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Axitinib

FDA approved axitinib use of treating advanced kidney cancer
Axitinib
Axitinib structure
CAS No.
319460-85-0
Chemical Name:
Axitinib
Synonyms
10mg;D03218;Inlyta;Axtinib;AXITINIB;AG 013736;AsifTinney;AVERMECTINB;Axitinib API;Axitinib Base
CBNumber:
CB81011728
Molecular Formula:
C22H18N4OS
Formula Weight:
386.47
MOL File:
319460-85-0.mol

Axitinib Properties

Melting point:
213-215°C
Density 
1.4
storage temp. 
-20°C Freezer
solubility 
DMSO: ≥8mg/mL
form 
powder
color 
white to tan
CAS DataBase Reference
319460-85-0(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn,N
Risk Statements  22-50/53
Safety Statements  60-61
RIDADR  UN 3077 9 / PGIII
WGK Germany  3
HS Code  29333990
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
H400 Very toxic to aquatic life Hazardous to the aquatic environment, acute hazard Category 1 Warning P273, P391, P501
Precautionary statements:
P273 Avoid release to the environment.

Axitinib price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich PZ0193 Axitinib ≥98% (HPLC) 319460-85-0 5mg $106 2018-11-13 Buy
Cayman Chemical 13813 Axitinib ≥98% 319460-85-0 100mg $118 2018-11-13 Buy
Cayman Chemical 13813 Axitinib ≥98% 319460-85-0 50mg $62 2018-11-13 Buy
Cayman Chemical 13813 Axitinib ≥98% 319460-85-0 500mg $496 2018-11-13 Buy

Axitinib Chemical Properties,Uses,Production

FDA approved axitinib use of treating advanced kidney cancer

January 27, 2012, the FDA approved axitinib for the treatment of advanced kidney cancer (renal cell carcinoma) which other drugs unanswer . Inlyta is manufactured and sold by Pfizer,and is a oral pill taken twice a day.
Renal cell carcinoma is a type of tumor originating from the tubular endothelial cells. Axitinib can prevent certain protein called kinases playing a role in tumor growth and metastasis .
Axitinib is a small molecule tyrosine kinase inhibitor, effective against multiple targets, including VEGF receptors 1, 2 and 3.
Dr. Richard Pazdur, hematology and oncology drugs office director of FDA Drug Evaluation and Research Centre, said: "This is the seven kind of drugs allowed treating metastatic or advanced renal cell carcinoma since 2005 . Overall, during this time ,record level of drug development has dramatically changed the treatment of metastatic renal cell carcinoma paradigm, and offers a variety of treatment options for patients. "
In recent years, the drug has been approved for the treatment of kidney cancer include sorafenib (2005), sunitinib (2006), temsirolimus(2007), everolimus (2009), bevacizumab(2009) and pazopanib(2009).
The above information is edited by the chemicalbook of Tian Ye.

Description

In January 2012, the US FDA approved axitinib (also referred to as AG-013736) for the treatment of advanced renal cell carcinoma (RCC) for patients who have not responded to prior therapy. Axitinib is a pan VEGF inhibitor and functions by binding to the intracellular tyrosine kinase catalytic domain of VEGF leading to blockade of signaling through this angiogenic pathway. Axitinib is50–400 times more potent for VEGF (enzyme Ki and cellular IC50s for VEGF 1, 2, and 3 are ~0.1 nM) than first-generation inhibitors like sorafenib and sunitinib. Axitinib also inhibits c-Kit and PDGFR(α/β) with enzyme Ki's of ~2 nM and was selective when tested against a broad panel of other protein kinases. Axitinib was discovered by a structure-based drug design approach and binds to the kinase domain of VEGF in a DFG-out conformation. Axitinib blocks VEGF-2 phosphorylation up to 7 h postdose in vivo and inhibits endothelial cell proliferation in xenograft tumors implanted in mice. Synthetic routes to axitinib employing a Migita coupling to form the diaryl sulfide and a Heck reaction to install the 2-styrylpyridine moiety have been reported.

Chemical Properties

Off-White Solid

Originator

Pfizer (United States)

Uses

A tyrosine kinase inhibitor; used in cancer therapy.

Uses

Axitinib (AG-013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ 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.

Uses

Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ 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.

Uses

Axitinib is a tyrosine kinase inhibitor. Axitinib is used in cancer therapy.

Definition

ChEBI: An indazole substituted at position 3 by a 2-(pyridin-2-yl)vinyl group and at position 6 by a 2-(N-methylaminocarboxy)phenylsulfanyl group. Used for the treatment of advanced renal cell carcinoma after failure of a first line systemic tr atment.

brand name

Inlyta

Enzyme inhibitor

This orally bioavailable anti-angiogenesis agent (FW = 386.47 g/mol; CAS 319460-85-0), also known by its code name AG013736, its trade name Inlyta?, and its systematic name N-methyl-2-[[3-[ (E) -2-pyridin-2- ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide, is a tyrosine kinase inhibitor that targets vascular endothelial growth factor receptors VEGFR-1 (IC50 = 0.1 nM), VEGFR-2 (IC50 = 0.3 nM), and VEGFR-3 (IC50 = 0.1-0.3 nM), as well as platelet-derived growth factor receptor, or PDGFR (IC50 = 1.6 nM), and cKIT, or CD117 (IC50 = 1.7 nM). Axitinib is cytostatic in xenograft models for breast cancer, renal cell carcinoma, and other tumors, presumably by acting as a vasculature-disrupting agent, or VDA . After inhibition of VEGF signaling, some normal capillaries regress in a systematic sequence of events initiated by a cessation of blood flow and followed by apoptosis of endothelial cells, migration of pericytes away from regressing vessels, and formation of empty basement membrane sleeves that can facilitate capillary regrowth. A Phase-3 trial indicates its superiority in prolonging progression-free survival (PFS) in previously treated renal cell carcinoma (RCC) patients, with axitinib-treated patients exhibiting a median PFS of 6.7 months versus 4.7 months for sorafenib. Axitinib potently inhibits CYP1A2, Ki = 0.11 μM.

Axitinib Preparation Products And Raw materials

Raw materials

Preparation Products


Axitinib Suppliers

Global( 237)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3203 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21930 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20680 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32457 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24196 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 209 58
Xiamen AmoyChem Co., Ltd
+86 (0)592-605 1114
sales@amoychem.com CHINA 6374 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 20516 58
Hebei Huanhao Biotechnology Co., Ltd.
86-0311-83975816 whatsapp +8618034554576
86-0311-83975816 grace@hbhuanhao.com CHINA 701 58

View Lastest Price from Axitinib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-15 Axitinib
319460-85-0
US $7.00 / KG 1KG 99% 100KG career henan chemical co
2019-04-18 Axitinib
319460-85-0
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.
2019-01-04 Axitinib cas 319460-85-0 (whatsapp:+8618830163278)
319460-85-0
US $14.00 / kg 1kg 99.8% 18tons Hebei Huanhao Biotechnology Co., Ltd.

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