0/250mg $600.0/1g
Purity: 98.0%
Stocking Period: 3 Day
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Zhejiang Hangyu API Co., Ltd
China
Product Name: Axitinib
Price: ￥Inquiry/1kg
Purity: 99.5%
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Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: Axitinib
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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Axitinib

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