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Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret, c-Kit and c-Src, respectively. Apatinib can induce autophagy and apoptosis.
Brand: BCM
Target: VEGFR2; RET
In Vitro: Apatinib (YN968D1) potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. YN968D1 suppress the activities of Ret, c-kit and c-src with an IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. YN968D1 had no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM. YN968D1 effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring
Boiling Point: 578.2±50.0 °C at 760 mmHg
Flashing Point: 303.5±30.1 °C
Vapour Pressure: 0.0±1.6 mmHg at 25°C
Solubility: Soluble in DMSO. Insoluble in Water.
Isomeric SMILES: C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4
InChIKey: WPEWQEMJFLWMLV-UHFFFAOYSA-N
InChI: 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)
Attribute [Chem Name] N-[4-(1-cyanocyclopentyl)phenyl]-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide [Synonym] Apatinib; Rivoceranib; YN968D1 [CAS No.] 811803-05-1 [Formula] C24H23N5O [Molecular] 397.47 [Form] Solid Powder [Storage] Stored at -20°C
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