Apatinib (YN968D1) mesylate - 10mM in DMSO , Vascular endothelial growth factor receptor 2 inhibitor, CAS No.1218779-75-9, Vascular endothelial growth factor receptor 2 inhibitor

CAS: 1218779-75-9 Cat. No.: A408044 Peso molecular: 493.58 Número EC: 881-162-7

GRADE & PURITY 10mM in DMSO

Synonyms

Rivoceranib mesylate | N-​[4-​(1-​cyanocyclopentyl)​phenyl]​-​2-​[(4-​pyridinylmethyl)​amino]​-3-​pyridinecarboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis
In vitro

Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGFR2. Apatinib can also potently suppress the activities of Ret, c-kit and c-src with IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). Apatinib effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. Apatinib reverses ABCB1- and ABCG2-mediated MDR by inhibiting their transport function, but not by blocking the AKT or ERK1/2 pathway or downregulating ABCB1 or ABCG2 expression. Apatinib significantly potentiates the cytotoxicity of established ABCB1 and ABCG2 substrates and increased the accumulation of DOX and Rho 123 in ABCB1- or ABCG2-overexpressing cells. Furthermore, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [¹²⁵I]iodoarylazidoprazosin in a concentration-dependent manner.

In vivo

Apatinib inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner. Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model. Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts.
Cell Data

cell lines：A375 cells

Concentrations：~25 μM

Incubation Time：72 h

Powder Purity:≥99%

Specifications

Sinónimos

Rivoceranib mesylate | N-​[4-​(1-​cyanocyclopentyl)​phenyl]​-​2-​[(4-​pyridinylmethyl)​amino]​-3-​pyridinecarboxamide

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

INHIBITOR

Mecanismo de acción

Vascular endothelial growth factor receptor 2 inhibitor

Nombres e identificadores

• Isómeros SMILES: CS(=O)(=O)O.C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4
• Peso molecular: 493.58
• Reaxy-Rn: 24083150
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24083150&ln=

Objetivos asociados (humanos)

KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: Insoluble; Water: Insoluble; Ethanol: Insoluble