Apatinib-d8 (free base)

• UNSPSC Description:

  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].

• Target Antigen:

  Autophagy; c-Kit; RET; Src; VEGFR

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  Autophagy;Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Purity:

  92.56

• Solubility:

  DMSO : 30 mg/mL (ultrasonic;warming)

• 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

• Molecular Weight:

  405.52

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.|[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.|[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.|[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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  No Development Reported

• CAS Number:

  2468771-43-7