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(1261432-00-1)Related Product Information

• Axitinib Impurity c
• Axitinib Impurity a
• BenzaMide, 2-[(3-iodo-1H-indazol-6-yl)thio]-N-Methyl-
• Axitinib Impurity d
• Axitinib Impurity 27
• Axitinib Impurity 23
• Axitinib Impurity 3
• Axitinib Impurity 26
• Axitinib Impurity 10
• Axitinib Impurity 4
• Axitinib Impurity 20
• Axitinib Impurity 18
• Axitinib Impurity 13
• 2-(1H-indazol-6-ylthio)-N-Methyl- BenzaMide
• Axitinib Impurity 3
• Axitinib Impurity 19
• Axitinib Impurity 14
• Axitinib Impurity 32