2468771-43-7
Chemical Structure
Apatinib-d8 free base
Synonym(s): YN968D1-d8 free base
- CAS No.: 2468771-43-7
- Formula:C24H15D8N5O
- Molecular Weight:405.52
IUPAC Name: N-(4-(1-cyanocyclopentyl-2,2,3,3,4,4,5,5-d8)phenyl)-2-((pyridin-4-ylmethyl)amino)nicotinamide
InChIKey: WPEWQEMJFLWMLV-MMBGVTJSSA-N
SMILES: O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC=C(C4(C#N)C([2H])([2H])C([2H])([2H])C([2H])([2H])C4([2H])[2H])C=C3
Biological Activity: Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Apatinib-d8 free base | 92.03% | Apatinib-d8 (free base) is the deuterium labeled Apatinib free base. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. | ||||||||||||||||||||
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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
- [2]. Roviello G, et al. Apatinib: A novel receptor tyrosine kinase inhibitor for the treatment of gastric cancer. Cancer Lett. 2016 Mar 28;372(2):187-91. [Content Brief]
- [3]. Scott LJ. Apatinib: A Review in Advanced Gastric Cancer and Other Advanced Cancers. Drugs. 2018 May;78(7):747-758. doi: 10.1007/s40265-018-0903-9. [Content Brief]
- [4]. Tian S, et al. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80. [Content Brief]
