A selective VEGFR2 inhibitor
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Labeled Version(s)
35055Apatinib-d8
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Apatinib

Item No. 21268

Technical Information
Formal Name
N-[4-(1-cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide
CAS Number
811803-05-1
Synonyms
  • YN968D1
Molecular Formula
C24H23N5O
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 1 mg/ml
λmax
236, 261, 345 nm
SMILES
O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC=C(C4(C#N)CCCC4)C=C3
InChi Code
InChI=1S/C24H23N5O/c25-17-24(11-1-2-12-24)19-5-7-20(8-6-19)29-23(30)21-4-3-13-27-22(21)28-16-18-9-14-26-15-10-18/h3-10,13-15H,1-2,11-12,16H2,(H,27,28)(H,29,30)
InChi Key
WPEWQEMJFLWMLV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Apatinib is a tyrosine kinase inhibitor that potently suppresses the kinase activity of vascular endothelial growth factor 2 (VEGFR2; IC50 = 1 nM).1 It is less effective against c-kit (IC50 = 429 nM), Ret (IC50 = 13 nM), and c-src (IC50 = 53 nM) and does not inhibit EGFR, Her-2, or FGFR1 (IC50s = >10 µM).1 Apatinib has been shown to inhibit the proliferation, migration, and tube formation of human umbilical vein endothelial cells stimulated by fetal bovine serum and, either alone, or in combination with chemotherapeutic agents, prevented the growth of several established human tumor xenograft models.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tian, S., Quan, H., Xie, C., et alYN968D1 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. 102(7), 1374-1380 (2011).