Axitinib NEW
| Price | Get Latest Price |
| Package | 25KG |
| Min. Order: | 1KG |
| Supply Ability: | 50000KG/month |
| Update Time: | 2023-10-10 |
Product Details
| Product Name: Axitinib | CAS No.: 319460-85-0 |
| EC-No.: 638-771-6 | Min. Order: 1KG |
| Purity: 99% | Supply Ability: 50000KG/month |
| Release date: 2023/10/10 |
| CAS: | 319460-85-0 |
| MF: | C22H18N4OS |
| MW: | 386.47 |
| EINECS: | 638-771-6 |
| Product Categories: | Pfizer compounds;API;All Inhibitors;Inhibitors;AG 013736;chemical;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators;319460-85-0 |
| Mol File: | 319460-85-0.mol |
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| Axitinib Chemical Properties |
| Melting point | 213-215°C |
| Boiling point | 668.9±55.0 °C(Predicted) |
| density | 1.4 |
| storage temp. | room temp |
| solubility | DMSO: ≥8mg/mL |
| pka | 12.70±0.40(Predicted) |
| form | powder |
| color | white to tan |
| Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| InChIKey | RITAVMQDGBJQJZ-FMIVXFBMSA-N |
| CAS DataBase Reference | 319460-85-0(CAS DataBase Reference) |
| Description | Axitinib is a VEGFR inhibitor (IC50s = 1.2, 0.25, and 0.29 nM for VEGFR1, -2, and -3, respectively). It also inhibits c-Kit and PDGFRβ (IC50s = 1.7 and 1.6 nM, respectively). It inhibits VEGF-induced migration of and tube formation by human umbilical vein endothelial cells (HUVECs). Axitinib (1-100 mg/kg) reduces microvessel density, a marker of angiogenesis, and tumor growth in MV522 colon carcinoma, A375 melanoma, SN12C-GFP renal carcinoma, and U87 glioma mouse xenograft models in a dose-dependent manner. Formulations containing axitinib have been used in the treatment of renal cell carcinoma. |
| 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 |
| Biochem/physiol Actions | Axitinib (AG-013736) is an orally available, potent (picomolar) and selective tyrosine kinase inhibitor that blocks VEGF receptors 1, 2 and 3. The drug blocks VEGF-mediated endothelial cell survival, tube formation, and downstream signaling through endothelial nitric oxide synthase, Akt and extracellular signal-regulated kinase. |
| Clinical Use | Sold under the brand name Inlyta® by Pfizer, Inc., axitinib was approved by the FDA in January 2012 for the treatment of advanced renal cell carcinoma (RCC), specifically after the failure of other systemic treatments. Axitinib slows cancer cell proliferation by inhibition of the vascular endothelial growth factor (VEGF)/VEGF receptor tyrosine (RTK) signaling pathway. In particular, axitinib is a potent inhibitor of VEGF/RTK 1-3, which selectively slows angiogenesis, vascular permeability, and blood flow in solid tumors. |
Packing &shipping&Payment
Packing:25kg/drum
Shipping:by sea or by air
Payment:T/T,western union,moneygram
Packaging Details drum
Port:Tianjin
Lead Time :
Shipping:by sea or by air
Payment:T/T,western union,moneygram
Packaging Details drum
Port:Tianjin
Lead Time :
| Quantity(Kilograms) | 1 - 10000 | >10000 |
| Est. Time(days) | 5 | To be negotiated |
Company information
Hebei Mojin Biotechnology Co., Ltd, Our company is a professional in 4'-Methylacetophenone,Levamisole hydrochloride ,N-Methylformamide and other chemical reagents research and development production enterprises. Our business covers more than 30 countries, most of the big customers come from Europe, America and other countries in the world, we can guarantee the quality and price. In recent decades, with the efforts of all employees, we have established many cooperative companies in shandong, henan, guangdong and other places. Our corporate purpose is based on the market, enhance the strength, take the road of scientific and environmental sustainable development, relying on the country. Technology r & d center, increase the investment in r & d, based on the domestic market, expand the international market, manufacturing quality products, sincere service to the society, into a modern, ecological, scientific and technological enterprise world.
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China- Since: 2017-12-08
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