Axitinib NEW

Price	$5	$0.1
Package	1KG	1000KG

Min. Order:	1KG
Supply Ability:	g-kg-tons, free sample is available
Update Time:	2024-03-26

Product Details

Product Name: Axitinib	CAS No.: 319460-85-0
Min. Order: 1KG	Purity: 98%
Supply Ability: g-kg-tons, free sample is available	Release date: 2024/03/26
Lead time: In stock, ready for shipment	Packaging: bag/bottle/drum/IBC
Delivery: By express, by air, by sea	Origin: Manufacturer, advantage product
COA, MSDS: Available, contact us for details	Name: Tina

1. Materials information

Names

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%

2. Packaging of materials

For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.

Or smaller package 1kg/bottle, 10kgs/bottle as request.

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3. Shipping & Delivery

By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

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By Air

Provide airport to airport service

Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

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By Sea

Provide seaport to seaport service

Suitable for goods over 100kg

Delivery: 2-45 days

Cost: low cost

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4. Contact information

For more details, pls contact us freely.

Email address: Tina@fdachem.com

Mob: 86 15225627621

WhatsApp/Skype/Wechat/LINE: 86 15225627621

Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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