| Identification | Back Directory | [Name]
N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide methanesulfonate | [CAS]
1218779-75-9 | [Synonyms]
YN 968D1
Apatinib methanesulfonate
Apatinib Mesylate(YN968D1)
N-(4-(1-cyanocyclopentyl)phenyl)-2-((pyridin-4-ylmethyl)amino)nicotinamide methanesulfonic acid
N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide methanesulfonate
N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide methanesulfonate ISO 9001：2015 REACH | [EINECS(EC#)]
1592732-453-0 | [Molecular Formula]
C24H23N5O.CH4O3S | [MOL File]
1218779-75-9.mol | [Molecular Weight]
493.578 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
≥49.4 mg/mL in DMSO; insoluble in H2O; ≥2.17 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [Water Solubility ]
Water: Insoluble |
| Hazard Information | Back Directory | [Biological Activity]
apatinib （yn968d1）is a potent inhibior of the vegf signaling pathway with the ic50 value of 1nm for vegfr-2 in in vitro enzyme experiments [1].. | [in vitro]
apatinib has shown the inhibition of tyrosine kinase activities with the ic50 values of 0.013μm, 0.429μm and 0.53μm for ret, c-kit and c-src, respectively. in addition, apatinib has been revealed to have no significant effects in egfr, her-2 or fgfr1 in concentrations up to 10μm. apart from these, apatinib has been reported to inhibit the growth factor-stimulated receptor phosphorylation at the cellular level. furthermore, apatinib has also reported to slightly inhibitor proliferation of huvec by 20% fbs with the ic50 value of 23.4μm and significantly inhibit stimulated by 20ng/ml vegf with the ic50 value of 0.17μm. once-daily oral administration of apatinib has been noted to produce a dose-dependent inhibition of tumor growth in human tumor xenografts in immunodeficient mice [1] | [storage]
Store at -20°C | [References]
[1] tian s1, quan h, xie c, guo h, lü f, xu y, li j, lou l. 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. |
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