| Company Name: |
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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| Tel: |
18818260767 |
| Email: |
sales@chemegen.com |
| Products Intro: |
Product Name:Axitinib-13C-d3
CAS:1261432-00-1
Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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| Company Name: |
Manhag Testing Technology Co., Ltd
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| Tel: |
400-818 0104 18918165978 |
| Email: |
zilin.ren@bestown.net.cn |
| Products Intro: |
Product Name:Axitinib-[13C,d3]
CAS:1261432-00-1
Purity:1mg Package:1mg
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| | Axitinib-13C-d3 Basic information |
| Product Name: | Axitinib-13C-d3 | | Synonyms: | Axitinib-13C-d3;[13C,2H3]-Axitinib;(E)-N-(methyl-13C-d3)-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)benzamide;Axitinib-[13C,D3] (Standard) | | CAS: | 1261432-00-1 | | MF: | C22H15D3N4OS | | MW: | 390.48 | | EINECS: | | | Product Categories: | | | Mol File: | 1261432-00-1.mol |  |
| | Axitinib-13C-d3 Chemical Properties |
| density | 1.357±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: soluble | | form | A solid | | color | White to off-white |
| | Axitinib-13C-d3 Usage And Synthesis |
| Description | Axitinib-13C-d3 is intended for use as an internal standard for the quantification of axitinib by GC- or LC-MS. 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. | | Uses | Axitinib-13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50 values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively[1][2]. | | References | [1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. DOI:10.1177/1060028018797110
[2] 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.;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;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. DOI:10.1016/j.celrep.2016.04.029 |
| | Axitinib-13C-d3 Preparation Products And Raw materials |
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